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2.7.7.49: RNA-directed DNA polymerase

This is an abbreviated version!
For detailed information about RNA-directed DNA polymerase, go to the full flat file.

Word Map on EC 2.7.7.49

Reaction

a 2'-deoxyribonucleoside 5'-triphosphate
+
DNAn
=
diphosphate
+
DNAn+1

Synonyms

Bst DNA polymerase, CS5 pol, DNA nucleotidyltransferase (RNA-directed), DNA polymerase, DNA polymerase I, FeLV RT, FIV RT, FV Pol, FV reverse transcriptase, Gag-Pol, HBV-pol, HIV reverse transcriptase, HIV-1 M RT, HIV-1 O RT, HIV-1 R, HIV-1 reverse transcriptase, HIV-1 RT, HIV-reverse transcriptase, HIV-RT, human hepatitis B virus polymerase, human immunodeficiency virus type 1 reverse transcriptase, iScript enzyme, K4 polymerase, K4PolI, M-MuLV reverse transcriptase, MMLV RT, Moloney Murine leukemia virus reverse transcriptase, Moloney murine leukemia virus RT, MoMLV RT, More, MuLV RT, MX162-RT, MX65-RT, nucleoside reverse transcriptase, nucleotidyltransferase, deoxyribonucleate, RNA-dependent, p66 RT, P72, PFV RT, Pol, polymerase/reverse transcriptase, prototype foamy virus reverse transcriptase, R2-RT, reverse transcriptase, reverse transcriptase/RNA dependent DNA polymerase, reverse-transcriptase, revertase, RNA dependent DNA polymerase, RNA revertase, RNA-dependent DNA polymerase, RNA-instructed DNA polymerase, RT, SFV RT, simian foamy virus reverse transcriptase, SS RT, SuperScript I reverse transcriptase, Superscript II, SUPERSCRIPT II reverse transcriptase, T. Z05 pol, telomerase, telomerase catalytic subunit, telomerase reverse transcriptase, TERT, Tgo-Pol, xenotropic murine leukemia virus-related virus reverse transcriptase, XMRV RT, XNA reverse transcriptase

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.7 Nucleotidyltransferases
                2.7.7.49 RNA-directed DNA polymerase

Inhibitors

Inhibitors on EC 2.7.7.49 - RNA-directed DNA polymerase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((1s,3s)-3-(7-amino-2H-2,3,5,6-tetraazabenzo[cd]azulen-2-yl)cyclobutyl)methyl tetrahydrogen triphosphate
-
-
(+)-Calanolide A
-
-
(-)-epigallocatechin-3-gallate
-
exposure to (-)-epigallocatechin-3-gallate reduces cellular proliferation and induced apoptosis in both MCF-7 and HL60 cells in vitro, although TERT mRNA expression is decreased only in MCF-7 cells
(2-amino-5-chlorophenyl)(2-chlorophenyl)methanone
-
-
(2-amino-5-chlorophenyl)(2-fluorophenyl)methanone
-
-
(2-amino-5-chlorophenyl)(phenyl)methanone
-
-
(4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one
AF324493, Q8Q2U5, Q8Q2V9
-
(4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-3,4-dihydroquinazolin-2(1H)-one
-
-
(R)-9-(2-phosphonomethoxypropyl)adenine
-
-
([[(2R,5R)-5-(6-amino-7H-purin-7-yl)-2,5-dihydrofuran-2-yl]oxy]methyl)phosphonic acid
-
-
([[(2R,5R)-5-(6-amino-7H-purin-7-yl)-4-fluoro-2,5-dihydrofuran-2-yl]oxy]methyl)phosphonic acid
-
-
([[(2S,5S)-5-(6-amino-7H-purin-7-yl)-2,5-dihydrofuran-2-yl]oxy]methyl)phosphonic acid
-
-
1,10-di-2',3'-dideoxy-3'-thiacytidine-decanoate
-
-
1,10-di-3'-azido-2',3'-dideoxythymidine-decanoate
-
-
1,10-di-3'-fluoro-2',3'-dideoxythymidine-decanoate
-
-
1,10-phenanthroline
-
-
1,12-di-2',3'-dideoxy-3'-thiacytidine-dodecanoate
-
-
1,12-di-3'-azido-2',3'-dideoxythymidine-dodecanoate
-
-
1,12-di-3'-fluoro-2',3'-dideoxythymidine-dodecanoate
-
-
1,14-di-2',3'-dideoxy-3'-thiacytidine-tetradecanoate
-
-
1,14-di-3'-azido-2',3'-dideoxythymidine-tetradecanoate
-
-
1,14-di-3'-fluoro-2',3'-dideoxythymidine-tetradecanoate
-
-
1,2-bis(2-oxopropoxy)anthracene-9,10-dione
-
-
1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione
-
-
1,4-di-2',3'-dideoxy-3'-thiacytidine-succinate
-
-
1-benzyl-4-(2,6-difluorophenyl)-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-4-(2,6-dimethylphenyl)-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-4-(3-chlorophenyl)-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-4-(4-fluorophenyl)-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-7,7-dimethyl-4-(4-nitrophenyl)-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-7,7-dimethyl-5-oxo-4-phenyl-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-benzyl-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-1H-pyrrolo[2,3-b]quinoline-3-carbonitrile
-
-
1-butyl-4-[2-fluoro-4-(trifluoromethyl)phenyl]-5-oxo-1,5-dihydroindeno[1,2-b]pyrrolo[3,2-e]pyridine-3-carbonitrile
-
-
1-tert-butyl-5-formyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
-
-
1-[2',5'-bis-O-(t-butyldimethylsilyl)beta-D-ribofuranosyl]-3'-spiro-5''-(4''amino-1'',2''-oxathiole-2'',2''-dioxide)-3-ethylthymine
-
-
12-(deoxyadenosin-N1-yl)nevirapine
-
-
12-(deoxyadenosin-N6-yl)nevirapine
-
-
12-(deoxycytidin-N3-yl)nevirapine
-
-
12-(deoxyguanosin-O6-yl)nevirapine
-
-
12-hydroxy-nevirapine
-
-
2',3'-dehydro-2',3'-deoxythymidine triphosphate
2',3'-Didehydro-2',3'-dideoxycytidine 5'-triphosphate
-
-
2',3'-didehydro-2',3'-dideoxythymidine
-
-
2',3'-didehydro-2',3'-dideoxythymidine 5'-triphosphate
-
strong but nonspecific inhibitor
2',3'-dideoxy-2',3'-dehydrothymidine 5'-triphosphate
2',3'-dideoxy-3'-thiacytidine
-
-
2',3'-dideoxy-5-fluoro-3'-thiacytidine
-
-
2',3'-dideoxy-CTP
-
-
2',3'-dideoxycytidine
-
-
2',3'-dideoxyguanosine triphosphate
-
-
2',3'-dideoxyinosine
-
-
2',3'-dideoxythymidine 5'-triphosphate
2',5'-Oligoadenylate
-
mixed type inhibition, not strictly competitive with dTTP. Inhibition is most dramatic in the absence of sulfhydryl reagents and is reduced when either dithiothreitol or 2-mercaptoethanol are included in the reaction. Partial protection at 0.1 mM dithiothreitol, significant protection at 1 mM or above
2'-deoxyxylofuranosylthymidine 5'-triphosphate
-
Mn2+ is requisite for the compound to exhibit inhibition, competitive with dTTP
2'-fluoro-N-cyclobutyladenosine triphosphate
-
-
2,4,6-trichloroquinoline
-
-
2,7-dihydroxy-2,4,6-cyclo-heptatrien-1-one
-
beta-thujaplicinol analogue. Compound has no effect on polymerase-dependent RNase H cleavages but significantly affects the rates of polymerase-independent RNase H cleavages. In a model, the compoouind binds to the RNase H active site after the primary polymerase-dependent RNase H cleavage has occurred and stabilizes the 3'-end of the DNA primer in the polymerase active site thus blocking the enzyme's ability to carry out the polymerase-independent cleavages
2-acetyl-4-[4-(dimethylamino)phenyl]indeno[1,2-b]pyrrolo[3,2-e]pyridin-5(1H)-one
-
-
2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
-
-
2-amino-4-(3-benzoylphenyl)thiazole-5-carboxamide
-
2-amino-4-(3-bromo-4-chlorophenyl)thiazole-5-carboxamide
-
2-amino-4-(3-chlorophenyl)thiazole-5-carboxamide
-
2-amino-4-(3-iodophenyl)thiazole-5-carboxamide
-
2-amino-4-(3-phenylphenyl)thiazole-5-carboxamide
-
2-amino-4-phenylthiazole-5-carboxamide
-
2-hydroxy-6-pentadecylbenzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
2-hydroxy-6-[(8Z)-pentadec-8-en-1-yl]benzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
2-naphthalenesulfonic acid
-
in the ternary enzyme-DNA-inhibitor complex, incorporation of the next nucleotide onto the primer is blocked. KM-1 can bind to the enzyme in both the absence and presence of DNA but weakens the affinity for DNA 140fold so that it favors DNA dissociation. KM-1 distorts enzyme conformation and misaligns DNA at the active site
2-pyridin-3-yl-1-(3,4,5-trimethoxybenzoyl)-1H-benzimidazole
-
-
2-pyridin-3-yl-1H-benzimidazole
-
-
2-[(10Z)-heptadec-10-en-1-yl]-6-hydroxybenzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
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
-
-
3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
-
-
3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
-
-
3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
-
-
3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
-
-
3'-azido-2',3'-dideoxyadenosine triphosphate
-
-
3'-azido-2',3'-dideoxyguanosine triphosphate
-
-
3'-azido-2',3'-dideoxythymidine
-
-
3'-Azido-2',3'-dideoxythymidine 5'-diphosphate
-
-
3'-Azido-2',3'-dideoxythymidine 5'-triphosphate
3'-azido-2',3'-dideoxythymidine-5'-triphosphate
-
3'-azido-3'-deoxythymidine
3'-azido-3'deoxythymidine 5'-triphosphate
3'-deoxyadenosine
-
inhibits HIV-1 proviral DNA synthesis in human macrophages more efficiently than in CD4+ T cells
3'-dideoxythymidine triphosphate
-
3'-fluoro-2',3'-dideoxythymidine
-
-
3'-gluoro-5'-(2-valyloxypropanoyl)-2',3'-dideoxyguanosine
-
-
3'-hydroxymethyl 2'-dATP
-
highly specific inhibitor
3'-hydroxymethyl 2'-dCTP
-
highly specific inhibitor
3'-hydroxymethyl 2'-dGTP
-
highly specific inhibitor
3'-hydroxymethyl 2'-dUTP
-
highly specific inhibitor
3,5-dimethyl-4-[[2-([(3R)-1-[(pyridin-4-yl)methyl]pyrrolidin-3-yl]amino)thieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations
3,5-dimethyl-4-[[2-([(3S)-1-[(pyridin-4-yl)methyl]pyrrolidin-3-yl]amino)thieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(4-nitrophenyl)methyl]-1,2,3,4-tetrahydropyridin-4-yl]amino)-5,7-dihydrothieno[3,4-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(4-nitrophenyl)methyl]piperidin-4-yl]amino)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(4-nitrophenyl)methyl]piperidin-4-yl]amino)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(4-nitrophenyl)methyl]piperidin-4-yl]amino)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(4-nitrophenyl)methyl]piperidin-4-yl]amino)-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]azepan-4-yl]amino)thieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]azetidin-3-yl]amino)thieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]piperidin-4-yl]amino)-5,6,7,8-tetrahydroquinazolin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]piperidin-4-yl]amino)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]piperidin-4-yl]amino)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([1-[(pyridin-4-yl)methyl]piperidin-4-yl]amino)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3,5-dimethyl-4-[[2-([8-[(pyridin-4-yl)methyl]-8-azabicyclo[3.2.1]octan-3-yl]amino)thieno[3,2-d]pyrimidin-4-yl]oxy]benzonitrile
-
-
3-(2,4-dinitrophenylhydrazonomethyl) rifamycin SV
-
-
3-(2-cyanoacetyl)phenyl diethyl phosphate
-
3-(3-chlorophenyl)-3-oxopropanenitrile
-
3-(3-iodophenyl)-3-oxopropanamide
-
3-(3-methylbut-2-en-1-yl)-4-[(3-methylbut-2-en-1-yl)oxy]quinolin-2(1H)-one
-
-
3-([3-bromo-2-oxo-5-[(pyridin-3-yloxy)methyl]-1,2-dihydropyridin-4-yl]oxy)-5-chlorobenzonitrile
-
-
3-([3-bromo-2-oxo-5-[(pyridin-4-yloxy)methyl]-1,2-dihydropyridin-4-yl]oxy)-5-chlorobenzonitrile
-
-
3-([3-bromo-5-fluoro-2-oxo-6-[2-(pyridin-4-yl)ethyl]-1,2-dihydropyridin-4-yl]oxy)-5-chlorobenzonitrile
-
-
3-([3-bromo-6-[2-(3-chlorophenyl)ethyl]-5-fluoro-2-oxo-1,2-dihydropyridin-4-yl]oxy)-5-chlorobenzonitrile
-
-
3-([6-[2-(1,3-benzoxazol-2-yl)ethyl]-3-chloro-2-oxo-1,2-dihydropyridin-4-yl]oxy)-5-chlorobenzonitrile
-
-
3-benzoyl-3-oxopropanenitrile
-
3-chloro-5-([3-chloro-2-oxo-6-[2-(pyridin-2-yl)ethyl]-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([3-chloro-2-oxo-6-[2-(pyridin-3-yl)ethyl]-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([3-chloro-2-oxo-6-[2-(pyridin-4-yl)ethyl]-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([3-chloro-6-methyl-2-oxo-5-[2-(pyridin-3-yl)ethyl]-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([3-chloro-6-[2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethyl]-5-fluoro-2-oxo-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([3-chloro-6-[2-(3-chlorophenyl)ethyl]-2-oxo-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-([6-[2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethyl]-3-(dimethylamino)-5-fluoro-2-oxo-1,2-dihydropyridin-4-yl]oxy)benzonitrile
-
-
3-chloro-5-[[3-chloro-2-oxo-6-(2-phenylethyl)-1,2-dihydropyridin-4-yl]oxy]benzonitrile
-
-
3-chloro-5-[[3-chloro-5-fluoro-2-oxo-6-(2-phenylethyl)-1,2-dihydropyridin-4-yl]oxy]benzonitrile
-
-
3-chloro-5-[[3-chloro-6-methyl-2-oxo-5-(phenoxymethyl)-1,2-dihydropyridin-4-yl]oxy]benzonitrile
-
-
3-cyclic amine derivative of rifamycin SV
-
0.2 mg/ml, more than 90% inhibition
-
3-pentadecylphenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-phenyl-3-oxopropanenitrile
-
3-piperazinoiminomethyl rifamycin SV
-
-
3-tridecylphenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[(10Z)-heptadec-10-en-1-yl]phenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-8-azabicyclo[3.2.1]octan-8-yl)methyl]benzamide
-
-
3-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azetidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,6,7,8-tetrahydroquinazolin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,7-dihydrofuro[3,4-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
3-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azepan-1-yl)methyl]benzamide
-
-
3-[(5-benzyl-3-bromo-2-oxo-1,2-dihydropyridin-4-yl)oxy]-5-chlorobenzonitrile
-
-
3-[(5-benzyl-3-bromo-6-methyl-2-oxo-1,2-dihydropyridin-4-yl)oxy]-5-chlorobenzonitrile
-
-
3-[(8Z)-pentadec-8-en-1-yl]phenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[11-(ethoxycarbonyl)-1,7,9,10,11,12-hexahydro-3,2-(metheno)-10-azaazuleno[1',8',7',6':3,4,5]cyclopenta[6,7]fluoreno[2,1,9,8-fghij]benzo[cd]cyclopenta[mno]acephenanthrylen-9-yl]-1-methylpyridinium
-
pyridinium fullerene derivative, 50% cytotoxicity above 0.05 mM
3-[6-bromo-3-[2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethyl]-2-fluorophenoxy]-5-chlorobenzonitrile
-
-
3-[[(3R)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzamide
-
exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations. Favorable pharmacokinetic properties with an oral bioavailability of 30.96% and a half-life of 11.1 h.Ppromising anti-HIV-1 drug candidate with potent antiviral activities and desirable drug-like properties.
3-[[(3S)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzamide
-
-
3-[[3-bromo-2-oxo-5-(pyridin-4-ylmethoxy)-1,2-dihydropyridin-4-yl]oxy]-5-chlorobenzonitrile
-
-
4'-ethynyl-2-amino-2'-deoxyadenosine triphosphate
4'-ethynyl-2-fluoro-2'-deoxyadenosine
-
a translocation defective RT inhibitor, able to inhibit both WT and multi-drug resistant strains of HIV several orders of magnitude, modeling of the ternary complex of HIV-1 RT/DNA/inhibitor, overview. The 4'-ethynyl group is stabilized in a hydrophobic pocket formed by enzyme residues Ala114, Tyr115, Phe160, Met184, and the aliphatic segment of Asp185
4'-ethynyl-2-fluoro-2'-deoxyadenosine triphosphate
4-((4-((4-(4-cyano-2,6-dimethylphenoxy)-5,7-dihydrofuro-[3,4-d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzamide
-
-
-
4-(3-benzoylphenyl)thiazole-5-carboxamide
-
4-(3-bromo-4-chlorophenyl)-1H-imidazole-5-carboxamide
-
4-(3-bromo-4-chlorophenyl)thiazole-5-carboxamide
-
4-(3-chlorophenyl)-1H-imidazole-5-carboxamide
-
4-(3-iodophenyl)-3-oxobutanenitrile
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]-1,2,3,4-tetrahydropyridin-4-yl)amino]-5,7-dihydrothieno[3,4-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]azepan-4-yl)amino]thieno[3,2-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]azetidin-3-yl)amino]thieno[3,2-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]piperidin-4-yl)amino]-5,6,7,8-tetrahydroquinazolin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]piperidin-4-yl)amino]-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]piperidin-4-yl)amino]-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]piperidin-4-yl)amino]-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(1-[[4-(methanesulfonyl)phenyl]methyl]piperidin-4-yl)amino]-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-([2-[(8-[[4-(methanesulfonyl)phenyl]methyl]-8-azabicyclo[3.2.1]octan-3-yl)amino]thieno[3,2-d]pyrimidin-4-yl]oxy)-3,5-dimethylbenzonitrile
-
-
4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
-
-
4-phenyl-1H-imidazole-5-carboxamide
-
4-phenylthiazole-5-carboxamide
-
4-[(2-[[(3R)-1-[[4-(methanesulfonyl)phenyl]methyl]pyrrolidin-3-yl]amino]thieno[3,2-d]pyrimidin-4-yl)oxy]-3,5-dimethylbenzonitrile
-
-
4-[(2-[[(3S)-1-[[4-(methanesulfonyl)phenyl]methyl]pyrrolidin-3-yl]amino]thieno[3,2-d]pyrimidin-4-yl)oxy]-3,5-dimethylbenzonitrile
-
-
4-[(3,5-dimethylphenyl)sulfanyl]quinolin-2(1H)-one
-
-
4-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-8-azabicyclo[3.2.1]octan-8-yl)methyl]benzamide
-
-
4-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-8-azabicyclo[3.2.1]octan-8-yl)methyl]benzene-1-sulfonamide
-
-
4-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azetidin-1-yl)methyl]benzamide
-
-
4-[(3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azetidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,6,7,8-tetrahydroquinazolin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,6,7,8-tetrahydroquinazolin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,7-dihydrofuro[3,4-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,7-dihydrofuro[3,4-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-5,7-dihydrothieno[3,4-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azepan-1-yl)methyl]benzamide
-
-
4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]azepan-1-yl)methyl]benzene-1-sulfonamide
-
-
4-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-(3-methoxypropyl)-8-(1-methyl-1H-pyrazol-4-yl)-2,5-dihydro-1H-indeno[1,2-d]pyrimidine
-
inhibits HIV-1 reverse transcriptase in a primer extension assay but has no measurable activity against human DNA polymerase gamma at 0.01 mM. It potently inhibits HIV-1 replication in vitro with 1.5 nM 50% effective concentration. The antiviral potency is unaffected by the presence of nonnucleotide RT inhibitor mutations L100I, K103N/Y181C, V106A, or Y188L. Viruses encoding K65R are hypersusceptible to inhibition by the compound, and it retains full activity against viruses encoding M184V. A recombinant virus encoding the RT W153L is highly resistant
4-[[(3R)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzamide
-
-
4-[[(3R)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzene-1-sulfonamide
-
-
4-[[(3S)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzamide
-
-
4-[[(3S)-3-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]pyrrolidin-1-yl]methyl]benzene-1-sulfonamide
-
-
4-[[2-([1-[(4-aminophenyl)methyl]piperidin-4-yl]amino)-5,7-dihydrothieno[3,4-d]pyrimidin-4-yl]oxy]-3,5-dimethylbenzonitrile
-
-
4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-7,8-dihydroxy-2H-chromen-2-one
-
5-benzyl-6-aminouracil
-
competitive with template-primer
5-tridecylbenzene-1,3-diol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
5-[(8Z)-pentadec-8-en-1-yl]benzene-1,3-diol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
6,6-bieckol
-
selective inhibitor, 96.33% inhibition at 0.01 mM
6-([2-[(4-cyanophenyl)amino]pyrimidin-4-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile
-
compound has potency below 10 nM towards wild-type HIV-1 and viral variants containing the clinically important Y181C and K103N/Y181C mutations, greater activity than efavirenz particularly towards the K103N-bearing variant, normal cytotoxicity, and solubility
6-([4-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile
6-chloro-1-(2,6-dichlorobenzyl)-1,3-dihydro-2H-benzimidazol-2-one
-
-
6-chloro-4-(2-fluorophenyl)quinolin-2(1H)-one
-
-
6-chloro-4-(3,5-dimethylphenoxy)quinolin-2(1H)-one
-
-
6-chloro-4-(phenylsulfanyl)quinolin-2(1H)-one
-
-
6-chloro-4-(phenylsulfinyl)quinolin-2(1H)-one
-
-
6-chloro-4-(phenylsulfonyl)quinolin-2(1H)-one
-
-
6-chloro-4-phenoxyquinolin-2(1H)-one
-
-
6-chloro-4-phenylquinolin-2(1H)-one
-
-
6-chloro-4-[(3,5-dimethylphenyl)sulfanyl]quinolin-2(1H)-one
-
-
6-chloro-4-[(3,5-dimethylphenyl)sulfinyl]quinolin-2(1H)-one
-
-
6-chloro-4-[(3,5-dimethylphenyl)sulfonyl]-3,4-dihydroquinoxalin-2(1H)-one
-
-
6-chloro-4-[(3,5-dimethylphenyl)sulfonyl]quinolin-2(1H)-one
-
-
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
-
noncompetitive inhibitor, KNA-53 inhibits the RNase H function and is inactive on the polymerase function of enzyme mutant Y181C
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
-
-
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
-
-
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate
-
noncompetitive inhibitor
9-(pyridin-3-yl)-1,7,9,10,11,12-hexahydro-3,2-(metheno)-10-azaazuleno[1',8',7',6':3,4,5]cyclopenta[6,7]fluoreno[2,1,9,8-fghij]benzo[cd]cyclopenta[mno]acephenanthrylene-11-carboxylic acid
-
pyridine fullerene derivative, 50% cytotoxicity above 0.05 mM
9-aminonevirapine
-
-
adefovir diphosphate
alpha-amomeric oligonucleotides
-
inhibit reaction with either homopolymeric or heteropolymeric substrates
-
alpha-d(A)15
-
0.032 mM, inhibits 50% of the RNA dependent DNA polymerase activity, reaction with poly(U) as template
-
alpha-d(T)16
-
0.08 mM, 50% inhibition of RNA dependent DNA polymerase activity when 0.0075 mM beta-pd(T)12-18 as primer, poly(A) as template
-
azidothymidine
azidothymidine triphosphate
-
-
capravirine
-
HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition
d4T-Monophosphate
-
-
dATP
-
replacement of dATP by ATP completely prevents synthesis
ddATP
ddTTP
-
inhibits the enzyme from the group M strain BH10 isolate and the enzyme from the Spanish HIV-1 group O isolate
Delavirdine
Dextran sulfate
-
IC50: 0.0044 mg/ml
-
didanosine
Dioxolan Thymidine
-
-
early growth response-1
-
overexpressio nof early growth response-1 decreases TERT protein production as well TERT mRNA transcription
-
efavirenz
emetine
-
plant alkaloid isolated from Psychotria ipecacuanha. Reverse transcriptase is blocked in the presence of emetine both both in in vitro reactions with isolated enzyme and intravirion, reaching 80% of reduction in HIV-1 infection, with low cytotoxic effect. Emetine also blocks HIV-1 infection of reverse transcriptase M184V mutants
Etravirine
flavanonol
-
low inhibition
flavone
-
low inhibition
GW8248
-
HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition
heparin
-
IC50: 0.0740 mg/ml
Hygrophorus russula RNase
-
RNase isolated from fruiting bodies of the edible mushroom Hygrophorus russula inhibits reverse transcriptase by 91.6% at the concentration of 2.4 mg/ml
-
lamivudine
lamivudine triphosphate
loviride
-
IC50: 0.0082-0.16 mM, depending on the substrate used.The enzyme from the group M strain BH10 isolate is sensitive. The enzyme from the Spanish HIV-1 group O isolate shows high-level resistance with IC50 above 0.2 mM
Mg2+
-
above 0.5 mM. Addition of Mg2+ to a reaction mixture that already contains Mn2+ does not inhibit the Mn2+-dependent synthesis
morpholinocytosine triphosphate
-
-
N-(4-chlorophenyl)acetamide
-
-
N-cyclobutyladenosine triphosphate
-
-
N-cyclobutyladenosine-phosphonyl diphosphate
-
-
N-methylisatin beta-thiosemicarbazone
-
0.4 mM, 88% inhibition with a 70S RSV RNA template-primer and 50% inhibition with a calf thymus DNA template-primer in the presence of 1% 2-mercaptoethanol
N-[4-[(4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]piperidin-1-yl)methyl]phenyl]methanesulfonamide
-
-
N2-benzylguanine
-
the enzyme is strongly blocked, ethyl or larger groups cause preferential misincorporation and strong blockage of replicative polymerase activity
N2-ethylguanine
-
the enzyme is strongly blocked, ethyl or larger groups cause preferential misincorporation and strong blockage of replicative polymerase activity
N2-isobutylguanine
-
the enzyme is strongly blocked, ethyl or larger groups cause preferential misincorporation and strong blockage of replicative polymerase activity
N2-methyl(9-anthracenyl)guanine
-
the enzyme is strongly blocked, ethyl or larger groups cause preferential misincorporation and strong blockage of replicative polymerase activity
NaCl
-
IC50: 40-50 mM
naldixic acid
-
noncompetitive with respect to TTP and polyriboadenylic acid. Inhibitory effect is higher with polyriboadenylic acid than with polyribocytidylic acid as a synthetic substrate
nevirapine
NF 345
-
IC50: 7 mg/ml
NF 346
-
IC50: 5 mg/ml
p-mercuribenzoate
-
0.02 mM, 96% loss of activity
phosphate
-
5 mM, reduced to 73% of maximal activity. 40 mM, reduced to 14% of maximal activity
Phosphonoformate
-
-
PHP protein
-
a dimeric 16 kDa antifungal protein, isolated from the seeds of Peganum harmala by cationic exchange chromatography and gel filtration, inhibitor isoelectric point is about 8.4. Inhibits the viral polymerase to 69.1%. The protein has also inhibitory effect on cell proliferation and fungal growth, overview
-
propan-2-yl 7-methoxy-2-[(methylsulfanyl)methyl]-3-thioxo-3,4-dihydroquinoxaline-1(2H)-carboxylate
-
-
Rilpivirine
RNA aptamer
-
RNA aptamers suppress viral replication by cumulative inhibition of reverse transcriptase at every stage of genome replication
-
stavudine
Streptonigrin
-
acts on the enzyme molecule in an enzyme-template primer complex by a series of reactions including oxidation-reduction
suramin
Tenofovir
tenofovir diphosphate
TMC-125
-
HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition
TMC278
nonnucleoside reverse transcriptase inhibitor
zidovudine
zidovudine triphosphate
-
-
additional information
-