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(2S)-5,7-dihydroxy-2-(2-hydroxy-1-(phenylsulfonyl)propan-2-yl)-9-methyl-3,4-dihydro-1H-benzo[7]annulen-6(2H)-one
-
-
(2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoic acid
-
-
(4-N,N-dimethylaminobenzoyl)-2-hydroxy-1-naphthyl hydrazone
-
specific
(5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
-
(6,6,12,12,18,18,18-heptaoxido-5,7,11,13,17-pentaoxa-6l5,12l5,18l5-triphosphaoctadec-1-yl)phosphonate
-
-
1,2-bis(2-oxopropoxy)anthracene-9,10-dione
-
9% inhibition
1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione
-
20% inhibition
1,2-dihydroxyanthracene-9,10-dione
-
i.e. alizarine, 8% inhibition
1,3,4,5-tetrahydrogalloylapitol
-
-
1,6,8-trihydroxy-3-methylanthraquinone
-
i.e. frangula-emodin
1,6-bis[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1,6-dibenzyl-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-(2-hydroxyethoxymethyl)-6-(phenylthio)thymine
-
-
1-(3-[[(4-benzyl-5-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]methyl]-4-methoxyphenyl)ethanone
-
-
1-(ethoxymethyl)-3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
1-(ethoxymethyl)-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-benzyl-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-hydroxy-4-((4-(morpholinomethyl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-((4-(pyridin-4-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[3-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[3-(4-morpholinylmethyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[4-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[4-(4-pyridinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[4-(quinolin-3-yl)anilino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[[4-(4-morpholinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[[4-(quinolin-3-yl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
GSK5724, exceptional RNase H inhibitory potency
1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-[([1,1'-biphenyl]-4-yl)methyl]-5-hydroxy-4-oxo-1,4-dihydropyridine-3-carboxylic acid
-
-
1-[[(4-fluorophenyl)methoxy]methyl]-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2-phenyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
-
2',3'-dideoxy-3'-triaz-2-en-2-ium-3-id-1-yl-3,4-dihydrothymidine
-
-
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-guanosine
-
40% inhibition of RNase H at 0.05 microM
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-[2-(4-nitrophenyl)ethyl]guanosine
-
69% inhibition of RNase H at 0.05 microM
2'-deoxy-P-thioguanylyl-(3'->5')-guanosine
-
65% inhibition of RNase H at 0.05 microM
-
2,3,7-trihydroxy-6-(3-nitrobenzyl)cyclohepta-2,4,6-trien-1-one
-
-
2,6-dimethoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2,7-dihydroxy-4-(propan-2-yl)cyclohepta-2,4,6-trien-1-one
2,7-dihydroxy-4-isopropyl-cyclohepta-2,4,6-triene
-
i.e. beta-thujaplicinol
2,7-dihydroxy-4-methyl-5-(2-methylbutanoyl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(4-nitrophenyl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(naphthalen-1-yl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(naphthalen-2-yl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-phenylcyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-[4-(trifluoromethyl)phenyl]cyclohepta-2,4,6-trien-1-one
-
2-(1,2-dihydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(1-benzylamino-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2,3-dihydro-1H-inden-1-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-(2,3-dihydro-1H-inden-2-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-(2,4-dichlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-(2-fluorophenyl)acetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-benzylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-bromobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chloro-4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-cyclohexylacetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-diethylamino-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-ethanesulfonyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-ethylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methylbenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,5-dimethylphenyl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)acetonitrile
-
-
2-(3-bromo-4-methoxybenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
inhibition of enzymatic activity, but no antiviral effect
2-(3-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3-phenylpropanamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(tert-butylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-([1,1'-biphenyl]-4-yl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydro pyrimidin-4-yl)acetonitrile
-
-
2-acetamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-amino-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
-
-
2-amino-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-benzamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-hydroxy-(4H)-isoquinoline-1,3-dione
-
inhibits RNase H in vitro with submicromolar potency
2-hydroxy-4-(2-phenyl)ethylisoquinoline-1,3(2H,4H)-dione
-
enol-form
2-hydroxy-4-(3-phenyl)propylisoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-(4-methylbenzyl)isoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-(4-trifluoromethylbenzyl)isoquinoline-1,3(2H-4H)-dione
-
keto-form
2-hydroxy-4-butylisoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-ethylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-4-isopropylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H, 4H)-dione
-
inhibits RNase H in vitro with nanomolar potency
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione
-
shows antiviral activity
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
2-hydroxy-4-pentylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-4-propylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-6-methoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2-hydroxy-6-phenylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxyisoquinoline-1,3(2H,4H)-dione
2-hydroxyisoquinoline-1,3(2H,4H)-dione magnesium complex
-
-
2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl 5-nitrofuran-2-carboxylate
-
-
2-oxo-2-(phenylamino)ethyl dibenzylcarbamodithioate
-
-
2-oxo-2-(propan-2-yloxy)ethyl 5-nitrofuran-2-carboxylate
-
-
2-oxo-2-(tetrahydrofuran-2-ylamino)ethyl 5-nitrofuran-2-carboxylate
-
-
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl benzyl(phenyl)carbamodithioate
-
-
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl dibenzylcarbamodithioate
-
-
2-oxo-2-[(2-phenylpropan-2-yl)amino]ethyl 5-nitrofuran-2-carboxylate
-
-
2-[(2,3,4-trichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[(2,4-dichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
-
2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[(2-bromo-5-chloro-1-benzothiophen-3-yl)methyl]-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-[(2-methoxy-5-methylphenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
-
-
2-[(2-methyl-1-phenylpropan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(2-methylbutan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(3,4-dichlorophenyl)methyl]-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-[(3-cyanophenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
-
-
2-[(3-cyanophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
-
2-[(4-hydroxybenzyl)(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(cyclohexanecarbonyl)amino]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[2-(2-fluoro-benzylamino)-1-hydroxy-1-methyl-ethyl]-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-[2-(4-bromophenyl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
-
-
2-[2-(biphenyl-4-yl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
-
-
2-[3-(4-chlorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[3-(4-fluorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[4-benzyl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridine
-
-
2-[benzyl(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[bis(4-methoxyphenyl)(phenyl)methoxy]ethyl 2-cyanoethyl dipropan-2-ylphosphoramidoite
-
-
2-[tert-butyl(2-phenylethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-oxo-3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-fluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-methoxybenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(pentafluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(phenyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[2-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[3-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[4-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[2-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[4-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[4-(benzyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
-
-
3'-[(E)-[2-(3,4,5-trihydroxybenzoyl)hydrazinylidene]methyl]biphenyl-4-carboxylic acid
-
-
3,3-dimethyl-2-oxobutyl 5-nitrofuran-2-carboxylate
-
-
3,4-dihydroxy-N'-[(E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
-
3,9,11,14,15-pentahydroxy-7-methoxy-10-methyl-5,6-dihydrobenzo[9,10]tetrapheno[2,3-c]furan-1,8,13(3H)-trione
-
-
3-(benzyloxy)-6-((2'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-(furan-2-yl)-4-(4-methoxybenzyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
-
3-(furan-2-yl)-4-phenyl-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
-
3-cyclopentyl-1,4-dihydroxy-1,8-naphthyridin-2(1H)-one
-
3-hydroxy-1,5,6,7-tetrahydro-2H-cyclopenta[4,5]thieno[2,3-d]pyrimidine-2,4(3H)-dione
-
-
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((3-(tetrahydrofuran-3-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-(4-(pyridin-4-yl)phenoxy)pyrimidine-2,4-(1H,3H)-dione
-
-
3-hydroxy-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrobromide
-
-
3-hydroxy-5,6-dimethylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5-methyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxylic acid
-
-
3-hydroxy-5-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-hydroxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-nitrophenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((40-methyl-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4'-(trifluoromethyl)-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4'-methoxy-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4-(trifluoromethyl)benzoyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4-methylbenzoyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(40-methyl-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(naphthalen-1-ylthio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(p-tolylthio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(phenylthio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-phenylthieno [3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-7-phenylquinazoline-2,4(1H,3H)-dione
-
-
3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-[2-(4-bromophenyl)-2-oxoethoxy]-1,8-dihydroxy-6-methylanthracene-9,10-dione
-
-
3-[4-(2-methyl-imidazo[4,5-c]pyridin-1-yl)-benzyl]-3H-benzothiazol-2-one
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-((3-(ethoxymethyl)-1-hydroxy-5-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,1'-biphenyl]-4-carbonitrile
-
-
4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
4-((cyclopropylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(([1,1'-biphenyl]-4-ylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(3-bromophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(4,4-difluoropiperidin-1-yl)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(4-bromophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(4-chlorophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(cyclohexanecarbonyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(cyclohexylacetyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-carbonyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-yl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-([[4-benzyl-5-(furan-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
-
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
4-acetyl-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-benzoyl-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-benzyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
keto-form; mixture of th mixed ketoenol forms
4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(furan-2-yl)-5-[(4-methoxybenzyl)sulfanyl]-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(furan-2-yl)-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-heptyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
enol form
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
keto-form; mixture of th mixed ketoenol forms
4-tert-butyl-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide
-
-
4-[1-4-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)-piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
35% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
72% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
26% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(morpholin-4-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
0.7% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
22% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1h)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
30% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
34% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
63% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
44% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
41% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
44% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
18% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(thiomorpholin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
74% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
78% inhibition at 0.01 mM
4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid
-
-
4-[5-(benzoylamino)thiophen-2-yl]-2,4-dioxobutanoic acid
-
-
4-[[(4-fluorophenyl)methyl]amino]-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-[[4'-(aminomethyl)biphenyl-4-yl]methyl]-1-hydroxy-1,8-naphthyridin-2(1H)-one
-
-
4-[[4'-(aminomethyl)[1,1'-biphenyl]-4-yl]methyl]-1-hydroxy-1,8-naphthyridin-2(1H)-one
-
-
4-[[4-([4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl]amino)pyrimidin-2-yl]amino]benzonitrile
-
i.e. TMC278 or rilpivirine, enzyme-bound structure, overview
5,6-dimethyl-2-(4-nitrophenyl)thieno[2,3-d]pyrimidin-4(3H)-one
Human immunodeficiency virus type 1 group M subtype B
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylaminoethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylsulfanylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-piperidin-1-ylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-2-imadazol-1-yl-1-methyl ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-isopropenyl-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
i.e. manicol, the alpha-hydroxytroplone potently and specifically inhibits HIV RT ribonuclease H, enzyme-bound structure, overview
5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
-
5-(4-chlorophenyl)-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
5-benzyl-6-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-bromo-6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-6-(4-fluorophenyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
6-( (3'- fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-bis(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dichloro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-difluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',4'-dimethoxy-[1,10-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-[1,1'-biphenyl ] - 4 -yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-2-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-2-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4-bromophenyl)thio)-3-hydroxy-5-iodopyrimidine-2,4(1H,3H)-dione
-
-
6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3',4'-dimethoxy-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3',5'-dimethyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3,5-dimethylbenzoyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3-bromobenzyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-chloro-3'-fluoro-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-fluoro-3'-methyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-fluoro-[1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4-bromobenzyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4-chlorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-(4-fluorobenzoyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4-fluorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-2-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-yl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylmethyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylthio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methoxypyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(ethoxymethyl)-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[(benzyloxy)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[2-(4-fluorophenyl)ethyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[3-(4-fluorophenyl)propyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[4-(4-fluorophenyl)butyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(2,4-difluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(3-chloro-2-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(4-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[3-(4-fluorophenyl)propoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[4-(4-fluorophenyl)butoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-[(4'-chloro[1,1'-biphenyl]-3-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)methyl]-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)methyl]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)oxy]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)sulfanyl]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester
-
i.e. RDS1643, RNase H inhibitor
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl]-2,4-dioxo-5-hexenoic acid ethyl ester
-
i.e. RDS-1643, shows relatively weak but selective inhibitory activity against RNase H
6-[4-(diethylamino)phenoxy]-3-[ethoxy(hydroxy)methyl]-1,4-dihydroxy-1,8-naphthyridin-2(1H)-one
-
7-(4-chlorophenyl)-3-hydroxyquinazoline-2,4(1H,3H)-dione
-
-
7-benzyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
7-benzyl-3-hydroxyhexahydropyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
7-ethyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
8-hydroxy-1,6-naphthyridine-7-carboxylic acid
-
-
9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-(2-oxopropoxy)-9,10-dihydroanthracen-1-yl acetate
-
10% inhibition
9,10-dioxo-2-(prop-2-en-1-yloxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-(prop-2-yn-1-yloxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-[(2-oxopentan-3-yl)oxy]-9,10-dihydroanthracen-1-yl acetate
-
inhibits the RNase H function and is inactive on the DNA polymerase function
9,10-dioxo-2-[(3-oxobutan-2-yl)oxy]-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl diacetate
-
12% inhibition
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate
-
-
actinomycin D
-
limits the enzyme to the first strand synthesis
bis[3-(phosphonatooxy)propyl] phosphate
-
-
delaviridine
-
a nonnucleoside reverse transcriptase inhibitor
Dextran sulfate
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 0.1 nM
-
dihydroxybenzoyl naphthyl hydrazone
-
-
dimethyl 3-(chloromethyl)-5,7-dihydroxy-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
dimethyl 5,7-dihydroxy-3-(methoxymethyl)-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
dimethyl 5,7-dihydroxy-3-methyl-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
ethyl (2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoate
-
-
ethyl (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
selectively inhibits RNase H activity in the low micromolar range
ethyl (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
-
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
ethyl 2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 2-(4-chlorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 4,6-dihydroxy-2,7-dimethyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
ethyl 4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
F3284-8495
-
specific inhibitor with low micromolar potency in vitro
GSK5750
-
active site inhibitor
guanylyl-(3'->5')-guanosine
-
89% inhibition of RNase H at 0.05 microM
manicol
source of manicol is the root bark of a rare Guyanan tree, Dulacia guianeinsis
methyl 2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate
-
-
methyl 4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,10-biphenyl]-4-carboxylate
-
-
methyl 4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
methyl 4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 4-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)benzoate
-
-
methyl 4-amino-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 7-bromo-4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
Mn2+
-
activation at 0.01-1 mM, inhibitory above
N-(3-((2-fluorophenyl)carbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)picolinamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(4-chlorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
-
N-(pyridin-2-yl)-2-(thiophene-2-carboxamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(pyridin-2-yl)-2-[2-(quinolin-6-yl)acetamido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
NaCl
-
inhibits substrate binding by the enzyme, in the samples that are pretreated with DTT, the addition of salt strongly inhibits the reaction and completely eliminates off-register cleavage
P-thioguanylyl-(3'->5')-guanosine
-
50% inhibition of RNase H at 0.05 microM
-
pyrimidinol carboxylic acid
-
-
RDS1643
-
RNase H inhibitor
tenofovir disoproxil
-
a nucleoside reverse transcriptase inhibitor
tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one
-
-
xylan polysulfate
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 8 nM
-
zalcitabine
-
a nucleoside reverse transcriptase inhibitor
zidovudine
-
a nucleoside reverse transcriptase inhibitor
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
-
61% inhibition of RNase H at 0.05 microM
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
-
11% inhibition of RNase H at 0.05 microM
2,7-dihydroxy-4-(propan-2-yl)cyclohepta-2,4,6-trien-1-one
-
inhibition of enzymatic activity, but no antiviral effect
2,7-dihydroxy-4-(propan-2-yl)cyclohepta-2,4,6-trien-1-one
-
-
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
inhibition of enzymatic activity, but no antiviral effect
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
inhibition of enzymatic activity, but no antiviral effect
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxyisoquinoline-1,3(2H,4H)-dione
an active site directed inhibitor, stabilizes RH domain helix E
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
inhibitor indentified by FRET-based high-throughput screening assay
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
-
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
-
inhibitor has little effect on bacterial RNase H activity in vitro
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
-
-
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
-
additionally inhibits HIV-1 replication effectively. Inhibitor has little effect on bacterial RNase H activity in vitro
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
-
-
Abacavir
-
a nucleoside reverse transcriptase inhibitor
beta-thujaplicinol
slow-binding RNase H inhibitor with noncompetitive kinetics that forms a tropylium ion that interacts favorably with reverse transcriptase and the RNA:DNA substrate
beta-thujaplicinol
-
shows submicromolar inhibitory activity against RNase H
beta-thujaplicinol
-
weak inhibition at 0.05 mM
beta-thujaplicinol
a non-competitive inhibitor of RNase H
didanosine
-
a nucleoside reverse transcriptase inhibitor
efavirenz
-
second generation non-nucleoside reverse transcriptase inhibitor, shows the effect of simultaneously reorienting domain motions and obstructing the p66 thumb fluctuations
efavirenz
-
stronger effect of mutation N348I on RNase H susceptibility to nevirapine as compared with efavirenz
efavirenz
-
a nonnucleoside reverse transcriptase inhibitor
Emtricitabine
-
a nucleoside reverse transcriptase inhibitor
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
interactions between MK1 and two Mn2+ ions, which are coordinated by the RNase H active site residues D443, E478, D498, and D549, binding structure, overview. In addition, G444, S499, A538, H539, V552, and S553 contribute to the binding site
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
-
-
Etravirine
-
a nonnucleoside reverse transcriptase inhibitor
heparin
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 0.5-1.5 nM
heparin
-
inhibits substrate binding by the enzyme, in the samples that are pretreated with DTT, the addition of heparin strongly inhibits the reaction and completely eliminates off-register cleavage
lamivudine
-
a nucleoside reverse transcriptase inhibitor
nevirapine
-
non-nucleoside RT inhibitors such as nevirapine interfere directly with the global hinge-bending mechanism that controls the cooperative motions of the p66 fingers and thumb subdomains. The net effect of nevirapine binding is to change the direction of domain movements rather than suppress their mobilities
nevirapine
-
a non-nucleoside RT inhibitor, NNRTI, stronger effect of mutation N348I on RNase H susceptibility to nevirapine as compared with efavirenz
nevirapine
a nonnucleoside reverse transcriptase inhibitor, NNRTI
nevirapine
-
a nonnucleoside reverse transcriptase inhibitor
NSC727447
-
mutation T473C increases sensitivity of the enzyme for NSC727447 by 50fold
NSC727447
Human immunodeficiency virus type 1 group M subtype B
-
raltegravir
-
-
stavudine
-
a nucleoside reverse transcriptase inhibitor
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
-
additionally inhibits DNA strand transfer and DNA polymerase activity of the retroviral reverse transcriptase
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
-
inhibits RNase H activity, does not significantly affect DNA polymerase activity of reverse transcriptase. In the absence of DNA synthesis, [2-(4-chlorophenyl)hydrazinylidene]propanedioic acid interferes with the translocation, or repositioning, of the enzyme on the RNA-DNA template duplex. Inhibitor is highly specific for human immunodeficiency virus. The dicarboxylic acid moiety is essential for activity, and Mg2+ chelates directly with a Kd value of 2.4 mM
additional information
-
synthesis of 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives as inhibitors of the RNase H activity of the reverse transcriptase of HIV-1, docking, study, overview. No inhibition by keto-5i and 5l
-
additional information
-
antiretroviral drugs inhibit the reverse-transcriptase (RT) of HIV. The differences between HIV-1 and HIV-2 RTs explain why some of the anti-HIV-1 drugs are not effective against HIV-2. One major difference between the two HIV RTs is the low ribonuclease H (RNase H) activity of HIV-2 RT relative to HIV-1 RT
-
additional information
-
identification and evaluation of thiocarbamate and triazole inhibitors targeting RNase H activity of HIV reverse transcriptase, overview
-
additional information
-
design, synthesis, and screening of derivatives of 5-nitro-furan-2-carboxylic acid as inhibitors of the RNAse H activity of HIV-1 reverse transcriptase, overview. Modulation of the 5-nitro-furan-2-carboxylic moiety results in a drastic decrease in inhibitory potency. Binding mode of active derivatives, in which three oxygen atoms aligned in a straight form at the nitro-furan moiety are coordinated to two divalent metal ions located at RNase H reaction site. The nitro-furan-carboxylic moiety is one of the critical scaffolds for RNase H inhibition. Cytotoxicity of the synthesized compounds, overview
-
additional information
-
non-nucleoside RT inhibitors, NNRTIs, bind to an allosteric site that is 10 A from the polymerase active site and 60 A from the RNase H active site
-
additional information
-
no inhibition by 5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-piperidin-1-ylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, 5,7-dihydroxy-2-(1-hydroxy-2-imadazol-1-yl-1-methyl ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, 2-(2-diethylamino-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, and 2-(1-benzylamino-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
additional information
structures of naphthyridinone-containing inhibitors bound to the RNase H active site, overview. This class of compounds binds to the active site via two metal ions that are coordinated by catalytic site residues, D443, E478, D498, and D549. The directionality of the naphthyridinone pharmacophore is restricted by the ordering of D549 and H539 in the RNase H domain
-
additional information
-
C-terminal domain mutations reduce RNase H activity either directly by affecting the RNase H cleavage activity of the enzyme, or indirectly by affecting the overall positioning of the template/primer strand, which in turn affects RNase H activity, template switching, polymerization and/or nucleotide excision. Effects of enzyme mutations on treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors, detailed overview. Nucleoside reverse transcriptase inhibitors are nucleoside analogues that lack the 3' OH on the sugar ring and competitively block reverse transcription by causing chain termination during DNA polymerization. Nucleoside reverse transcriptase inhibitors are prodrugs that require intracellular phosphorylation to the 5'-triphosphate formed by host cell kinases in order to become active. Nonnucleoside reverse transcriptase inhibitors in general are non-competitive inhibitors of RT that bind to a hydrophobic pocket near the polymerase active site, inducing conformational changes that inhibit RT enzymatic activity. Inhibition mechanisms of the two inhibitor classes, overview
-
additional information
-
mechanisms of catalysis and drug inhibition of polymerase and RNase H functions of RT by nucleos(t)ide reverse transcriptase inhibitor and non-nucleoside reverse transcriptase inhibitor drugs, and molecular mechanisms of drug resistance, detailed overview
-
additional information
-
discovery and development of bona fide RNase H inhibitors, overview
-
additional information
-
not inhibited by GSK5750
-
additional information
-
design, synthesis and biological evaluations of N-hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H, antiviral activity, overview. The compounds potently and selectively inhibit RNase H with considerable potency against HIV-1 in cell culture. They also show inhibition of integrase strand transfer (INST) activity. Structure-activity-relationship analysis. Molecular modeling of analogues 3-hydroxy-6-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione and 5-(4-chlorophenyl)-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione at the RNase H active site. Analysis of the enzyme's crystal structure in complex with inhibitor 6-benzyl-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
additional information
-
major chemotypes reported as HIV RNase H active site inhibitors, overview. Design, synthesis, biochemical and antiviral evaluations of a 6-arylthio subtype of the 3-hydroxypyrimidine-2,4-dione (HPD) chemotype as inhibitors of the enzyme. The analogues inhibit RT RNase H in single-digit nanomolar range without inhibiting RT polymerase (pol) at concentrations up to 0.01 mM showing high inhibitory selectivity. Many of the analogues also inhibit integrase strand transfer (INST) activity in low to sub micromolar range. Most analogues inhibit HIV progression in low micromolar range without cytotoxicity. Molecular docking and modelling
-
additional information
-
6-biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibit HIV reverse transcriptase-associated RNase H, overview. Design, synthesis, biochemical and antiviral evaluations of a 6-biphenylmethyl subtype of the 3-hydroxypyrimidine-2,4-dione (HPD) chemotype. The subtype potently inhibits RT RNase H in low nanomolar range without inhibiting RT polymerase (pol) or integrase strand transfer (INST) at the highest concentrations tested. A few analogues inhibit HIV in low micromolar range without cytotoxicity at concentrations up to 0.1 mM in cell-based assays. EC50 values and antiviral activity of the compounds, overview
-
additional information
-
pharmacophore-based design and sythesis of 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H, enzyme inhibition shows tolerance of a nonflexible linker, overview. 3-Hydroxypyrimidine-2,4-dione (HPD) subtypes with a nonflexible C-6 carbonyl linkage exhibit potent and selective biochemical inhibitory profiles with strong RNase H inhibition at low nM, weak to moderate integrase strand transfer (INST) inhibition at low micromolecular range, and no to marginal RT polymerase (pol) inhibition up to 0.010 mM. A few analogues also demonstrate significant antiviral activity without cytotoxicity. EC50 values of the compounds, overview
-
additional information
-
3-hydroxypyrimidine-2,4-diones act as selective active site inhibitors of HIV reverse transcriptase-associated RNase H, design, synthesis, and biochemical evaluations, overview. No inhibition by 9z. The activity and selectivity profiles of subtype 11 are manifested with a few selected analogues demonstrating exceptional potency in inhibiting RNase H. Although they also inhibit RT pol, the micromolar activity reflects a sizable selectivity (14-49 fold) strongly favoring RNase H inhibition. The compounds also show inhibition of integrase strand transfer (INST) activity. Molecular modelling
-
additional information
library screening of alpha-hydroxytropolones synthesized through a convenient oxidopyrylium cycloaddition/ring-opening sequence, synthetic alpha-hydroxytropolones act as inhibitors of HIV reverse transcriptase ribonuclease H activity, structure-function analysis, overview. Homology model of substrate- and inhibitor-bound HIV-1 RNase H, molecular docking. beta-Thujaplicinol and manicol share a rare alpha-hydroxytropolone moiety that crystal-structure analysis reveals to be a key for the potent inhibition of the enzyme. Unfortunately, both of these natural products display cytotoxicity in cell-based antiviral assays that precludes cellular antiviral activity. The slight steric change from a methyl to chloromethylene to methoxymethylene decreases the inhibitory potency by close to a full order of magnitude. Enzyme residue Tyr501, which is predicted computationally to be involved in interactions with the side chain, is blocked by the substrate. HIV-1 cytopathicity assays are performed, cytotoxicity of synthetic alpha-hydroxytropolones and beta-thujaplicinol against CEM-SS cells
-
additional information
-
library screening of alpha-hydroxytropolones synthesized through a convenient oxidopyrylium cycloaddition/ring-opening sequence, synthetic alpha-hydroxytropolones act as inhibitors of HIV reverse transcriptase ribonuclease H activity, structure-function analysis, overview. Homology model of substrate- and inhibitor-bound HIV-1 RNase H, molecular docking. beta-Thujaplicinol and manicol share a rare alpha-hydroxytropolone moiety that crystal-structure analysis reveals to be a key for the potent inhibition of the enzyme. Unfortunately, both of these natural products display cytotoxicity in cell-based antiviral assays that precludes cellular antiviral activity. The slight steric change from a methyl to chloromethylene to methoxymethylene decreases the inhibitory potency by close to a full order of magnitude. Enzyme residue Tyr501, which is predicted computationally to be involved in interactions with the side chain, is blocked by the substrate. HIV-1 cytopathicity assays are performed, cytotoxicity of synthetic alpha-hydroxytropolones and beta-thujaplicinol against CEM-SS cells
-
additional information
-
extracts of Uvaria angolensis from tropical zone of Cameroon (Mount Kalla in Yaounde City) are a promising source of inhibitors of HIV-1 reverse transcriptase-associated RNA-dependent DNA polymerase (RDDP) and HIV-1 RNase H functions. Usage of stem bark methanol extract that inhibits both HIV-1 RNase H function and RDDP activity with IC50 values of 0.001 mg/ml and 0.00062 mg/ml, respectively, and, after been fractionated with different solvents, its solid residue shows an IC50 of 0.00010 mg/ml and of 0.00023 mg/ml against RNase H and RDDP, respectively. Methanol and water extracts from leaves and twigs, are also effective but much less than stem bark extracts. Determination of cytotoxicity
-
additional information
-
binding mode and resistance profile for a dual-target pyrrolyl diketo acid scaffold against HIV-1 integrase and reverse-transcriptase-associated ribonuclease H (RNase H), using wild-type and mutant enzymes, and detail energy components contribution of calculated binding free energies of studied inhibitors binding to HIV-1 IN and RNase H wild-types and mutants, overview
-
additional information
Human immunodeficiency virus type 1 group M subtype B
inhibitor library screening, identification and synthesis of cycloheptathiophene-3-carboxamide derivatives as allosteric HIV-1 ribonuclease H inhibitors, binding mode of compounds 2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one, 2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, and 2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, overview
-
additional information
Human immunodeficiency virus type 1 group M subtype B
development and evaluation of inhibitors against the RNase H active site of HIV-1 reverse transcriptase. The RNase H active site of HIV-1 RT is sufficiently different from the active sites of the two cellular human enzymes, RNase H1 and RNase H2, that compounds can be developed as selective inhibitors of viral RH. Antiviral activities of compounds XZ456, XZ460, XZ462, and MK463 against wild-type enzyme and against HIV-1 vectors that carry well-known INSTI, NNRTI, and NRTI resistance mutations, overview. XZ456 and XZ460 both inhibit these NRTI mutants with efficacies similar to their antiviral activities against wild-type HIV-1. Conversely, the NRTI-resistant mutants cause a 3 to 4fold reduction in susceptibility to XZ462 and MK463. Compounds are tested in viral replication and cytotoxicity assays. For enzyme-inhibitor structural modelling, coordinates of the following retroviral RT-RT inhibitor structures are used: HIV RT-MK1 (PDB ID 3LP0) and HIV RT-MK2 (PDB ID 3LP1). The compounds target the catalytic magnesium ions in the HIV-1 RNase H
-
additional information
-
inhibitory potency and binding of dumbbell oligonucleotides to MoMuL virus RNase H, overview. The best dumbbell oligonucleotide, inhibitor contained phosphorothioate residues in both the loops
-
additional information
-
magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain, overview. 2-Hydroxyisoquinoline-1,3(2H,4H)-dione forms a 1:1 complex with Mg2+, but a 1:2 complex with Mn2+,
-
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0.00051
(2S)-5,7-dihydroxy-2-(2-hydroxy-1-(phenylsulfonyl)propan-2-yl)-9-methyl-3,4-dihydro-1H-benzo[7]annulen-6(2H)-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.0193
(5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0192
(5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.087
(5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0161
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.028
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0077
(5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.075
1,6,8-trihydroxy-3-methylanthraquinone
Human immunodeficiency virus 1
-
-
0.013
1,6-bis[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.015
1,6-dibenzyl-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0008
1-(3-[[(4-benzyl-5-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]methyl]-4-methoxyphenyl)ethanone
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0021
1-(ethoxymethyl)-3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.025
1-(ethoxymethyl)-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
above, pH and temperature not specified in the publication
0.01
1-benzyl-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
1-hydroxy-4-((4-(morpholinomethyl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000079
1-hydroxy-4-((4-(pyridin-4-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.0002
1-hydroxy-4-([[3-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000398
1-hydroxy-4-([[3-(4-morpholinylmethyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.0001
1-hydroxy-4-([[4-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000016
1-hydroxy-4-([[4-(4-pyridinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.0007
1-hydroxy-4-[4-(quinolin-3-yl)anilino]pyrido[2,3-d]pyrimidin-2(1H)-one
0.00005
1-hydroxy-4-[[4-(4-morpholinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000003
1-hydroxy-4-[[4-(quinolin-3-yl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0062
1-[[(4-fluorophenyl)methoxy]methyl]-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.04
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
Human immunodeficiency virus 1
-
-
0.04
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-[2-(4-nitrophenyl)ethyl]guanosine
Human immunodeficiency virus 1
-
-
0.0215
2,6-dimethoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0006
2,7-dihydroxy-4-(propan-2-yl)cyclohepta-2,4,6-trien-1-one
Human immunodeficiency virus 1
-
-
0.0019
2-(1,2-dihydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00096
2-(1-benzylamino-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.0061
2-(2,3-dihydro-1H-inden-1-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0055
2-(2,3-dihydro-1H-inden-2-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.01224
2-(2,4-dichlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0099
2-(2-(2-fluorophenyl)acetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01488
2-(2-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0013
2-(2-benzylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00457
2-(2-bromobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0075
2-(2-chloro-4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0239
2-(2-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0671
2-(2-cyclohexylacetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0005
2-(2-diethylamino-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00024
2-(2-ethanesulfonyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00038
2-(2-ethylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.01373
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.1
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid
Human immunodeficiency virus type 1 group M subtype B
above, pH 7.8, 37°C
0.02189
2-(2-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01425
2-(2-methoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0183
2-(2-methylbenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.05348
2-(2-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0012
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
Human immunodeficiency virus 1
-
-
0.00084
2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00401
2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0037
2-(3,5-dimethylphenyl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)acetonitrile
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0009
2-(3-bromo-4-methoxybenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
Human immunodeficiency virus 1
-
-
0.02047
2-(3-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0146
2-(3-phenylpropanamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.02143
2-(4-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01778
2-(4-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00472
2-(4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.02047
2-(4-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.018
2-(tert-butylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.00076
2-([1,1'-biphenyl]-4-yl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydro pyrimidin-4-yl)acetonitrile
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.1
2-acetamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
above, pH 7.8, 37°C
0.0071
2-amino-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.002
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0201
2-amino-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0148
2-benzamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0668
2-hydroxy-4-(3-phenyl)propylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.08
2-hydroxy-4-(4-methylbenzyl)isoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0427
2-hydroxy-4-(4-trifluoromethylbenzyl)isoquinoline-1,3(2H-4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0132
2-hydroxy-4-butylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0388
2-hydroxy-4-ethylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0185
2-hydroxy-4-isopropylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.000061
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H, 4H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000061
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione
Moloney murine leukemia virus
-
pH 8.0, 37°C
0.0388 - 0.07
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
0.0336
2-hydroxy-4-pentylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0468
2-hydroxy-4-propylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.001507
2-hydroxy-6-methoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0013
2-hydroxy-6-phenylisoquinoline-1,3(2H,4H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00012 - 0.0591
2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0301
2-hydroxyisoquinoline-1,3(2H,4H)-dione magnesium complex
Moloney murine leukemia virus
-
pH 8.0, 37°C
0.0043
2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0019
2-oxo-2-(phenylamino)ethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0132
2-oxo-2-(propan-2-yloxy)ethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0042
2-oxo-2-(tetrahydrofuran-2-ylamino)ethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0266
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl benzyl(phenyl)carbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0033
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0082
2-oxo-2-[(2-phenylpropan-2-yl)amino]ethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0033
2-[(2,3,4-trichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.0058
2-[(2,4-dichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0019
2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
0.00017
2-[(2-bromo-5-chloro-1-benzothiophen-3-yl)methyl]-5,6-dihydroxypyrimidine-4-carboxylic acid
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0083
2-[(2-methoxy-5-methylphenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0043
2-[(2-methyl-1-phenylpropan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0058
2-[(2-methylbutan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0114
2-[(3-cyanophenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0047
2-[(3-cyanophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.005
2-[(4-hydroxybenzyl)(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0166
2-[(cyclohexanecarbonyl)amino]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0012
2-[2-(2-fluoro-benzylamino)-1-hydroxy-1-methyl-ethyl]-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.021
2-[2-(4-bromophenyl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.1
2-[2-(biphenyl-4-yl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0099
2-[3-(4-chlorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0145
2-[3-(4-fluorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0017
2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine
0.0026
2-[4-benzyl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridine
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0077
2-[benzyl(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0142
2-[tert-butyl(2-phenylethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0098
2-[tert-butyl(3-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.05
2-[tert-butyl(3-oxo-3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.05
2-[tert-butyl(3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0085
2-[tert-butyl(4-fluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0075
2-[tert-butyl(4-methoxybenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0069
2-[tert-butyl(4-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0068
2-[tert-butyl(pentafluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0009
2-[tert-butyl(phenyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.009
2-[tert-butyl[2-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0085
2-[tert-butyl[3-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.008
2-[tert-butyl[4-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0128
2-[[2-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0087
2-[[4-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.05
2-[[4-(benzyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0011 - 0.0041
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
0.0007 - 0.0034
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
0.0009 - 0.0067
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
0.0012 - 0.0069
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
0.0001
3'-[(E)-[2-(3,4,5-trihydroxybenzoyl)hydrazinylidene]methyl]biphenyl-4-carboxylic acid
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0219
3,3-dimethyl-2-oxobutyl 5-nitrofuran-2-carboxylate
Human immunodeficiency virus 1
-
pH 7.5, 37°C
0.0081
3-(benzyloxy)-6-((2'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0065
3-(furan-2-yl)-4-(4-methoxybenzyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0047
3-(furan-2-yl)-4-phenyl-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0001
3-hydroxy-1,5,6,7-tetrahydro-2H-cyclopenta[4,5]thieno[2,3-d]pyrimidine-2,4(3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0014 - 0.0041
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
0.0095
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0036 - 0.0089
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
0.0062
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0017 - 0.0072
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
0.0027 - 0.0066
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
0.0037 - 0.01
3-hydroxy-1-methyl-6-(4-(pyridin-4-yl)phenoxy)pyrimidine-2,4-(1H,3H)-dione
0.0001
3-hydroxy-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0003
3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrobromide
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
3-hydroxy-5,6-dimethylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
3-hydroxy-5-methyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxylic acid
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
3-hydroxy-5-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
3-hydroxy-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.011
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00024 - 0.00049
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
0.0012 - 0.0038
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0025 - 0.013
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0028 - 0.0093
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0028 - 0.022
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.000012
3-hydroxy-6-((2-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000017
3-hydroxy-6-((2-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000037
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000007
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000025
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000008
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0009 - 0.015
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.00022 - 0.00043
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
0.0057
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0006 - 0.0043
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.001 - 0.017
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0008 - 0.0051
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.00015 - 0.00025
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
0.002 - 0.016
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.000005
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000013
3-hydroxy-6-((3-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000013
3-hydroxy-6-((3-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000013
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000007
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000047
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000039
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00038 - 0.0038
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.00018 - 0.00045
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
0.0039 - 0.021
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.000004
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0023 - 0.022
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0005 - 0.0031
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0002 - 0.0004
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
0.0004 - 0.0047
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0013 - 0.0066
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
0.0016 - 0.012
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
0.000006
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0004 - 0.0007
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
0.000031
3-hydroxy-6-((4-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000011
3-hydroxy-6-((4-hydroxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000012
3-hydroxy-6-((4-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000012
3-hydroxy-6-((4-nitrophenyl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000006
3-hydroxy-6-((40-methyl-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000026
3-hydroxy-6-(4'-(trifluoromethyl)-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00053
3-hydroxy-6-(4'-methoxy-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000081
3-hydroxy-6-(4-(trifluoromethyl)benzoyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000093
3-hydroxy-6-(4-methylbenzoyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000021
3-hydroxy-6-(40-methyl-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000007
3-hydroxy-6-(naphthalen-1-ylthio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000033
3-hydroxy-6-(p-tolylthio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000016
3-hydroxy-6-(phenylthio)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
3-hydroxy-6-phenylthieno [3,2-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000084
3-hydroxy-6-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
3-hydroxy-7-phenylquinazoline-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.029
3-[2-(4-bromophenyl)-2-oxoethoxy]-1,8-dihydroxy-6-methylanthracene-9,10-dione
Human immunodeficiency virus 1
-
-
0.0012 - 0.0037
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
0.0011 - 0.0037
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
0.0019 - 0.013
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
0.0025 - 0.011
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
0.0052
4'-((3-(ethoxymethyl)-1-hydroxy-5-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000024
4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000398
4-((cyclopropylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.00001
4-(([1,1'-biphenyl]-4-ylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000501
4-(4,4-difluoropiperidin-1-yl)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000032
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.004
4-([[4-benzyl-5-(furan-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0002 - 0.2
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
0.0149
4-benzyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0012
4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole
0.00021
4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole
0.001
4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole
0.0038
4-benzyl-3-(furan-2-yl)-5-[(4-methoxybenzyl)sulfanyl]-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0028
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(furan-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
0.006
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.001 - 0.0059
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
0.001
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.045
4-heptyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0078 - 0.038
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
0.0035
4-tert-butyl-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0066
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0068
4-[1-[(4-fluorophenyl)methyl]-7-(morpholin-4-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0033
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0262
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0185
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0287
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0057
4-[1-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
Human immunodeficiency virus 1
-
in 50 mM Tris-HCl, pH 8.0, at 37°C
0.0032
4-[5-(benzoylamino)thiophen-2-yl]-2,4-dioxobutanoic acid
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000158
4-[[(4-fluorophenyl)methyl]amino]-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
in 50 mM Tris, pH 8.0, 80 mM KCl, 10 mM MgCl2, at 22°C
0.000045
4-[[4'-(aminomethyl)biphenyl-4-yl]methyl]-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0012
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylaminoethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00093
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylsulfanylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00082
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-piperidin-1-ylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00911
5,7-dihydroxy-2-(1-hydroxy-2-imadazol-1-yl-1-methyl ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00068
5,7-dihydroxy-2-(1-hydroxy-ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
Human immunodeficiency virus 1
-
pH 8.0, 37°C
0.00004
5-(4-chlorophenyl)-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.015
5-benzyl-6-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00007
5-bromo-6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.017
5-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-6-(4-fluorophenyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0038 - 0.0296
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
0.0026 - 0.0322
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
0.000028
6-( (3'- fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000085
6-((2',4'-bis(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0000092
6-((2',4'-dichloro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000015
6-((2',4'-difluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.001 - 0.0042
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.00031 - 0.0024
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.0015 - 0.0053
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.0019 - 0.0069
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.00047 - 0.0007
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.0066
6-((2-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.000008
6-((2-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00001
6-((2-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000015
6-((2-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0005 - 0.003
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.000004
6-((3',4'-dimethoxy-[1,10-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0006 - 0.004
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.0016 - 0.0092
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.00019 - 0.00032
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.0067
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000006
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000005
6-((3'-chloro-4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000038
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000015
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000016
6-((3'-chloro-[1,1'-biphenyl ] - 4 -yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00002
6-((3'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0000077
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0000076
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000004
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000018
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000006
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000005
6-((3'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000011
6-((3-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000011
6-((3-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000014
6-((3-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00043
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0000094
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000012
6-((4'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0033 - 0.013
6-((4'-chloro-[1,1'-biphenyl]-2-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.00022 - 0.00045
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.000005
6-((4'-chloro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00047 - 0.00066
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.0024 - 0.011
6-((4'-chloro-[1,1'-biphenyl]-4-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.000007
6-((4'-chloro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0000088
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000011
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000005
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000012
6-((4'-fluoro-[1,1'-biphenyl]-2-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002 - 0.0003
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
0.000005
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000006
6-((4'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0016 - 0.0044
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
0.00012
6-((4-bromophenyl)thio)-3-hydroxy-5-iodopyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00001
6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000012
6-((4-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00001
6-((4-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000037
6-((4-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000074
6-(3',4'-dimethoxy-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000063
6-(3',5'-dimethyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00009
6-(3,5-dimethylbenzoyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000013
6-(3-bromobenzyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000023
6-(4'-chloro-3'-fluoro-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000019
6-(4'-fluoro-3'-methyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000027
6-(4'-fluoro-[1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000011
6-(4-bromobenzyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00007
6-(4-chlorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000085
6-(4-fluorobenzoyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
6-(4-fluorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0047
6-([1,1'-biphenyl]-2-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0011
6-([1,1'-biphenyl]-3-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000017
6-([1,1'-biphenyl]-3-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00085 - 0.0035
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
0.000016
6-([1,1'-biphenyl]-3-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.001
6-([1,1'-biphenyl]-3-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00042
6-([1,1'-biphenyl]-4-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000022
6-([1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0062
6-([1,1'-biphenyl]-4-yl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0008 - 0.0051
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
0.005
6-([1,1'-biphenyl]-4-ylmethyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000016
6-([1,1'-biphenyl]-4-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0019 - 0.006
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
0.00009
6-([1,1'-biphenyl]-4-ylthio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.011
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methoxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.007
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0068
6-benzyl-1-(ethoxymethyl)-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0025
6-benzyl-1-[(benzyloxy)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0066
6-benzyl-1-[2-(4-fluorophenyl)ethyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0038
6-benzyl-1-[3-(4-fluorophenyl)propyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0009
6-benzyl-1-[4-(4-fluorophenyl)butyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0018
6-benzyl-1-[[(2,4-difluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0009
6-benzyl-1-[[(3-chloro-2-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0021
6-benzyl-1-[[(4-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0028
6-benzyl-1-[[3-(4-fluorophenyl)propoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0018
6-benzyl-1-[[4-(4-fluorophenyl)butoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000043
6-benzyl-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00022
6-[(4'-chloro[1,1'-biphenyl]-3-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00025
6-[([1,1'-biphenyl]-4-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00013
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl]-2,4-dioxo-5-hexenoic acid ethyl ester
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
7-(4-chlorophenyl)-3-hydroxyquinazoline-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0001
7-benzyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.00033
7-benzyl-3-hydroxyhexahydropyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0002
7-ethyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.039
9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.013
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.000186 - 0.00047
ARK-2452
-
0.00007 - 0.0038
beta-thujaplicinol
0.01
dolutegravir
Human immunodeficiency virus 1
-
above, pH and temperature not specified in the publication
0.0082
ethyl (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0073
ethyl (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0063
ethyl (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0086
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0112
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.008
ethyl (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.00011
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0252
ethyl 2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.07258
ethyl 2-(4-chlorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0011 - 0.0048
F3284-8495
0.0019 - 0.0022
F3385-2581
0.0007 - 0.0021
F3385-2588
0.0004 - 0.0008
F3385-2590
0.00033
GSK5750
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.000015
methyl 4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,10-biphenyl]-4-carboxylate
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.000031
methyl 4-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)benzoate
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0137
N-(3-((2-fluorophenyl)carbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)picolinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01036
N-(pyridin-2-yl)-2-(thiophene-2-carboxamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01644
N-(pyridin-2-yl)-2-[2-(quinolin-6-yl)acetamido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.004
NSC727447
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01
raltegravir
Human immunodeficiency virus 1
-
above, pH and temperature not specified in the publication
0.0022 - 0.003
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
0.0007
1-hydroxy-4-[4-(quinolin-3-yl)anilino]pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.0007
1-hydroxy-4-[4-(quinolin-3-yl)anilino]pyrido[2,3-d]pyrimidin-2(1H)-one
Human immunodeficiency virus 1
-
enzyme activity reaction with substrates HTS-1-3, pH and temperature not specified in the publication
0.0388
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
Moloney murine leukemia virus
-
pH 8.0, 37°C
0.07
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.00012
2-hydroxyisoquinoline-1,3(2H,4H)-dione
Human immunodeficiency virus 1
-
-
0.0059
2-hydroxyisoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0591
2-hydroxyisoquinoline-1,3(2H,4H)-dione
Moloney murine leukemia virus
-
pH 8.0, 37°C
0.0019
2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.0019
2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0017
2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.0017
2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0011
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0032
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0041
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0007
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0023
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0034
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0009
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0046
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0067
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0012
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0039
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0069
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0014
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0039
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0041
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0036
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0066
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0089
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0017
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0062
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0072
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0027
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0035
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0066
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0037
3-hydroxy-1-methyl-6-(4-(pyridin-4-yl)phenoxy)pyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.01
3-hydroxy-1-methyl-6-(4-(pyridin-4-yl)phenoxy)pyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00024
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00046
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00049
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0012
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0021
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0038
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0025
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.013
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0028
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0089
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0093
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0028
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.022
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0009
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0022
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0043
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.011
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.012
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.015
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00022
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0004
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00043
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0006
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0035
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0043
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.001
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0094
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.017
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0008
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0035
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0051
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00015
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00025
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00025
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.002
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.016
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.016
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00038
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00044
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00045
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00075
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0027
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0038
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00018
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00037
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00045
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0039
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.021
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0023
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.022
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0005
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0026
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0031
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0002
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00025
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0003
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0003
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0004
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0004
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.004
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0047
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0013
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.005
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0066
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0016
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.011
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.012
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0004
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0005
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0007
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0012
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0033
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0037
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0011
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0026
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0037
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0019
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.011
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.013
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0025
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0047
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.011
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0002
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.0002
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
Human immunodeficiency virus 1
-
pH and temperature not specified in the publication
0.2
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0012
4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.0012
4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.00021
4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.00021
4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.001
4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH 8.0, 25°C
0.001
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0059
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
Human immunodeficiency virus 1
-
pH not specified in the publication, temperature not specified in the publication
0.0078
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.038
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
Human Immunodeficiency Virus
-
pH 8.0, 37°C
0.0038
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
Human immunodeficiency virus 1
-
-
0.0084
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
Moloney murine leukemia virus
-
-
0.0265
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
Human immunodeficiency virus 1
-
-
0.0296
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
Human immunodeficiency virus 1
-
-
0.0026
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
Human immunodeficiency virus 1
-
-
0.0086
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
Moloney murine leukemia virus
-
-
0.0267
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
Human immunodeficiency virus 1
-
-
0.0322
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
Human immunodeficiency virus 1
-
-
0.001
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0021
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0042
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00031
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00054
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0024
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0015
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0043
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0053
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0019
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0045
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0069
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00047
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00051
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0007
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0005
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0022
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.003
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0006
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0028
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.004
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0016
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0072
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0092
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00019
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00025
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00032
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0033
6-((4'-chloro-[1,1'-biphenyl]-2-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.013
6-((4'-chloro-[1,1'-biphenyl]-2-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00022
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.00037
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00045
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00047
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0006
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.00066
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0024
6-((4'-chloro-[1,1'-biphenyl]-4-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.011
6-((4'-chloro-[1,1'-biphenyl]-4-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0002
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0003
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0003
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0016
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0038
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0044
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.00085
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0034
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0035
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0008
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0035
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.0051
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.0019
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-1, pH and temperature not specified in the publication
0.0053
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-2, pH and temperature not specified in the publication
0.006
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
Human immunodeficiency virus 1
-
enzyme activity reaction with substrate HTS-3, pH and temperature not specified in the publication
0.000186
ARK-2452
Human immunodeficiency virus 1
-
pH 8.0, 37°C, purified recombinant mutant p51-G-TCR construct
-
0.00047
ARK-2452
Human immunodeficiency virus 1
-
pH 8.0, 37°C, purified recombinant wild-type HIV-1 reverse transcriptase RNase H
-
0.00007
beta-thujaplicinol
Human immunodeficiency virus 1
-
mutant enzyme Y501A, at pH 7.8 and 37°C
0.00009
beta-thujaplicinol
Human immunodeficiency virus 1
-
mutant enzyme N474A, at pH 7.8 and 37°C
0.00015
beta-thujaplicinol
Human immunodeficiency virus 1
-
mutant enzyme R448A, at pH 7.8 and 37°C
0.000176
beta-thujaplicinol
Human immunodeficiency virus 1
-
pH 8.0, 37°C, purified recombinant mutant p51-G-TCR construct
0.00019
beta-thujaplicinol
Human immunodeficiency virus 1
-
mutant enzyme Q475A, at pH 7.8 and 37°C
0.00022
beta-thujaplicinol
Human immunodeficiency virus 1
-
mutant enzyme R557A, at pH 7.8 and 37°C
0.000257
beta-thujaplicinol
Human immunodeficiency virus 1
-
pH 8.0, 37°C, purified recombinant wild-type HIV-1 reverse transcriptase RNase H
0.0038
beta-thujaplicinol
Human immunodeficiency virus 1
-
at pH 7.8 and 37°C
0.0011
F3284-8495
Human immunodeficiency virus 1
-
10 mM Mg2+, at pH 8.0 and 37°C
0.0048
F3284-8495
Human immunodeficiency virus 1
-
1 mM Mg2+, at pH 7.4 and 37°C
0.0019
F3385-2581
Human immunodeficiency virus 1
-
10 mM Mg2+, at pH 8.0 and 37°C
0.0022
F3385-2581
Human immunodeficiency virus 1
-
1 mM Mg2+, at pH 7.4 and 37°C
0.0007
F3385-2588
Human immunodeficiency virus 1
-
10 mM Mg2+, at pH 8.0 and 37°C
0.0021
F3385-2588
Human immunodeficiency virus 1
-
1 mM Mg2+, at pH 7.4 and 37°C
0.0004
F3385-2590
Human immunodeficiency virus 1
-
10 mM Mg2+, at pH 8.0 and 37°C
0.0008
F3385-2590
Human immunodeficiency virus 1
-
1 mM Mg2+, at pH 7.4 and 37°C
0.0022
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
Human immunodeficiency virus 1
-
pH 7.6, 37°C
0.003
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
Human immunodeficiency virus 1
-
pH 7.6, 37°C
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D549A
-
mutation in polypeptide p66, decrease in RNase H activity
D549N
-
mutation in polypeptide p66, decrease in RNase H activity
Q294P
-
site-directed mutagenesis, the Q294P mutant of HIV-2 RT has about 10fold higher RNase H activity than the wild-type. Infectious HIV-2 cannot bear the replacement of the RT's Gln294 by the HIV-1 RT Pro counterpart, as it results in substantially reduced HIV-2 replication and fast reversions to the wild-type Gln294 virus
A360I
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
A360I/V
-
site-directed mutagenesis, a connection/RNase H domain mutant
A360K
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
A400T
-
mutation in the connection domain
A554K
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
A554L
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
A554T
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
C280E
-
RNase H activity similar to wild-type
C280H
-
RNase H activity similar to wild-type
C280L
-
RNase H activity similar to wild-type
C280M
-
RNase H activity similar to wild-type
C280P
-
significant reduction in RNase H activity. A heterodimer p66C280p/p51C280P shows about 8% of wild-type RNaseH activity, 6% of strand transfer activity, and 105% of DNA polymerase activity. A heterodimer p66C280P/p51 shows about 60% of wild-type RNaseH activity, 80% of strand transfer activity, and 100% of DNA polymerase activity. A heterodimer p66/p51C280W shows about 30% of wild-type RNaseH activity, 6% of strand transfer activity, and 99% of DNA polymerase activity
C280Q
-
RNase H activity similar to wild-type
C280R
-
RNase H activity similar to wild-type
C280S/K172A/K173A
-
p66/p51 HIV-1 reverse transcriptase 52A mutant variant, the mutation C208S resides in both subunits, the p66 subunit also contains the mutations K172A and K173A
C280W
-
significant reduction in RNase H activity. A heterodimer p66C280W/p51C280W shows about 11% of wild-type RNaseH activity, 6% of strand transfer activity, and 100% of DNA polymerase activity. A heterodimer p66C280W/p51 shows about 44% of wild-type RNaseH activity, 80% of strand transfer activity, and 98% of DNA polymerase activity. A heterodimer p66/p51C280W shows about 29% of wild-type RNaseH activity, 7% of strand transfer activity, and 100% of DNA polymerase activity
C280Y
-
RNase H activity similar to wild-type
C282S
-
site-directed mutagenesis, the mutation avoids non-specific cross-linking in both subunits, p66 and p51 subunits of HIV-1
D443A
-
site-directed mutagenesis, altered inhibitor binding compared to wild-type enzyme
D549A
-
site-directed mutagenesis, altered inhibitor binding compared to wild-type enzyme
D549N
-
mutation increases the 3'-azido-3'-deoxythymidine concentration needed to inhibit viral replication by 50% 12fold by increasing the time available for excision of incorporated nucleoside reverse transcriptase inhibitors from terminated primers and results in 5- to 10fold reduction in viral titers in a single-replication cycle assay
D67N/K70R/T215F
-
site-directed mutagenesis
D67N/K70R/T215F/Q509L
-
site-directed mutagenesis
E396A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
E399D
-
mutation in the connection domain
E438N
site-directed mutagenesis, the mutation disrupts RNH folding, viral infectivity is eliminated by the mutation
E438N/T477A
site-directed mutagenesis, addition of the T477A mutation restores correct folding of the RNH domain despite the presence of the E438N mutation
E44A
-
mutation involved in lamivudine resistance
E44D
-
mutation involved in lamivudine resistance
E475A
-
site-directed mutagenesis, the mutant shows only minimally altered substrate specificity or enzyme activity compared to the wild-type enzyme. But the efficiency with which most mutants catalyzed polymerization-independent RNase H cleavage is sharply reduced. This deficiency is more pronounced when the mutant enzyme is challenged to process the (+) strand polypurine tract (PPT) primer from either (+) RNA or a PPT/(+) DNA RNA/DNA chimera
E478A
-
site-directed mutagenesis, altered inhibitor binding compared to wild-type enzyme
E478Q/N348I
-
mutation of RNase H active site and connection domain
E89K
-
mutation involved in foscarnet resistance
F160S
-
site-directed mutagenesis
F227L
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
F440A
site-directed mutagenesis, the mutation disrupts RNH folding, viral infectivity is eliminated by the mutation. Molecular dynamics simulations suggest that the T477A mutation affects the processing site by altering relative orientations of secondary structure elements
F440A/T477A
site-directed mutagenesis, addition of the T477A mutation restores correct folding of the RNH domain despite the presence of the F440A mutation
G190S
-
site-directed mutagenesis, the mutant virus shows moderately reduced fitness compared to that of the wild-type virus
G333D
-
mutation in the connection domain
G335C
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
G359A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
G509L
-
Glu to Leu substitution at residue 509 in the ribonuclease H domain of HIV-1 reverse transcriptase confers zidovudine resistance, mechanism, overview. Q509L increases zidovudine monophosphate excision activity of RT on RNA/DNA template/primers, but not DNA/DNA template/primers, due to Q509L decreasing a secondary RNase H cleavage event that reduces the RNA/DNA duplex length to 10 nucleotides and significantly impairs the enzyme's ability to excise the chain-terminating nucleotide. Mutation Q509L does not affect initial rates of the polymerase-directed RNase H activity but only polymerase-independent cleavages that occur after a template/primer dissociation event. Q509L decreases the affinity of the enzyme to bind template/primers with duplex lengths less than 18 nucleotides in the polymerase-independent RNase H cleavage mode, while not affecting the enzyme's affinity to bind the same template/primers in an zidovudine monophosphate excision competent mode
G544Stop
-
C-terminal truncation of p66 polypeptide. Loss of RNase H activity, while dimerization with polypepitde p51 and DNA polymerase activity are not significantly affected
H539F
-
mutation in isolated RNase H domain, mutant fails to bind RNA/DNA hybrids. Structure of mutant is similar to wild-type
H539N
-
increases the 3'-azido-3'-deoxythymidine concentration needed to inhibit viral replication by 50% 180fold relative to wild-type by increasing the time available for excision of incorporated nucleoside reverse transcriptase inhibitors from terminated primers
H539S
-
active site mutant
I505G
-
site-directed mutagenesis, the mutant exhibits a dimerization defect. The efficiency with which most mutants catalyzed polymerization-independent RNase H cleavage is sharply reduced. This deficiency is more pronounced when the mutant enzyme is challenged to process the (+) strand polypurine tract (PPT) primer from either (+) RNA or a PPT/(+) DNA RNA/DNA chimera
K219E
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
K219N
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
K390A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
K395A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
K451R
-
mutation present in viral isolates of 11% of antiviral treatment-experienced patients but remaining 100% conserved among treatment-naive patients
K540A
-
site-directed mutagenesis, altered inhibitor binding compared to wild-type enzyme
K558E
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, associated with an increase in thymidine analogue mutations, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
K558G
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, associated with an increase in thymidine analogue mutations, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
K558R
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, associated with an increase in thymidine analogue mutations, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
K65R/Q151M/A62V/V75I/F77L/F116Y
-
mutation involved in nucleos(t)ide reverse transcriptase inhibitor resistance
L100I
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
L429M/E514L
N-terminal truncated constructs include RHDELTANT, corresponding to p66 residues 429-560 with an N-terminal Leu429Met mutation, an extended linker construct, RHDELTANT-EL, in which an additional Pro-Asp-Gln sequence is introduced into RHDELTANT immediately following Gln512, and RHDELTANT(E514L) in which RHDELTANT contains an E514L substitution in the alphaB-alphaD linker
L469H
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
L469I
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
L469M
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
L469T
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
L74V
-
mutation involved in nucleos(t)ide reverse transcriptase inhibitor resistance
M184V
-
naturally occuring mutation in HIV infection patients, arises with abacavir, emtricitabine, or lamivudine treatment
M230L
-
the naturally occuring mutation leads to reduced RNase H activity of the HIV reverse transcriptase
N474A/Q475A
-
mutation reduces the viral titer 5- to 10fold, , reduction in the efficiency of DNA synthesis. Mutant is less efficient than the wild-type enzyme in its ability to remove a polypurine tract primer from a model substrate and has an altered RNase H cleavage specificity
N494D
-
mutant closely resembles the wild-type RNase H, exhibits an endonuclease activity and a processive RNase H activity, gives rise to small RNA hydrolysis products, and acts in concert with the reverse transcriptase
P236L
-
site-directed mutagenesis, the mutant virus shows substantially reduced fitness compared to that of the wild-type virus
P537Stop
-
C-terminal truncation of p66 polypeptide. Loss of RNase H activity, while dimerization with polypepitde p51 and DNA polymerase activity are not significantly affected
Q151M
-
mutation involved in nucleos(t)ide reverse transcriptase inhibitor resistance
Q151M/A62V/V75I/F77L/F116Y
-
mutation involved in nucleos(t)ide reverse transcriptase inhibitor resistance
Q475E
-
mutant exhibits a retarded endonuclease activity and an impaired 3'-5' processive RNA cleavage activity, gives rise to predominantly larger RNA hydrolysis products, is less processive in the presence of competitor substrate, and is defective in its ability to hydrolyze the polypurine tract and homopolymeric hybrids
Q500A
-
mutation reduces the viral titer less than 2-fold
R557A
-
the mutant shows about 5fold reduced kcat value compared to the wild type enzyme
R557S
-
active site mutant
R72A
-
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type. The R72A mutation might impair the nucleotide-induced conformational change but does not affect the RNase H activity directly, kinetic parameters governing TTP binding and incorporation by the HIVRT mutant, overview. The mutation causes impaired TTP induced conformational change on RNase H activity
T369I
-
mutation in the connection domain
T470E
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
T470K
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
T470P
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
T470S
-
naturally occuring mutation in HIV infection patients, the mutation renders the patient more prevalent amongst treatment-experienced patients, treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors
T473C
-
the mutation increases the sensitivity of the enzyme for inhibitor NSC727447 by 50fold
T473M
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
T477A
site-directed mutagenesis, addition of the T477A mutation restores correct folding of the RNH domain despite the presence of the F440A or E438N mutations
V552Stop
-
C-terminal truncation of p66 polypeptide. Mutant retains endonuclease activity but lacks the directional processing feature of wild-type and barely supports transfer of nascent (-)-stranded DNA between RNA templates
W229F
-
mutation in primer grip residue, specificity of cleavage is not compromised, efficiency is reduced to 33-44% of wild-type
W229F/Y232W
-
mutation in primer grip residues, specificity of cleavage is not compromised, efficiency is reduced to 33-44% of wild-type
W229Y
-
mutation in primer grip residue, specificity of cleavage is not compromised, efficiency is reduced to 33-44% of wild-type
W535A
-
site-directed mutagenesis, altered inhibitor binding compared to wild-type enzyme
W71A
-
site-directed mutagenesis, the mutant is probably less rigidly locked on the substrate DNA/RNA hybrid, parameters governing TTP binding and incorporation by the HIVRT mutant, overview. The mutation causes impaired TTP induced conformational change on RNase H activity
W71D
-
site-directed mutagenesis, the mutant is probably less rigidly locked on the substrate DNA/RNA hybrid, parameters governing TTP binding and incorporation by the HIVRT mutant, overview. The mutation causes impaired TTP induced conformational change on RNase H activity
W88G
-
mutation involved in foscarnet resistance
Y188C
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
Y188L
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
Y229F/Y232F
-
mutation in primer grip residues, specificity of cleavage is not compromised, efficiency is reduced to 33-44% of wild-type
Y232W
-
mutation in primer grip residue, specificity of cleavage is not compromised, efficiency is reduced to 33-44% of wild-type
Y318F
-
mutation in the connection domain
E478Q
-
RNase H active site mutant
-
E478Q/N348I
-
mutation of RNase H active site and connection domain
-
K103N
-
a classic NNRTI resistance mutation
-
N348I
-
connection domain mutant, altered RNase H cleavage pattern compared to the wild-type HIV-1 RT
-
Y181C
-
a classic NNRTI resistance mutation
-
E396A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
-
K390A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
-
K395A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
-
K65R
-
naturally occuring mutation in HIV infection patients, arises with abacavir, didanosine, emtricitabine, lamivudine, or tenofovir disoproxil fumarate treatment
-
M230L
-
the naturally occuring mutation leads to reduced RNase H activity of the HIV reverse transcriptase
-
Y501A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
-
Q294P
-
site-directed mutagenesis of a residue in the catalytically inactive p54 subunit resulting in an increase in RNase H activity comparable with that of HIV-1 reverse transcriptase
D443N
Human immunodeficiency virus type 1 group M subtype B
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
E478Q
Human immunodeficiency virus type 1 group M subtype B
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
G140S/Q148H
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant INSTI
K70R
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NRTI
L100I/K103N
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
M184V
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NRTI
V106A
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
Y181C
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
Y188L
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
D443N
Human immunodeficiency virus type 1 group M subtype B BH10
-
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
-
E478Q
Human immunodeficiency virus type 1 group M subtype B BH10
-
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
-
K70R
Human immunodeficiency virus type 1 group M subtype B BH10
-
site-directed mutagenesis, mutant NRTI
-
M184V
Human immunodeficiency virus type 1 group M subtype B BH10
-
site-directed mutagenesis, mutant NRTI
-
V106A
Human immunodeficiency virus type 1 group M subtype B BH10
-
site-directed mutagenesis, mutant NNRTI
-
Y181C
Human immunodeficiency virus type 1 group M subtype B BH10
-
site-directed mutagenesis, mutant NNRTI
-
Y188L
Human immunodeficiency virus type 1 group M subtype B BH10
-
site-directed mutagenesis, mutant NNRTI
-
D443N
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
E478Q
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
F61A
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
K358R/A359G/S360A
Human immunodeficiency virus type 1 group O subtype B
-
the mutant shows highly increased strand transfer efficiency compared to wild-type
K65R/E478Q
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
L92P
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
L92P/D443N
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows decreased dissociation rate constant (koff) compared to wild-type
L92P/E478Q
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
T355A/Q357M
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
T355A/Q357MK358R/A359G/S360A
Human immunodeficiency virus type 1 group O subtype B
-
the mutant shows highly increased strand transfer efficiency compared to wild-type
V148I
Human immunodeficiency virus type 1 group O subtype B
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
V148I/K358R/A359G/S360A
Human immunodeficiency virus type 1 group O subtype B
-
the mutant shows highly increased strand transfer efficiency compared to wild-type
D443N
Human immunodeficiency virus type 1 group O subtype B ESP49
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
-
E478Q
Human immunodeficiency virus type 1 group O subtype B ESP49
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
-
L92P
Human immunodeficiency virus type 1 group O subtype B ESP49
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
-
V148I
Human immunodeficiency virus type 1 group O subtype B ESP49
-
site-directed mutagenesis, the mutant shows increased dissociation rate constant (koff) compared to wild-type
-
A554S
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
D460N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
D488E
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
D549N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
E529D
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
H539N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
I505A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
I506L
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K451R
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K476A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K476N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K512Q
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K527N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K530R
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K558E
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
K558R
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
L469F
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
L491S
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
N474A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Q475A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Q500A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Q509L
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Q547K
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
T470N
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
T473A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
V518I
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Y501A
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
Y501F
Human immunodeficiency virus type 1 subtype C
-
naturally occurring mutation in the RNase H region of HIV-1 subtype C infected individual
A128T
-
the mutant strain is resistant to 2-hydroxyisoquinoline-1,3(2H,4H)-dione inhibitors in contrast to the wild-type
C635V
-
site-directed mutagenesis, the mutant shows slightly reduced reverse transcriptase and RNAse H activities compared the wild-type enzyme
D583A
-
site-directed mutagenesis, RNase H-inactive mutant, that shows increased intrinsic thermal stability compared to the wild-type enzyme. The mutant loses RNase H activity through abolishing of Mg2+ binding to the RNase H domain
D583N
-
less than 0.5% of wild-type activity, no binding of Mn2+
D653N
-
4% of wild-type activity
E562Q
-
less than 0.5% of wild-type activity, no binding of Mn2+
G140S/Q148H
-
the mutant strain is resistant to 2-hydroxyisoquinoline-1,3(2H,4H)-dione inhibitors in contrast to the wild-type
H638G
-
15% of wild-type activity
D358N
-
mutation eliminates Mg2+- and Mn2+-dependent RNase H function
D426N
-
mutation eliminates Mg2+- and Mn2+-dependent RNase H function
D469N
-
reduced RNase H activity in presence of Mg2+, decrease of turnover rate in presence of Mn2+. Mutant fails to support DNA strand transfer and release of the (+)-strand polypurine tract primer from (+)-RNA
E401Q
-
mutation eliminates Mg2+- and Mn2+-dependent RNase H function
H427A
-
reduced RNase H activity in presence of Mg2+, decrease of turnover rate in presence of Mn2+. Mutant fails to support DNA strand transfer and release of the (+)-strand polypurine tract primer from (+)-RNA
Y459A
-
reduced RNase H activity in presence of Mg2+, decrease of turnover rate in presence of Mn2+. Mutant fails to support DNA strand transfer and release of the (+)-strand polypurine tract primer from (+)-RNA
E478Q
-
mutation in polypeptide p66, loss of RNase H activity
E478Q
-
the efficiency with which mutant RT catalyzes transfer of nascent DNA between RNA templates is severely reduced
A360V
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
A360V
-
naturally occuring mutant from clinical isolates, a connection/RNase H domain mutant that shows reduced RNase H activity
A371V
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B, whereas the G335D and A371V substitutions are commonly observed in 69% and 75% of non-B HIV-1 isolates, respectively
A371V
-
mutation in the connection domain
A371V
-
site-directed mutagenesis, a connection/RNase H domain mutant
A376S
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B. Mutations N348I, A376S and Q509L do confer varying amounts of nevirapine resistance by themselves, even in the absence of excision-enhancing mutations
A376S
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
C280S
-
site-directed mutagenesis
C280S
-
RNase H activity similar to wild-type
D67N
-
mutation involved in zidovudine resistance
D67N
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
E312Q
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B
E312Q
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
E478Q
-
inactive
E478Q
-
mutation in isolated RNase H domain, mutant fails to bind RNA/DNA hybrids. Structure of mutant is similar to wild-type
E478Q
-
RNase H active site mutant
E706Q
-
site-directed mutagenesis of HIV-1 reverse transcriptase, inactive mutant
E706Q
-
site-directed mutagenesis of the recombinant mutant construct G, E706 in construct G corresponds to E478 in HIV-1 reverse transcriptase, inactive mutant
G190A
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
G190A
-
site-directed mutagenesis, the mutant virus shows moderately reduced fitness compared to that of the wild-type virus
G333E
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B
G333E
-
mutation in the connection domain
G335D
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B, whereas the G335D and A371V substitutions are commonly observed in 69% and 75% of non-B HIV-1 isolates, respectively
G335D
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
I505A
-
no discernible effect on viral titer
I505A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
K103N
-
a classic NNRTI resistance mutation
K103N
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
K103N
-
site-directed mutagenesis, the mutant virus shows fitness similar to that of the wild-type virus
K103N
-
site-directed mutagenesis, the mutation does not affect RNase H function
K219Q
-
mutation involved in zidovudine resistance
K219Q
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
K476A
-
mutation reduces the viral titer less than 2fold
K476A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
K476A
-
site-directed mutagenesis, the mutant shows only minimally altered substrate specificity or enzyme activity compared to the wild-type enzyme. But the efficiency with which most mutants catalyzed polymerization-independent RNase H cleavage is sharply reduced. This deficiency is more pronounced when the mutant enzyme is challenged to process the (+) strand polypurine tract (PPT) primer from either (+) RNA or a PPT/(+) DNA RNA/DNA chimera
K65R
-
mutation involved in nucleos(t)ide reverse transcriptase inhibitor resistance
K65R
-
naturally occuring mutation in HIV infection patients, arises with abacavir, didanosine, emtricitabine, lamivudine, or tenofovir disoproxil fumarate treatment
K70R
-
mutation involved in zidovudine resistance
K70R
-
naturally occuring mutation in HIV infection patients, is common to stavudine, tenofovir disoproxil fumarate, and zidovudine therapy
K70R
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
L210W
-
mutation involved in zidovudine resistance
L210W
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-1 pathway
M41L
-
mutation involved in zidovudine resistance
M41L
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-1 pathway
N348I
mutations N348I, A376S and Q509L do confer varying amounts of nevirapine resistance by themselves, even in the absence of excision-enhancing mutations
N348I
-
connection domain mutant, altered RNase H cleavage pattern compared to the wild-type HIV-1 RT
N348I
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
N348I
-
naturally occuring mutant from clinical isolates, a connection/RNase H domain mutant that shows reduced RNase H activity
N474A
-
mutation reduces the viral titer less than 2fold
N474A
-
the mutant shows about 40fold reduced kcat value compared to the wild type enzyme
Q475A
-
mutation reduces the viral titer 5- to 10fold
Q475A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
Q475A
-
the mutant shows about 10fold reduced kcat value compared to the wild type enzyme
Q509L
mutations N348I, A376S and Q509L do confer varying amounts of nevirapine resistance by themselves, even in the absence of excision-enhancing mutations
Q509L
-
mutation in the RNase H domain, the mutation significantly contributes to zidovudine resistance
Q509L
-
site-directed mutagenesis, a connection/RNase H domain mutant
R448A
-
no discernible effect on viral titer
R448A
-
the mutant shows about 3fold reduced kcat value compared to the wild type enzyme
T215F
-
mutation involved in zidovudine resistance
T215F
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-2 pathway
T215Y
-
mutation involved in zidovudine resistance
T215Y
-
thymidine analogue mutation, TAMs, arising with zidovudine and stavudine treatment, take the TAM-1 pathway
T473A
-
mutation abolishes viral replication
T473A
-
site-directed mutagenesis, the mutant shows only minimally altered substrate specificity or enzyme activity compared to the wild-type enzyme. But the efficiency with which most mutants catalyzed polymerization-independent RNase H cleavage is sharply reduced. This deficiency is more pronounced when the mutant enzyme is challenged to process the (+) strand polypurine tract (PPT) primer from either (+) RNA or a PPT/(+) DNA RNA/DNA chimera
V106A
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
V106A
-
site-directed mutagenesis, the mutant virus shows moderately reduced fitness compared to that of the wild-type virus
V365I
the E312Q, G333E, G335D, V365I, A371V and A376S substitutions in RNase H subdomain of HIV-1 reverse transcriptase are present in 26% of subtype B
V365I
-
mutation in the connection domain, the mutation significantly contributes to zidovudine resistance
Y181C
-
a classic NNRTI resistance mutation
Y181C
-
mutation involved in non-nucleoside reverse transcriptase inhibitor resistance
Y181C
-
site-directed mutagenesis, the mutant shows resistance to non-nucleoside reverse transcriptase inhibitors
Y181C
-
site-directed mutagenesis, the mutant virus shows fitness similar to that of the wild-type virus
Y181C
-
site-directed mutagenesis, the mutation does not affect RNase H function
Y501A
-
mutation reduces the viral titer 5- to 10fold, reduction in the efficiency of DNA synthesis. Mutant is less efficient than the wild-type enzyme in its ability to remove a polypurine tract primer from a model substrate and has an altered RNase H cleavage specificity
Y501A
-
naturally occuring mutation in HIV infection patients, the mutation increases zidovudine resistance and decreased reverse trancriptase template switching
Y501A
-
site-directed mutagenesis, the mutant shows only minimally altered substrate specificity or enzyme activity compared to the wild-type enzyme. But the efficiency with which most mutants catalyzed polymerization-independent RNase H cleavage is sharply reduced. This deficiency is more pronounced when the mutant enzyme is challenged to process the (+) strand polypurine tract (PPT) primer from either (+) RNA or a PPT/(+) DNA RNA/DNA chimera
Y501A
-
the mutant shows about 400fold reduced kcat valuecompared to the wild type enzyme
D524A
-
mutant lacks RNase H activity, but retains reverse transcriptase activity. Elimination of RNase H activity enhances the intrinsic thermal stability of the protein rather than its affinity to template-primer
D524A
-
site-directed mutagenesis, RNase H-inactive mutant, that shows increased intrinsic thermal stability compared to the wild-type enzyme. The mutant loses RNase H activity through abolishing of Mg2+ binding to the RNase H domain
D524N
-
less than 0.5% of wild-type activity, no binding of Mn2+
D524N
-
loss of catalytic activity. Construction of vectors encapsidated in virions engineered to contain phenotypic mixtures of wild-type and RNase H catalytic site point mutant D524N reverse transcriptase. There is a steady decline in direct repeat deletion frequency that correlates with decreases in functional RNase H, with greater than fourfold decreases in repeat deletion frequency observed when 95% of virion reverse transcriptase is RNase H defective
additional information
-
an HIV-1 mutant can tolerate an about 10fold higher RNase H activity
additional information
-
naturally occurring polymophisms at position 294 in HIV-2 are Q, E, L, H, and K
additional information
-
chemical modifications by thiol-specific reagents of cysteine 280, located in a helix I in the thumb subdomain of the polymerase domain, affect substantially only the RNase H activity
additional information
-
construction of chimeric HIV-1/HIV-2 reverse transcriptases, in which protein segments and/or subunits are exchanged. The RNase H specific activity of the chimeric enzymes is either high like HIV-1 reverse transcriptase or low like HIV-2 reverse transcriptase. The origin of the thumb subdomain in the small subunit of the chimeric reverse transcriptases, residues 244-322 determines the level of the RNase H activity
additional information
-
construction of two chimeric enzymes by swapping the RNase H domains between HIV-1 RT and Moloney murine leukemia virus MuLV RT. Chimeric HIV-1 RT, having the RNase H domain of MuLV RT, inherits the divalent cation preference characteristic of MuLV RT on the DNA template with no significant change on the RNA template. Chimeric MuLV RT, likewise partially inherits the metal ion preference of HIV-1 RT. Unlike the wild-type MuLV RT, chimeric MuLV RT is able to use both Mn-dNTP and Mg-dNTP on the RNA template with similar efficiency, while a 30-fold higher preference for Mn.dNTP was seen on the DNA template. The metal preferences for the RNase H activity of chimeric HIV-1 RT and chimeric MuLV RT are, respectively, Mn2+ and Mg2+, a property acquired through their swapped RNase H domains. Chimeric HIV-1 RT displays higher fidelity and discrimination against rNTPs than against dNTPs substrates, a property inherited from MuLV RT. The overall fidelity of the chimeric MuLV RT is decreased in comparison to the parental MuLV RT, suggesting that the RNase H domain profoundly influences the function of the polymerase domain
additional information
-
construction of an N-terminally His-tagged mutant p51-G-TCR construct designed to encode the p51 subunit joined by a linker to the thumb (T), connection (C), and RNase H (R) domains of p66, the p51-G-TCR RNase H construct displays Mg2+-dependent activity using a fluorescent nonspecific assay and shows the same cleavage pattern as HIV-1 reverse transcriptase on substrates that mimic the tRNA removal required for second-strand transfer reactions. The RNase H of the p51-G-TCR RNase H construct and wild-type HIV-1 reverse transcriptase have similar Kms for an RNA-DNA hybrid substrate and show similar inhibition kinetics to two known inhibitors of the HIV-1 reverse transcriptase RNase H, molecular modeling
additional information
-
RNase H primer grip mutations suppress polymerization-independent RNase H cleavage. Alteration of RNase H primer grip residues Thr473, Asn474, and Gln475 has little influence on cleavage specificity. Altering the RNase H domain of HIV-1 RT can impact significantly on the ability of mutant enzymes to catalyze DNA synthesis, but all RNase H primer grip mutants show little difference in their DNA-dependent DNA polymerase activity
additional information
effect of N-terminal deletion on monomer-dimer interconversion kinetics, overview. The mutant exhibits large perturbations of the Ile522 and Ile526 resonances corresponding to residues located near the Tyr427 binding pocket, as well as smaller but significant perturbations for several other Ile resonances, consistent with a more subtle, global structural perturbation. As a result of the faster monomer-dimer interconversion rate, even the initial spectrum obtained for the purified dimer sample exhibits significant monomer resonances
additional information
-
effect of N-terminal deletion on monomer-dimer interconversion kinetics, overview. The mutant exhibits large perturbations of the Ile522 and Ile526 resonances corresponding to residues located near the Tyr427 binding pocket, as well as smaller but significant perturbations for several other Ile resonances, consistent with a more subtle, global structural perturbation. As a result of the faster monomer-dimer interconversion rate, even the initial spectrum obtained for the purified dimer sample exhibits significant monomer resonances
additional information
-
mutation of the N-terminal residue of RNase H which is important in the life cycle of HIV-1, change of this residue to several different amino acids. Selection of mutants is based on the N-end rule designation or the structure of the specific amino acid compared to that of the wild-type residue of tyrosine. Compared to wild-type AETF/YVD, the mutants show the following cleavage sites: AETF/MVD, AETF/FVD, AETF/WVD, AETF/TVD, AETF/LVD, AETF/KVD, AETF/AVD, AETF/PVD, AETF/GVD, AETF/SVD, and AETF/VVD, being stabilizing or destabilizing for the N-end rule, packaging and processing of viral polyproteins with RNaseH N-terminal mutations, overview. Reverse transcriptase with an RNase H N-terminal mutation is still degraded in the absence of active viral protease
additional information
-
the isolated RNase H domain of HIV-1 RT (RNHHIV) is inactive, possibly due to the lack of a substrate binding ability, disorder of a loop containing His539, and increased flexibility. To examine whether the activity of RNHHIV is restored by the attachment of TmaHBD or BstNTD to its N-terminus, two chimeric proteins, TmaHBD-RNHHIV and BstNTD-RNHHIV, are constructed and characterized. Both chimeric proteins bind to RNA/DNA hybrid more strongly than RNHHIV and exhibit enzymatic activity in the presence of Mn2+ ions. They do not exhibit activity or exhibited very weak activity in the presence of Mg2+ ions
additional information
-
construction of chimeric HIV-1/HIV-2 reverse transcriptases, in which protein segments and/or subunits are exchanged. The RNase H specific activity of the chimeric enzymes is either high like HIV-1 reverse transcriptase or low like HIV-2 reverse transcriptase. The origin of the thumb subdomain in the small subunit of the chimeric reverse transcriptases, residues 244-322 determines the level of the RNase H activity
additional information
-
construction of chimeric HIV-1/HIV-2 reverse transcriptases, in which protein segments and/or subunits are exchanged. The RNase H specific activity of the chimeric enzymes is either high like HIV-1 reverse transcriptase or low like HIV-2 reverse transcriptase. The origin of the thumb subdomain in the small subunit of the chimeric reverse transcriptases, residues 244-322 determines the level of the RNase H activity
-
additional information
-
construction of chimeric HIV-1/HIV-2 reverse transcriptases, in which protein segments and/or subunits are exchanged. The RNase H specific activity of the chimeric enzymes is either high like HIV-1 reverse transcriptase or low like HIV-2 reverse transcriptase. The origin of the thumb subdomain in the small subunit of the chimeric reverse transcriptases, residues 244-322 determines the level of the RNase H activity
-
additional information
Human immunodeficiency virus type 1 group O subtype B
-
the kinetics of wild-type and mutant enzymes are determined with the RNA/DNA template-primer R33B/20A. Rates of nontemplated nucleotide addition of wild-type and mutant HIV-1 RTs using blunt-ended DNA/DNA substrates, overview. Non-templated nucleotide addition and strand transfer are mechanistically independent
additional information
Human immunodeficiency virus type 1 group O subtype B ESP49
-
the kinetics of wild-type and mutant enzymes are determined with the RNA/DNA template-primer R33B/20A. Rates of nontemplated nucleotide addition of wild-type and mutant HIV-1 RTs using blunt-ended DNA/DNA substrates, overview. Non-templated nucleotide addition and strand transfer are mechanistically independent
-
additional information
Human immunodeficiency virus type 1 subtype C
-
characterization of nucleoside reverse transcriptase inhibitor (NRTI)-associated mutations in the RNase H region of HIV-1 subtype C infected individuals, overview. Mutations are identified by comparing with NRTI-associated RNase H mutations previously identified from subtype B drug-resistance studies
additional information
-
deletion of 204 nucleotides at the 3'-terminus results in 4fold increase in activity level upon recombinant expression and allows for high-level production of the protein
additional information
-
construction of two chimeric enzymes by swapping the RNase H domains between HIV-1 RT and Moloney murine leukemia virus MuLV RT. Chimeric HIV-1 RT, having the RNase H domain of MuLV RT, inherits the divalent cation preference characteristic of MuLV RT on the DNA template with no significant change on the RNA template. Chimeric MuLV RT, likewise partially inherits the metal ion preference of HIV-1 RT. Unlike the wild-type MuLV RT, chimeric MuLV RT is able to use both Mn-dNTP and Mg-dNTP on the RNA template with similar efficiency, while a 30-fold higher preference for Mn.dNTP was seen on the DNA template. The metal preferences for the RNase H activity of chimeric HIV-1 RT and chimeric MuLV RT are, respectively, Mn2+ and Mg2+, a property acquired through their swapped RNase H domains. Chimeric HIV-1 RT displays higher fidelity and discrimination against rNTPs than against dNTPs substrates, a property inherited from MuLV RT. The overall fidelity of the chimeric MuLV RT is decreased in comparison to the parental MuLV RT, suggesting that the RNase H domain profoundly influences the function of the polymerase domain
additional information
-
site-directed chemical modification of the RNase H domain by selectively PEGylating Cys635, one of the eight cysteine residues present in the reverse transcriptase, specifically inactivates its ribonucleolytic activity, PEGylation as a tool for engineering the M-MuLV RT derivative deficient in RNase H activity, overview
additional information
-
construction of a chimeric enzyme containing the first 425 amino acid residues from the N-terminal domain of HIV-1 reverse transcriptase, i.e. the polymerase domain, and 200 amino acid residues from the C-terminal domain of murine leukemia virus reverse transcriptase, i.e. RNase H-domain. The chimeric enzyme exists as a monomer with intact DNA polymerase and RNase-H functions. It is able to catalyze both endonucleolytic and processive RNase-H functions in a manner similar to the wild type HIV-1 reverse transcriptase and murineleukemia virus reverse transcriptase
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Roth, M.J.; Tanese, N.; Goff, S.P.
Purification and characterization of murine retroviral reverse transcriptase expressed in Escherichia coli
J. Biol. Chem.
260
9326-9335
1985
Moloney murine leukemia virus
brenda
Rausch, J.W.; Lener, D.; Miller, J.T.; Julias, J.G.; Hughes, S.H.; Le Grice, S.F.J.
Altering the RNase H primer grip of human immunodeficiency virus reverse transcriptase modifies cleavage specificity
Biochemistry
41
4856-4865
2002
Human immunodeficiency virus 1
brenda
Lener, D.; Budihas, S.R.; Le Grice, S.F.J.
Mutating conserved residues in the ribonuclease H domain of Ty3 reverse transcriptase affects specialized cleavage events
J. Biol. Chem.
277
26486-26495
2002
Saccharomyces cerevisiae
brenda
Sevilya, Z.; Loya, S.; Hughes, S.H.; Hizi, A.
The ribonuclease H activity of the reverse transcriptases of human immunodeficiency viruses type 1 and type 2 is affected by the thumb subdomain of the small protein subunits
J. Mol. Biol.
311
957-971
2001
Human immunodeficiency virus 1, Human immunodeficiency virus 2, Human immunodeficiency virus 2 D-194, Human immunodeficiency virus 2 ROD
brenda
Sevilya, Z.; Loya, S.; Duvshani, A.; Adir, N.; Hizi, A.
Mutagenesis of cysteine 280 of the reverse transcriptase of human immunodeficiency virus type-1: The effects on the ribonuclease H activity
J. Mol. Biol.
327
19-30
2003
Human immunodeficiency virus 1
brenda
Schultz, S.J.; Zhang, M.; Champoux, J.J.
Sequence, distance, and accessibility are determinants of 5'-end-directed cleavages by retroviral RNases H
J. Biol. Chem.
281
1943-1955
2006
Human immunodeficiency virus 1, Moloney murine leukemia virus
brenda
Schultz, S.J.; Zhang, M.; Champoux, J.J.
Recognition of internal cleavage sites by retroviral RNases H
J. Mol. Biol.
344
635-652
2004
Human immunodeficiency virus 1, Moloney murine leukemia virus
brenda
Brehm, J.H.; Mellors, J.W.; Sluis-Cremer, N.
Mechanism by which a glutamine to leucine substitution at residue 509 in the ribonuclease H domain of HIV-1 reverse transcriptase confers zidovudine resistance
Biochemistry
47
14020-14027
2008
Human immunodeficiency virus 1
brenda
Fuji, H.; Urano, E.; Futahashi, Y.; Hamatake, M.; Tatsumi, J.; Hoshino, T.; Morikawa, Y.; Yamamoto, N.; Komano, J.
Derivatives of 5-nitrofuran-2-carboxylic acid carbamoyl methyl ester inhibit RNase H activity associated with HIV-1 reverse transcriptase
J. Med. Chem.
52
1380-1387
2009
Human immunodeficiency virus 1, Moloney murine leukemia virus
brenda
Waters, J.; ONeal, W.; White, K.; Wakeford, C.; Lansdon, E.; Harris, J.; Svarovskaia, E.; Miller, M.; Borroto-Esoda, K.
Mutations in the thumb-connection and RNase H domain of HIV type-1 reverse transcriptase of antiretroviral treatment-experienced patients
Antivir. Ther. (Lond. )
14
231-239
2009
Human immunodeficiency virus 1
brenda
Allen, S.; Krawczyk, S.; McGee, L.; Bischofberger, N.; Mulato, A.; Cherrington, J.
Inhibition of HIV-1 RNase H activity by nucleotide dimers and monomers
Antiviral Chem. Chemother.
7
37-45
1996
Human immunodeficiency virus 1, Moloney murine leukemia virus
-
brenda
Mizrahi, V.
Analysis of the ribonuclease H activity of HIV-1 reverse transcriptase using RNA-DNA hybrid substrates derived from the gag region of HIV-1
Biochemistry
28
9088-9094
1989
Human immunodeficiency virus 1
brenda
Furfine, E.S.; Reardon, J.E.
Human immunodeficiency virus reverse transcriptase ribonuclease H: specificity of tRNA(Lys3)-primer excision
Biochemistry
30
7041-7046
1991
Avian myeloblastosis virus, Human Immunodeficiency Virus, Moloney murine leukemia virus
brenda
Peliska, J.A.; Balasubramanian, S.; Giedroc, D.P.; Benkovic, S.J.
Recombinant HIV-1 nucleocapsid protein accelerates HIV-1 reverse transcriptase catalyzed DNA strand transfer reactions and modulates RNase H activity
Biochemistry
33
13817-13823
1994
Human immunodeficiency virus 1
brenda
Cirino, N.M.; Cameron, C.E.; Smith, J.S.; Rausch, J.W.; Roth, M.J.; Benkovic, S.J.; Le Grice, S.F.
Divalent cation modulation of the ribonuclease functions of human immunodeficiency virus reverse transcriptase
Biochemistry
34
9936-9943
1995
Human Immunodeficiency Virus
brenda
Ghosh, M.; Williams, J.; Powell, M.D.; Levin, J.G.; Le Grice, S.F.
Mutating a conserved motif of the HIV-1 reverse transcriptase palm subdomain alters primer utilization
Biochemistry
36
5758-5768
1997
Human immunodeficiency virus 1
brenda
Gabbara, S.; Davis, W.R.; Hupe, L.; Hupe, D.; Peliska, J.A.
Inhibitors of DNA strand transfer reactions catalyzed by HIV-1 reverse transcriptase
Biochemistry
38
13070-13076
1999
Human immunodeficiency virus 1
brenda
Davis, W.R.; Tomsho, J.; Nikam, S.; Cook, E.M.; Somand, D.; Peliska, J.A.
Inhibition of HIV-1 reverse transcriptase-catalyzed DNA strand transfer reactions by 4-chlorophenylhydrazone of mesoxalic acid
Biochemistry
39
14279-14291
2000
Human immunodeficiency virus 1
brenda
Starnes, M.; Cheng, Y.
Human immunodeficiency virus reverse transcriptase-associated RNase H activity
J. Biol. Chem.
264
7073-7077
1989
Human Immunodeficiency Virus
brenda
Cirino, N.M.; Kalayjian, R.C.; Jentoft, J.E.; Le Grice, S.F.
Fluorimetric analysis of recombinant p15 HIV-1 ribonuclease H
J. Biol. Chem.
268
14743-14749
1993
Human immunodeficiency virus 1
brenda
Volkmann, S.; Wohrl, B.; Tisdale, M.; Moelling, K.
Enzymatic analysis of two HIV-1 reverse transcriptase mutants with mutations in carboxyl-terminal amino acid residues conserved among retroviral ribonucleases H
J. Biol. Chem.
268
2674-2683
1993
Human immunodeficiency virus 1
brenda
Ghosh, M.; Howard, K.J.; Cameron, C.E.; Benkovic, S.J.; Hughes, S.H.; Le Grice, S.F.
Truncating alpha-helix E of p66 human immunodeficiency virus reverse transcriptase modulates RNase H function and impairs DNA strand transfer
J. Biol. Chem.
270
7068-7076
1995
Human immunodeficiency virus 1
brenda
Rausch, J.W.; Le Grice, S.F.J.
Substituting a conserved residue of ribonuclease H domain alters substrate hydrolysis by retroviral reverse transcriptase
J. Biol. Chem.
272
8602-8610
1997
Human Immunodeficiency Virus
brenda
Misra, H.; Pandey, P.; Pandey, V.
An enzymatically active chimeric HIV-1 reverse transcriptase (RT) with the RNase-H domain of murine leukemia virus RT exists as a monomer
J. Biol. Chem.
273
9785-9789
1998
murine leukemia virus
brenda
Schultz, S.J.; Zhang, M.; Kelleher, C.D.; Champoux, J.J.
Analysis of plus-strand primer selection, removal, and reutilization by retroviral reverse transcriptases
J. Biol. Chem.
275
32299-32309
2000
Moloney murine leukemia virus
brenda
Gao, H.; Sarafianos, S.; Arnold, E.; Hughes, S.
Similarities and differences in the RNase H activities of human immunodeficiency virus type 1 reverse transcriptase and Moloney murine leukemia virus reverse transcriptase
J. Mol. Biol.
294
1097-1113
1999
Human immunodeficiency virus 1, Moloney murine leukemia virus
brenda
Moelling, K.; Schulze, T.; Diringer, H.
Inhibition of human immunodeficiency virus type 1 RNase H by sulfated polyanions
J. Virol.
63
5489-5491
1989
Human immunodeficiency virus 1
brenda
Fu, T.; Taylor, J.
When retroviral reverse transcriptases reach the end of their RNA templates
J. Virol.
66
4271-4278
1992
Human immunodeficiency virus 1
brenda
Brincat, J.L.; Pfeiffer, J.K.; Telesnitsky, A.
RNase H activity is required for high-frequency repeat deletion during Moloney murine leukemia virus replication
J. Virol.
76
88-95
2002
Moloney murine leukemia virus
brenda
Nikolenko, G.; Palmer, S.; Maldarelli, F.; Mellors, J.; Coffin, J.; Pathak, V.
Mechanism for nucleoside analog-mediated abrogation of HIV-1 replication: Balance between RNase H activity and nucleotide excision
Proc. Natl. Acad. Sci. USA
102
2093-2098
2005
Human immunodeficiency virus 1
brenda
Julias, J.; McWilliams, M.; Sarafianos, S.; Arnold, E.; Hughes, S.
Mutations in the RNase H domain of HIV-1 reverse transcriptase affect the initiation of DNA synthesis and the specificity of RNase H cleavage in vivo
Proc. Natl. Acad. Sci. USA
99
9515-9520
2002
Human immunodeficiency virus 1
brenda
Goedken, E.R.; Marqusee, S.
Metal binding and activation of the ribonuclease H domain from Moloney murine leukemia virus
Protein Eng.
12
975-980
1999
Moloney murine leukemia virus
brenda
Kern, G.; Handel, T.; Marqusee, S.
Characterization of a folding intermediate from HIV-1 ribonuclease H
Protein Sci.
7
2164-2174
1998
Human immunodeficiency virus 1
brenda
Temiz, N.; Bahar, I.
Inhibitor binding alters the directions of domain motions in HIV-1 reverse transcriptase
Proteins Struct. Funct. Genet.
49
61-70
2002
Human immunodeficiency virus 1
brenda
Davies II, J.; Hostomska, Z.; Hostomsky, Z.; Jordan, S.; Matthews, D.
Crystal structure of the ribonuclease H domain of HIV-1 reverse transcriptase
Science
252
88-95
1991
Human immunodeficiency virus 1
brenda
Jones, F.D.; Hughes, S.H.
In vitro analysis of the effects of mutations in the G-tract of the human immunodeficiency virus type 1 polypurine tract on RNase H cleavage specificity
Virology
360
341-349
2007
Human immunodeficiency virus 1
brenda
Hachiya, A.; Shimane, K.; Sarafianos, S.G.; Kodama, E.N.; Sakagami, Y.; Negishi, F.; Koizumi, H.; Gatanaga, H.; Matsuoka, M.; Takiguchi, M.; Oka, S.
Clinical relevance of substitutions in the connection subdomain and RNase H domain of HIV-1 reverse transcriptase from a cohort of antiretroviral treatment-naive patients
Antiviral Res.
82
115-121
2009
Human immunodeficiency virus 1 (P03366)
brenda
Seckler, J.; Howard, K.; Barkley, M.; Wintrode, P.
Solution structural dynamics of HIV-1 reverse transcriptase heterodimer
Biochemistry
48
7646-7655
2009
Human immunodeficiency virus 1 (P03366)
brenda
Di Grandi, M.; Olson, M.; Prashad, A.S.; Bebernitz, G.; Luckay, A.; Mullen, S.; Hu, Y.; Krishnamurthy, G.; Pitts, K.; OConnell, J.
Small molecule inhibitors of HIV RT Ribonuclease H
Bioorg. Med. Chem. Lett.
20
398-402
2010
Human immunodeficiency virus 1
brenda
Mizuno, M.; Yasukawa, K.; Inouye, K.
Insight into the mechanism of the stabilization of Moloney murine leukaemia virus reverse transcriptase by eliminating RNase H activity
Biosci. Biotechnol. Biochem.
74
440-442
2010
Moloney murine leukemia virus
brenda
Kharlamova, T.
Synthesis of phenacyl derivatives of frangula-emodin and their HIV-1 RNase H activity
Chem. Nat. Compd.
45
500-502
2009
Human immunodeficiency virus 1
-
brenda
Kirschberg, T.A.; Balakrishnan, M.; Squires, N.H.; Barnes, T.; Brendza, K.M.; Chen, X.; Eisenberg, E.J.; Jin, W.; Kutty, N.; Leavitt, S.; Liclican, A.; Liu, Q.; Liu, X.; Mak, J.; Perry, J.K.; Wang, M.; Watkins, W.J.; Lansdon, E.B.
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information
J. Med. Chem.
52
5781-5784
2009
Human immunodeficiency virus 1
brenda
Esposito, F.; Fanti, V.; Marzeddu, R.; Randaccio, P.; Tramontano, E.; Zinzula, L.
Validation of a computed radiography device to monitor the HIV-1 RNase H activity
Nucl. Instrum. Meth. Phys. Res. A
607
226-228
2009
Human immunodeficiency virus 1
-
brenda
Wahba, A.S.; Esmaeili, A.; Damha, M.J.; Hudson, R.H.
A single-label phenylpyrrolocytidine provides a molecular beacon-like response reporting HIV-1 RT RNase H activity
Nucleic Acids Res.
38
1048-1056
2010
Human immunodeficiency virus 1
brenda
Himmel, D.M.; Maegley, K.A.; Pauly, T.A.; Bauman, J.D.; Das, K.; Dharia, C.; Clark, A.D.; Ryan, K.; Hickey, M.J.; Love, R.A.; Hughes, S.H.; Bergqvist, S.; Arnold, E.
Structure of HIV-1 reverse transcriptase with the inhibitor beta-thujaplicinol bound at the RNase H active site
Structure
17
1625-1635
2009
Human immunodeficiency virus 1 (P03366)
brenda
Talele, T.; Upadhyay, A.; Pandey, V.
Influence of the RNase H domain of retroviral reverse transcriptases on the metal specificity and substrate selection of their polymerase domains
Virol. J.
6
159-170
2009
Human immunodeficiency virus 1, Moloney murine leukemia virus
brenda
Xu, H.; Quan, Y.; Schader, S.; Oliveira, M.; Bar-Magen, T.; Wainberg, M.
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity
Antimicrob. Agents Chemother.
54
2401-2408
2010
Human immunodeficiency virus 1, Human immunodeficiency virus 1 HXB2
brenda
Farias, R.V.; Vargas, D.A.; Castillo, A.E.; Valenzuela, B.; Cote, M.L.; Roth, M.J.; Leon, O.
Expression of an Mg2+-dependent HIV-1 RNase H construct for drug screening
Antimicrob. Agents Chemother.
55
4735-4741
2011
Human immunodeficiency virus 1
brenda
Yanagita, H.; Urano, E.; Matsumoto, K.; Ichikawa, R.; Takaesu, Y.; Ogata, M.; Murakami, T.; Wu, H.; Chiba, J.; Komano, J.; Hoshino, T.
Structural and biochemical study on the inhibitory activity of derivatives of 5-nitro-furan-2-carboxylic acid for RNase H function of HIV-1 reverse transcriptase
Bioorg. Med. Chem.
19
816-825
2011
Human immunodeficiency virus 1
brenda
Kumar, A.
Binding of dumbbell oligonucleotides to MoMuLV reverse transcriptase: inhibitory properties of RNase H activity
E-J. Chem.
7
701-708
2010
Moloney murine leukemia virus
-
brenda
Billamboz, M.; Bailly, F.; Lion, C.; Calmels, C.; Andreola, M.L.; Witvrouw, M.; Christ, F.; Debyser, Z.; De Luca, L.; Chimirri, A.; Cotelle, P.
2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4
Eur. J. Med. Chem.
46
535-546
2011
Human Immunodeficiency Virus
brenda
Esposito, F.; Kharlamova, T.; Distinto, S.; Zinzula, L.; Cheng, Y.C.; Dutschman, G.; Floris, G.; Markt, P.; Corona, A.; Tramontano, E.
Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases
FEBS J.
278
1444-1457
2011
Human immunodeficiency virus 1
brenda
Biondi, M.J.; Beilhartz, G.L.; McCormick, S.; Goette, M.
N348I in HIV-1 reverse transcriptase can counteract the nevirapine-mediated bias toward RNase H cleavage during plus-strand initiation
J. Biol. Chem.
285
26966-26975
2010
Human immunodeficiency virus 1, Human immunodeficiency virus 1 HXB-2
brenda
Billamboz, M.; Bailly, F.; Lion, C.; Touati, N.; Vezin, H.; Calmels, C.; Andreola, M.; Christ, F.; Debyser, Z.; Cotelle, P.
Magnesium chelating 2-hydroxyisoquinoline-1,3(2H, 4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: Discovery of a novel selective inhibitor of the ribonuclease H function
J. Med. Chem.
54
1812-1824
2011
Moloney murine leukemia virus
brenda
Chung, S.; Himmel, D.; Jiang, J.; Wojtak, K.; Bauman, J.; Rausch, J.; Wilson, J.; Beutler, J.; Thomas, C.; Arnold, E.; Le Grice, S.
Synthesis, activity, and structural analysis of novel alpha-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H
J. Med. Chem.
54
4462-4473
2011
Human immunodeficiency virus 1
brenda
Su, H.P.; Yan, Y.; Prasad, G.S.; Smith, R.F.; Daniels, C.L.; Abeywickrema, P.D.; Reid, J.C.; Loughran, H.M.; Kornienko, M.; Sharma, S.; Grobler, J.A.; Xu, B.; Sardana, V.; Allison, T.J.; Williams, P.D.; Darke, P.L.; Hazuda, D.J.; Munshi, S.
Structural basis for the inhibition of RNase H activity of HIV-1 reverse transcriptase by RNase H active site-directed inhibitors
J. Virol.
84
7625-7633
2010
Human immunodeficiency virus 1 (P0C6F2), Human immunodeficiency virus 1 HXB2 (P0C6F2)
brenda
Wang, J.; Bambara, R.A.; Demeter, L.M.; Dykes, C.
Reduced fitness in cell culture of HIV-1 with nonnucleoside reverse transcriptase inhibitor-resistant mutations correlates with relative levels of reverse transcriptase content and RNase H activity in virions
J. Virol.
84
9377-9389
2010
Human immunodeficiency virus 1
brenda
Radzvilavicius, T.; Lagunavicius, A.
Selective inactivation of M-MuLV RT RNase H activity by site-directed PEGylation: an improved ability to synthesize long cDNA molecules
New Biotechnol.
29
285-292
2012
Moloney murine leukemia virus
brenda
Lu, M.; Ngo, W.; Mei, Y.; Munshi, V.; Burlein, C.; Loughran, M.; Williams, P.; Hazuda, D.; Miller, M.; Grobler, J.; Diamond, T.; Lai, M.
Purification of untagged HIV-1 reverse transcriptase by affinity chromatography
Protein Expr. Purif.
71
231-239
2010
Human immunodeficiency virus 1
brenda
Delviks-Frankenberry, K.A.; Nikolenko, G.N.; Pathak, V.K.
The connection between HIV drug resistance and RNase H
Viruses
2
1476-1503
2010
Human immunodeficiency virus 1, Human immunodeficiency virus 1 HXB2
brenda
Singh, K.; Marchand, B.; Kirby, K.; Michailidis, E.; Sarafianos, S.
Structural aspects of drug resistance and inhibition of HIV-1 reverse transcriptase
Viruses
2
606-638
2010
Human immunodeficiency virus 1
brenda
Beilhartz, G.; Goette, M.
HIV-1 ribonuclease H: structure, catalytic mechanism and inhibitors
Viruses
2
900-926
2010
Human immunodeficiency virus 1, Human immunodeficiency virus 2
brenda
Sarafianos, S.G.; Das, K.; Tantillo, C.; Clark, A.D., Jr.; Ding, J.; Whitcomb, J.M.; Boyer, P.L.; Hughes, S.H.; Arnold, E.
Crystal structure of HIV-1 reverse transcriptase in complex with a polypurine tract RNA:DNA
EMBO J.
20
1449-1461
2001
Human immunodeficiency virus 1 (P03366)
brenda
Broecker, F.; Andrae, K.; Moelling, K.
Premature activation of the HIV RNase H drives the virus into suicide: a novel microbicide?
AIDS Res. Hum. Retroviruses
28
1397-1403
2012
Human Immunodeficiency Virus
brenda
Corona, A.; Di Leva, F.S.; Thierry, S.; Pescatori, L.; Cuzzucoli Crucitti, G.; Subra, F.; Delelis, O.; Esposito, F.; Rigogliuso, G.; Costi, R.; Cosconati, S.; Novellino, E.; Di Santo, R.; Tramontano, E.
Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by diketo acid derivatives
Antimicrob. Agents Chemother.
58
6101-6110
2014
Human immunodeficiency virus 1
brenda
Muchiri, J.M.; Li, D.; Dykes, C.; Bambara, R.A.
Efavirenz stimulates HIV-1 reverse transcriptase RNase H activity by a mechanism involving increased substrate binding and secondary cleavage activity
Biochemistry
52
4981-4990
2013
Human immunodeficiency virus 1
brenda
Ilina, T.; Labarge, K.; Sarafianos, S.G.; Ishima, R.; Parniak, M.A.
Inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H activity
Biology
1
521-541
2012
Human immunodeficiency virus 1
brenda
Velthuisen, E.J.; Johns, B.A.; Gerondelis, P.; Chen, Y.; Li, M.; Mou, K.; Zhang, W.; Seal, J.W.; Hightower, K.E.; Miranda, S.R.; Brown, K.; Leesnitzer, L.
Pyridopyrimidinone inhibitors of HIV-1 RNase H
Eur. J. Med. Chem.
83
609-616
2014
Human immunodeficiency virus 1
brenda
Corona, A.; Masaoka, T.; Tocco, G.; Tramontano, E.; Le Grice, S.F.
Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase
Future Med. Chem.
5
2127-2139
2013
Human immunodeficiency virus 1
brenda
Beilhartz, G.L.; Ngure, M.; Johns, B.A.; DeAnda, F.; Gerondelis, P.; Goette, M.
Inhibition of the ribonuclease H activity of HIV-1 reverse transcriptase by GSK5750 correlates with slow enzyme-inhibitor dissociation
J. Biol. Chem.
289
16270-16277
2014
Human immunodeficiency virus 1
brenda
Costi, R.; Metifiot, M.; Chung, S.; Cuzzucoli Crucitti, G.; Maddali, K.; Pescatori, L.; Messore, A.; Madia, V.N.; Pupo, G.; Scipione, L.; Tortorella, S.; Di Leva, F.S.; Cosconati, S.; Marinelli, L.; Novellino, E.; Le Grice, S.F.; Corona, A.; Pommier, Y.; Marchand, C.; Di Santo, R.
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase
J. Med. Chem.
57
3223-3234
2014
Human immunodeficiency virus 1
brenda
Himmel, D.M.; Myshakina, N.S.; Ilina, T.; Van Ry, A.; Ho, W.C.; Parniak, M.A.; Arnold, E.
Structure of a dihydroxycoumarin active-site inhibitor in complex with the RNase H domain of HIV-1 reverse transcriptase and structure-activity analysis of inhibitor analogs
J. Mol. Biol.
426
2617-2631
2014
Human immunodeficiency virus 1
brenda
Zheng, X.; Mueller, G.A.; DeRose, E.F.; London, R.E.
Metal and ligand binding to the HIV-RNase H active site are remotely monitored by Ile556
Nucleic Acids Res.
40
10543-10553
2012
Human immunodeficiency virus 1
brenda
Alvarez, M.; Barrioluengo, V.; Afonso-Lehmann, R.N.; Menendez-Arias, L.
Altered error specificity of RNase H-deficient HIV-1 reverse transcriptases during DNA-dependent DNA synthesis
Nucleic Acids Res.
41
4601-4612
2013
Human immunodeficiency virus 1
brenda
Zheng, X.; Pedersen, L.C.; Gabel, S.A.; Mueller, G.A.; Cuneo, M.J.; DeRose, E.F.; Krahn, J.M.; London, R.E.
Selective unfolding of one ribonuclease H domain of HIV reverse transcriptase is linked to homodimer formation
Nucleic Acids Res.
42
5361-5377
2014
Human immunodeficiency virus 1
brenda
Das, K.; Martinez, S.E.; Bandwar, R.P.; Arnold, E.
Structures of HIV-1 RT-RNA/DNA ternary complexes with dATP and nevirapine reveal conformational flexibility of RNA/DNA: insights into requirements for RNase H cleavage
Nucleic Acids Res.
42
8125-8137
2014
Human immunodeficiency virus 1 (P03366)
brenda
Corona, A.; Desantis, J.; Massari, S.; Distinto, S.; Masaoka, T.; Sabatini, S.; Esposito, F.; Manfroni, G.; Maccioni, E.; Cecchetti, V.; Pannecouque, C.; Le Grice, S.; Tramontano, E.; Tabarrini, O.
Studies on cycloheptathiophene-3-carboxamide derivatives as allosteric HIV-1 ribonuclease H inhibitors
ChemMedChem
11
1709-1720
2016
Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group M subtype B BH10 (P03366)
brenda
Kankanala, J.; Kirby, K.A.; Huber, A.D.; Casey, M.C.; Wilson, D.J.; Sarafianos, S.G.; Wang, Z.
Design, synthesis and biological evaluations of N-hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H
Eur. J. Med. Chem.
141
149-161
2017
Human immunodeficiency virus 1
brenda
Wang, L.; Tang, J.; Huber, A.D.; Casey, M.C.; Kirby, K.A.; Wilson, D.J.; Kankanala, J.; Xie, J.; Parniak, M.A.; Sarafianos, S.G.; Wang, Z.
6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity
Eur. J. Med. Chem.
156
652-665
2018
Human immunodeficiency virus 1
brenda
Wang, L.; Tang, J.; Huber, A.D.; Casey, M.C.; Kirby, K.A.; Wilson, D.J.; Kankanala, J.; Parniak, M.A.; Sarafianos, S.G.; Wang, Z.
6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H
Eur. J. Med. Chem.
156
680-691
2018
Human immunodeficiency virus 1
brenda
Tang, J.; Do, H.T.; Huber, A.D.; Casey, M.C.; Kirby, K.A.; Wilson, D.J.; Kankanala, J.; Parniak, M.A.; Sarafianos, S.G.; Wang, Z.
Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H tolerance of a nonflexible linker
Eur. J. Med. Chem.
166
390-399
2019
Human immunodeficiency virus 1
brenda
Moelling, K.; Broecker, F.; Russo, G.; Sunagawa, S.
RNase H as gene modifier, driver of evolution and antiviral defense
Front. Microbiol.
8
1745
2017
Human immunodeficiency virus 1
brenda
Li, A.; Li, J.; Johnson, K.A.
HIV-1 reverse transcriptase polymerase and RNase H (ribonuclease H) active sites work simultaneously and independently
J. Biol. Chem.
291
26566-26585
2016
Human immunodeficiency virus 1
brenda
Luczkowiak, J.; Matamoros, T.; Menendez-Arias, L.
Template-primer binding affinity and RNase H cleavage specificity contribute to the strand transfer efficiency of HIV-1 reverse transcriptase
J. Biol. Chem.
293
13351-13363
2018
Human immunodeficiency virus type 1 group O subtype B, Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group O subtype B ESP49, Human immunodeficiency virus type 1 group M subtype B BH10 (P03366)
brenda
Tang, J.; Liu, F.; Nagy, E.; Miller, L.; Kirby, K.A.; Wilson, D.J.; Wu, B.; Sarafianos, S.G.; Parniak, M.A.; Wang, Z.
3-Hydroxypyrimidine-2,4-diones as selective active site inhibitors of HIV reverse transcriptase-associated RNase H design, synthesis, and biochemical evaluations
J. Med. Chem.
59
2648-2659
2016
Human immunodeficiency virus 1
brenda
Oda, M.; Xi, Z.; Inaba, S.; Slack, R.; Ishima, R.
Binding thermodynamics of metal ions to HIV-1 ribonuclease H domain
J. Therm. Anal. Calorim.
135
2647-2653
2019
Human immunodeficiency virus type 1 group M subtype B, Human immunodeficiency virus type 1 group M subtype B BH10
brenda
Boso, G.; Oervell, C.; Somia, N.
The nature of the N-terminal amino acid residue of HIV-1 RNase H is critical for the stability of reverse transcriptase in viral particles
J. Virol.
89
1286-1297
2015
Human immunodeficiency virus 1
-
brenda
Boyer, P.L.; Smith, S.J.; Zhao, X.Z.; Das, K.; Gruber, K.; Arnold, E.; Burke, T.R.; Hughes, S.H.
Developing and evaluating inhibitors against the RNase H active site of HIV-1 reverse transcriptase
J. Virol.
92
e02203-17
2018
Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group M subtype B BH10 (P03366)
brenda
Murelli, R.P.; D'Erasmo, M.P.; Hirsch, D.R.; Meck, C.; Masaoka, T.; Wilson, J.A.; Zhang, B.; Pal, R.K.; Gallicchio, E.; Beutler, J.A.; Le Grice, S.F.
Synthetic alpha-hydroxytropolones as inhibitors of HIV reverse transcriptase ribonuclease H activity
MedChemComm
7
1783-1788
2016
Human immunodeficiency virus 1 (P05959), Human immunodeficiency virus 1, Human immunodeficiency virus 1 RF (P05959)
brenda
Permanasari, E.D.; Yasukawa, K.; Kanaya, S.
Enzymatic activities of RNase H domains of HIV-1 reverse transcriptase with substrate binding domains of bacterial RNases H1 and H2
Mol. Biotechnol.
57
526-538
2015
Human immunodeficiency virus 1
brenda
Ngoutane Mfopa, A.; Corona, A.; Eloh, K.; Tramontano, E.; Frau, A.; Boyom, F.F.; Caboni, P.; Tocco, G.
Uvaria angolensis as a promising source of inhibitors of HIV-1 RT-associated RNA-dependent DNA polymerase and RNase H functions
Nat. Prod. Res.
32
640-647
2018
Human immunodeficiency virus 1
brenda
Zheng, X.; Pedersen, L.C.; Gabel, S.A.; Mueller, G.A.; DeRose, E.F.; London, R.E.
Unfolding the HIV-1 reverse transcriptase RNase H domain - how to lose a molecular tug-of-war
Nucleic Acids Res.
44
1776-1788
2016
Human immunodeficiency virus 1 (P04585), Human immunodeficiency virus 1
brenda
Figiel, M.; Krepl, M.; Poznanski, J.; Golab, A.; Sponer, J.; Nowotny, M.
Coordination between the polymerase and RNase H activity of HIV-1 reverse transcriptase
Nucleic Acids Res.
45
3341-3352
2017
Human immunodeficiency virus 1
brenda
Yang, F.; Zheng, G.; Fu, T.; Li, X.; Tu, G.; Li, Y.H.; Yao, X.; Xue, W.; Zhu, F.
Prediction of the binding mode and resistance profile for a dual-target pyrrolyl diketo acid scaffold against HIV-1 integrase and reverse-transcriptase-associated ribonuclease H
Phys. Chem. Chem. Phys.
20
23873-23884
2018
Human immunodeficiency virus 1
brenda
Slack, R.L.; Spiriti, J.; Ahn, J.; Parniak, M.A.; Zuckerman, D.M.; Ishima, R.
Structural integrity of the ribonuclease H domain in HIV-1 reverse transcriptase
Proteins
83
1526-1538
2015
Human immunodeficiency virus 1 (P03366)
brenda
Herzig, E.; Hizi, A.
The importance of glutamine 294 that affects the ribonuclease H activity of the reverse transcriptase of HIV-2 to viral replication
Virology
483
13-20
2015
Human Immunodeficiency Virus
brenda
Ngcapu, S.; Theys, K.; Libin, P.; Marconi, V.C.; Sunpath, H.; Ndungu, T.; Gordon, M.L.
Characterization of nucleoside reverse transcriptase inhibitor-associated mutations in the RNase H region of HIV-1 subtype C infected individuals
Viruses
9
330-339
2017
Human immunodeficiency virus type 1 subtype C
brenda