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(1H-naphtho[2,3-d]imidazol-2-yl)methyl 4-aminobenzoate
(1R,2R,3R,5S)-2,3,5-trihydroxy-5-(propylcarbamoyl)cyclohexyl (4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoate
-
(1S,3R,4S,5R)-1,3,4,5-tetrahydroxycyclohexane-1-carboxylic acid
-
(2-methoxy-4-nitrophenyl)methylene diacetate
-
(2-[acetyl[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 785 nM
(2-[formyl[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 749 nM
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: above 0.001 mM
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methylsulfonyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 498 nM
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](sulfamoyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 93 nM
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 499 nM
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 132 nM
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methylsulfonyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 68 nM
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](sulfamoyl)amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 24 nM
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
-
isozyme IMPDH II IC50: 13 nM
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
(2E)-3-furan-2-yl-N-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]prop-2-enamide
-
isozyme IMPDH II IC50: 0.002 mM
(2E)-3-{3-[N''-cyano-N'-(4-cyano-3-methoxyphenyl)carbamimidamido]phenyl}prop-2-enoic acid
-
(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-enal
-
(2E)-4-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-2-methylbut-2-enoic acid
-
(2E)-4-{6-methoxy-7-methyl-3-oxo-4-[2-(trimethylsilyl)ethoxy]-1,3-dihydro-2-benzofuran-5-yl}-2-methylbut-2-enal
-
(2E)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-phenylprop-2-enamide
-
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
(2E)-N-hydroxy-3-[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]prop-2-enamide
-
(2E)-N-hydroxy-3-[4-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]prop-2-enamide
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(2,3-dihydro-1-benzofuran-7-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(2-acetyl-1-methyl-2,3-dihydro-1H-benzimidazol-4-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(2-methoxyquinoxalin-5-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(2-methyl-4-oxo-3,4-dihydro-2H-1-benzopyran-6-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(2H-1,3-benzodioxol-5-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(3,4-dimethoxybenzene-1-sulfonyl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(3-methoxy-4-methylphenyl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(3-methoxyquinoxalin-5-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(4-cyano-3-methoxyphenyl)carbamoyl]amino}phenyl)ethyl]carbamate
i.e. VX-4997
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(4-methyl-2,3-dihydro-1-benzofuran-6-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(4-oxo-3,4-dihydro-2H-1-benzopyran-6-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(5,6-dihydro-1,4-dioxin-2-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(6,7-dimethoxynaphthalen-1-yl)carbamoyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(E)-1-(3,4-dimethoxyanilino)-2-nitroethenyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[(E)-1-(4-cyano-3-methoxyanilino)-2-nitroethenyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[4-(4-cyano-3-methoxyphenyl)piperazine-1-carbonyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[5-(4-cyano-3-methoxyphenyl)-1H-benzimidazol-2-yl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-(3-{[6-(4-cyano-3-methoxyphenyl)pyrazine-2-carbonyl]amino}phenyl)ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-{3-[2-(3,4-dimethoxyphenoxy)acetamido]phenyl}ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-{3-[2-(4-cyano-3-methoxyphenoxy)acetamido]phenyl}ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-{3-[3-(4-cyano-3-methoxyphenyl)-2,4-dioxoimidazolidin-1-yl]phenyl}ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl [(1S)-1-{3-[N'-(3,4-dimethoxyphenyl)carbamimidamido]phenyl}ethyl]carbamate
-
(2R)-1-cyanobutan-2-yl {(1S)-1-[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]ethyl}carbamate
-
(2R)-1-cyanobutan-2-yl {(1S)-1-[3-({[3-methoxy-4-(morpholin-4-yl)phenyl]carbamoyl}amino)phenyl]ethyl}carbamate
-
(2R)-1-cyanobutan-2-yl {(1S)-1-[3-({[3-methoxy-4-(oxan-4-yl)phenyl]carbamoyl}amino)phenyl]ethyl}carbamate
-
(2R)-1-cyanobutan-2-yl {(1S)-1-[3-({[4-(3,6-dihydro-2H-pyran-4-yl)-3-methoxyphenyl]carbamoyl}amino)phenyl]ethyl}carbamate
-
(2R)-1-cyanobutan-2-yl-[(1S)-1-(3-{[(3,4-dimethoxyphenyl)carbamoyl]amino}phenyl)-ethyl] carbamate
-
(2R)-2-phenyl-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
(2R)-2-[(naphthalen-1-yl)oxy]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
(2S)-1-cyanobutan-2-yl [(1R)-1-(3-{[(3,4-dimethoxyphenyl)carbamothioyl]amino}phenyl)ethyl]carbamate
-
(2S)-1-cyanobutan-2-yl [(1R)-1-(3-{[(4-cyano-3-methoxyphenyl)carbamothioyl]amino}phenyl)ethyl]carbamate
-
(2S)-1-cyanobutan-2-yl [(1R)-1-{3-[N''-cyano-N'-(4-cyano-3,5-dimethoxyphenyl)carbamimidamido]phenyl}ethyl]carbamate
-
(2S)-1-cyanobutan-2-yl [(1R)-1-{3-[N'-(3,4,5-trimethoxyphenyl)carbamimidamido]phenyl}ethyl]carbamate
-
(2S)-1-cyanobutan-2-yl [(1R)-1-{3-[N'-(4-cyano-3,5-dimethoxyphenyl)carbamimidamido]phenyl}ethyl]carbamate
-
(2S)-2-(2,3-dichloroanilino)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(2-hydroxyphenyl)-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-6-yl]propanamide
-
(2S)-2-(2,3-dichlorophenoxy)-N-[2-[4-(N'-hydroxycarbamimidoyl)phenyl]-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-(2,3-dimethoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-(2-chloro-3-nitrophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-(2-chlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-[(1-naphthyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
competitive versus NAD+
(2S)-2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
competitive versus NAD+, displays excellent IMPDH inhibitory activity and moderate stability in mouse liver microsomes
(2S)-N-(4-iodophenyl)-2-(4-methoxyphenoxy)propanamide
7759844
(2S)-N-[5-(4-bromophenyl)-1H-imidazol-2-yl]-2-[4-(1-methyl-1H-imidazol-4-yl)phenoxy]propanamide
AT080
(3aR,4R,6S,7aR)-6-hydroxy-2,2-dimethyl-6-(propylcarbamoyl)hexahydro-2H-1,3-benzodioxol-4-yl (4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoate
-
(3aR,4R,7S,8aR)-7-hydroxy-2,2-dimethyltetrahydro-2H-4,7-methano[1,3]dioxolo[4,5-c]oxepin-6(4H)-one
-
(3aR,5R,7R,7aS)-5,7-dihydroxy-2,2-dimethyl-N-propylhexahydro-2H-1,3-benzodioxole-5-carboxamide
-
(3S)-oxolan-3-yl {[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]methyl}carbamate
(3S,4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3,4-dimethylhex-4-enoic acid
-
(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetaldehyde
-
(4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
derivative of mycophenolic acid. IC50 value for K562 cells proliferation 8.2 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 8.2 microM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2R)-2-phenylpropyl]hex-4-enamide
73.94% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2S)-2-phenylpropyl]hex-4-enamide
59.15% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(2-methylphenyl)ethyl]hex-4-enamide
84% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(4-methylphenyl)ethyl]hex-4-enamide
73.42% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(pyridin-2-yl)ethyl]hex-4-enamide
59.38% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(pyridin-4-yl)ethyl]hex-4-enamide
57.38% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[3-(morpholin-4-yl)propyl]hex-4-enamide
36.05% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-{[(1-nitro-4a,9a-dihydroacridin-9-yl)amino]methyl}hex-4-enamide
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-{[(4-nitro-9-oxo-4a,9,9a,10-tetrahydroacridin-1-yl)amino]methyl}hex-4-enamide
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enal
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-(3-methoxyphenyl)-4-methylhex-4-enamide
30.82% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-(4-methoxyphenyl)-4-methylhex-4-enamide
54.84% inhibition at 0.01 mM
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-[2-(4-methoxyphenyl)ethyl]-4-methylhex-4-enamide
96.13% inhibition at 0.01 mM
(4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoic acid
derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.59 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.59 microM
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-[(4-butylphenyl)methyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
93.62% inhibition at 0.01 mM
(4E)-N-[2-(2-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
72.04% inhibition at 0.01 mM
(4E)-N-[2-(2H-1,3-benzodioxol-5-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
87.09% inhibition at 0.01 mM
(4E)-N-[2-(4-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
81.36% inhibition at 0.01 mM
(4E)-N-[2-(furan-2-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
67.18% inhibition at 0.01 mM
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
(5E)-N-hydroxy-7-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-5-methylhept-5-enamide
-
comparison with inhibition of histone deacetylase and K562 cell proliferation
(5S)-7-amino-5-(4-chlorophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
F2K
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid
(E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide
(E)-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-1-(thiophen-2-yl)methanimine
-
(R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
(S)-2-(2,3-dichlorophenoxy)-N-(2-(2-methoxypyridin-4-yl)benzo-[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(2-oxo-1,2-dihydropyridin-4-yl)benzo[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(3-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl)benzo-[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl)benzo[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(hydrazinecarbonyl)phenyl)-benzo[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(trifluoromethoxy)phenyl)-benzo[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-fluorophenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanethioamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)imidazo-[1,2-a]pyridin-6-yl)propanamide
-
(S)-2-(2,3-dichlorophenoxy)-N-(2-(6-methoxypyridin-3-yl)benzo-[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-fluorophenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2,3-difluorophenoxy)-N-(2-(6-methoxypyridin-3-yl)benzo-[d]oxazol-5-yl)propanamide
-
(S)-2-(2,3-difluorophenoxy)-N-(2-(pyridin-4-yl)benzo[d]oxazol-5-yl)propanamide
-
(S)-2-(2-(aminomethyl)phenoxy)-N-(2-(4-methoxyphenyl)benzo-[d]oxazol-5-yl)propanamide
-
(S)-2-(2-(benzyloxy)phenoxy)-N-(2-(4-cyanophenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2-cyano-3-fluorophenoxy)-N-(2-(pyridin-4-yl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2-cyanophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
-
(S)-2-(2-cyanophenoxy)-N-(2-(pyridin-4-yl)benzo[d]oxazol-5-yl)-propanamide
-
(S)-2-(3-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]-oxazol-2-yl)phenoxy)acetic acid
-
(S)-2-(4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]-oxazol-2-yl)phenoxy)acetic acid
-
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)-N-hydroxybenzamide
-
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)benzamide
-
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)benzoic acid
-
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)pyridine-1-oxide
-
(S)-N-(2-(2,3-dichlorophenoxy)propyl)-2-(4-methoxyphenyl)-benzo[d]oxazol-5-amine
-
(S)-N-(2-(4-(1H-tetrazol-5-yl)phenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
-
(S)-N-(2-(4-(aminomethyl)phenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-((1-hydroxy-1,3-dihydrobenzo-[c][1,2]oxaborol-7-yl)oxy)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-((2,3-dichlorophenyl)amino)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3,4-trifluorophenoxy)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3-difluorophenoxy)propanamide
-
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2-hydroxyphenoxy)propanamide
-
(S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
([[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]oxy]methyl)phosphonic acid
-
isozyme IMPDH II IC50: 246 nM
([[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]oxy]methyl)phosphonic acid
-
isozyme IMPDH II IC50: 23 nM
({hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl}methyl)phosphonic acid
-
1,4-dimethyl-6-nitro-2H-cyclopenta[d]pyridazine
-
1-(2,2-dimethylpropanoyl)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1'H-spiro[pyrrolidine-3,2'-quinazolin]-4'(3'H)-one
-
IC50: 0.094 mM, isozyme IMPDH II
1-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)-3-quinolin-7-ylurea
displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes
1-(3-methylphenyl)-3-[4-(1,3-oxazol-5-yl)phenyl]urea
-
isozyme IMPDH II IC50: 640 nM
1-(4-bromophenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]ethan-1-one
-
1-(4-chloro-5-nitrocyclohexa-1,5-dien-1-yl)-3-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes
1-(benzyloxy)-3-(3-pyridin-4-yl-1H-indol-6-yl)urea
-
1-methyl-6-[(5-phenyl-1,3-oxazol-2-yl)amino]-1H-indole-3-carbonitrile
-
1-phenylsulfonylindol-3-yl boronic acid
-
-
1-tert-butyl 5-methyl (3R,5R)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
-
IC50: 35 nM, isozyme IMPDH II
1-tert-butyl 5-methyl (3R,5S)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
-
IC50: 948 nM, isozyme IMPDH II
1-tert-butyl 5-methyl (3S,5R)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
-
IC50: 35 nM, isozyme IMPDH II
1-tert-butyl 5-methyl (3S,5S)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
-
26% inhibition at 10 micromol, isozyme IMPDH II
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
1-[(4-methoxyphenyl)methyl]-5-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
52.4% inhibition at 0.05 mM
1-[2-(cyclododecyloxy)-2-oxoethyl]-1-methylpiperidin-1-ium
-
i.e. 5F02, about 40% inhibition at 4 mM, less than 20% inhibition at 1 and 8 mM
1-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]-3-quinolin-7-ylurea
displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes
1-[3,4-bis(benzyloxy)-5-oxo-2,5-dihydrofuran-2-yl]ethane-1,2-diyl diacetate
-
1-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
-
isozyme IMPDH II IC50: 43 nM
1-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
-
isozyme IMPDH II IC50: 19 nM
1-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
-
isozyme IMPDH II IC50: 500 nM
1-{5-O-[hydroxy({hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl}methyl)phosphoryl]-beta-D-ribofuranosyl}-1H-benzimidazol-4-amine
-
14,16-dihydroxy-3,8-dimethyl-3,4,5,6,9,10-hexahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione
inhibition of leukemia K562 cells proliferation, IC50 of 71.3 microM
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
2'-deoxy-ATP
-
18% inhibition at 0.5 mM
2'-deoxy-GDP
-
12% inhibition at 0.5 mM
2'-deoxy-GTP
-
21% inhibition at 0.5 mM
2'-methylthiazole-4-carboxamide adenine dinucleotide
-
noncompetitive inhibition, less cytotoxic against K562 tumor cells
2,2,2-trichloroethyl (1-oxo-1,3-dihydro-2-benzofuran-5-yl)carbamate
-
2-(1,3-oxazol-5-yl)-5-[(5-phenyl-1,3-oxazol-2-yl)amino]phenol
-
isozyme IMPDH II IC50: 0.0016 mM
2-(1-benzothiophen-3-yl)-6-methoxy-5-(1,3-oxazol-2-yl)-1H-indole-3-carbaldehyde
-
2-(1-benzothiophen-3-yl)-6-methoxy-5-(1,3-oxazol-5-yl)-1H-indole-3-carbaldehyde
-
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
2-(2,4-dichlorophenoxy)-N-[2-(pyridin-2-yl)-1,3-benzoxazol-5-yl]propanamide
-
2-(2-chlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)-N-(6,7,8,9-tetrahydrodibenzo[b,d]furan-2-yl)acetamide
D67
2-(4-benzoylphenyl)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)propanamide
95.2% inhibition at 0.05 mM
2-(4-fluoronaphthalen-1-yl)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
99.9% inhibition at 0.05 mM
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
2-(dimethylamino)-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 200 nM
2-(methyl{2-[(2lambda~5~-triaza-1,2-dien-2-yl)acetyl]phenyl}amino)-2-oxoethyl acetate
-
2-([2-[2-(furan-2-yl)phenyl]-4-oxo-4H-1-benzopyran-3-yl]oxy)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
2-amino-oxazole-cyanoindoles
-
-
-
2-anilino-5-fluorobenzene-1,4-dicarboxylic acid
-
2-benzyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 180 nM
2-beta-D-ribofuranosylthiazole-4-carboxamide
-
NSC 286193, RTC
2-beta-D-ribofuranosylthiazole-4-carboxamide 5'-phosphate
-
RTC monophosphate
2-chloro-5-[[(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]benzamide
P32
2-chloro-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]-N,N-dimethylbenzamide
-
2-chloro-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]benzamide
-
2-chloro-N,N-diethyl-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]benzamide
-
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl[carbamoyl)amino]benzamide
P41
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
2-cyano-1-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-3-phenylguanidine
-
isozyme IMPDH II IC50: 240 nM
2-ethyl-5'-O-[hydroxy({hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl}methyl)phosphoryl]adenosine
-
2-ethyl-9-[5-O-[hydroxy(2-[hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]ethyl)phosphoryl]-beta-L-ribofuranosyl]-9H-purin-6-amine
inhibition of leukemia K562 cells proliferation, IC50 of 4.0 microM; inhibition of leukemia K562 cells proliferation, IC50 of 4.0 microM
2-fluoro-9-oxo-4a,9,9a,10-tetrahydroacridine-3-carboxylic acid
-
2-furan-3-yl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 32 nM
2-hydroxy-N-[2-(2-[[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methylacetamide
-
isozyme IMPDH II IC50: 41 nM
2-mercaptoethanol
-
inhibits above 2 mM
2-methoxy-1-methyl-4-nitrobenzene
-
2-methoxy-4-nitrobenzaldehyde
-
2-methyl-3-(pyrid-4-yl)indole
-
IC50: 343 nM
2-methylquinolin-8-yl 4-methylnaphthalene-1-sulfonate
-
ZINC58646829
2-oxo-4-(trifluoromethyl)-2H-1-benzopyran-7-yl 5-methylquinoline-8-sulfonate
-
ZINC46542062
2-phenoxy-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
2-tert-butyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 0.01 mM
2-[(2-{2-[3-methoxy-4-(1,3-oxazol-5-yl)anilino]-1,3-oxazol-5-yl}phenyl)(methyl)amino]-2-oxoethyl acetate
-
2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
racemic variant, competitive versus NAD+. Compound displays good antiparasitic activity in a Toxoplasma gondii strain that relies on Cryptosporidium parvum IMPDH, EC50 20 nM. No toxicity is observed against four mammalian cells lines
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
2-[2-(Z)-fluorovinyl]-inosine 5'-phosphate
-
is a time-dependent inactivator
2-[4-([1-[(2-fluorophenyl)methyl]-1H-1,2,3-triazol-5-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
71% inhibition at 0.05 mM
2-[4-([1-[(3,4-dichlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
2-[4-([1-[(3-chlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
2-[4-([1-[(3-methoxyphenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
2-[4-([1-[(3-methoxyphenyl)methyl]-1H-1,2,3-triazol-5-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
35% inhibition at 0.05 mM
2-[4-([1-[([1,1'-biphenyl]-4-yl)methyl]-1H-1,2,3-triazol-5-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
72.6% inhibition at 0.05 mM
2-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]propan-2-amine
-
2-[methyl[2-(2-[[3-(1,3-oxazol-5-yl)-1H-indol-6-yl]amino]-1,3-oxazol-5-yl)phenyl]amino]-2-oxoethyl acetate
-
2-[[2-(2-chlorophenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
2264A
inhibits lymphocyte proliferation; inhibits lymphocyte proliferation
2264B
inhibits lymphocyte proliferation; inhibits lymphocyte proliferation
3'-methylthiazole-4-carboxamide adenine dinucleotide
-
noncompetitive inhibition, less cytotoxic against K562 tumor cells
3'-[N''-cyano-N'-(4-cyano-3-methoxyphenyl)carbamimidamido][1,1'-biphenyl]-3-carboxylic acid
-
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
3-(2-[[(4-chlorophenyl)carbamoyl]amino]propan-2-yl)-N-hydroxybenzene-1-carboximidamide
3-(2-{2-[3-methoxy-4-(1,3-oxazol-5-yl)anilino]-1,3-oxazol-5-yl}phenyl)-1-(morpholin-4-yl)butan-2-one
i.e. BMS-337197
3-(4-chlorophenyl)-4-(4-ethoxyphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
3-cyanoindole
-
inhibits isozyme IMPDH II at 0.03 mM
3-cyanoindole-based inhibitors
-
synthesis and initial structureactivity relationships of 3-cyanoindole-based inhibitors with isozyme IMPDH II, IC50: 33-420 nM, comparison to other inhibitor structural classes, overview
-
3-formyl-1-methylindole
-
-
3-hydroxy-N-methyl-N-[2-(2-[[3-methyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]propanamide
-
isozyme IMPDH II IC50: 100 nM
3-hydroxy-N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methylpropanamide
-
isozyme IMPDH II IC50: 21 nM
3-methoxy-4-(1,3-oxazol-5-yl)aniline
-
3-methoxy-4-(oxazol-5-yl)aniline
-
-
3-phenyl quinolone derivatives
-
several, isozyme IMPDH II IC50: 5-160 nM, overview
-
3-{3-[N''-cyano-N'-(4-cyano-3-methoxyphenyl)carbamimidamido]phenyl}propanoic acid
-
4-(3-bromo-4-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
4-(4-acetamidophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
4-(4-acetamidophenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
4-(4-bromophenyl)-1H-imidazole
NMR744
4-(5-bromo-2-fluorophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
4-(5-bromo-2-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
4-acetyl-N-(3-chloro-4-fluorophenyl)-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
4-isothiocyanato-1,2-dimethoxybenzene
-
4-isothiocyanato-2-methoxybenzonitrile
-
4-nitro-1-beta-D-ribofuranosyl-1H-benzimidazole
-
4-pyridylindole
-
IC50: 0.00115 mM
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinolin-2(1H)-one
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
4-[(5-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazol-1-yl)methyl]benzonitrile
43.5% inhibition at 0.05 mM
4-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-6-phenyl-1,3,5-triazin-2-ol
-
5'-amino-5'-deoxyadenosine
-
5'-deoxy-5'-[(3-{[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoyl]amino}-2-oxopropyl)amino]adenosine
-
5'-O-([1-[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]-1H-1,2,3-triazol-4-yl[methyl)adenosine
MAD1, uncompetitive inhibitor
5'-O-([1-[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]-1H-1,2,3-triazol-4-yl]methyl)adenosine
an uncompetitive inhibitor with a strong preference for the E-XMP reaction intermediate, enzyme binding structure analysis, overview
5'-O-({[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]sulfamoyl}methanesulfonyl)adenosine
-
5'-O-[hydroxy({hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl}methyl)phosphoryl]adenosine
-
5'-thio-IMP
-
competitive inhibitor
5,5'-dithiobis(2-nitrobenzoate)
-
-
5,6,7,8-tetrahydroquinoxalin-6-yl 8-methylquinoline-5-sulfonate
-
ZINC89780094
5-(2-methoxy-4-nitrophenyl)-1,3-oxazole
-
5-(4-isothiocyanato-2-methoxyphenyl)-1,3-oxazole
-
5-([[2-([1,1'-biphenyl]-3-yl)propan-2-yl]carbamoyl]amino)-2-chlorobenzamide
-
-
5-aminoisobenzofuran-1(3H)-one
-
5-bromoisoquinolin-6-amine
-
5-chloro-1,4-dimethyl-2H-cyclopenta[d]pyridazine-6-carbonitrile
-
6,6'-oxydi(1,4-dihydroquinoxaline-2,3-dione)
binds in the nicotinamide subsite and does not interact with ADP
6-((E)-4-(((1-(50-deoxy-adenosin-50-yl)-1H-1,2,3-triazol-4-yl)-methyl)amino)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
-
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
6-(4-ethylpiperazin-1-yl)pyridine-3-carbonitrile
-
6-Chloro-9-beta-D-ribofuranosylpurine 5 '-phosphate
6-chloroinosine 5'-phosphate
6-Chloropurine
irreversible inhibitor
6-Chloropurine ribonucleoside 5'-phosphate
6-mercaptopurine ribonucleotide
-
-
6-thioguanosine
-
expression of isoform IMPDH2 increases modestly in response to 6-thioguanosine exposure. However, the basal enzyme activity decreases when the cells are exposed to a proliferation-blocking 6-thioguanosine concentration
6-thioinosine 5'-phosphate
6-{(2E)-4-[4-({[(2S,5R)-5-(6-amino-7,8-dihydro-9H-purin-9-yl)oxolan-2-yl]methoxy}methyl)-1H-1,2,3-triazol-1-yl]-3-methylbut-2-en-1-yl}-7-hydroxy-5-methoxy-4-methyl-2-benzofuran-1(3H)-one
-
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1'H-spiro[cyclopentane-1,2'-quinazolin]-4'(3'H)-one
-
IC50: 328 nM, isozyme IMPDH II
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1-(piperidin-1-ylcarbonyl)-1'H-spiro[pyrrolidine-3,2'-quinazolin]-4'(3'H)-one
-
IC50: 0.068 mM, isozyme IMPDH II
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-2,3,5,6-tetrahydro-1'H-spiro[pyran-4,2'-quinazolin]-4'(3'H)-one
-
IC50: 526 nM, isozyme IMPDH II
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-N-phenyl-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.393 mM, isozyme IMPDH II
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4,6-dihydro-1'H-spiro[cyclopenta[b]thiophene-5,2'-quinazolin]-4'(3'H)-one
-
IC50: 96 nM, isozyme IMPDH II
7'-methoxy-3'-methyl-N,N-bis(1-methylethyl)-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.071 mM, isozyme IMPDH II
7'-methoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-N-phenyl-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.064 mM, isozyme IMPDH II
7-amino-5-(4-chlorophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
7-amino-5-(4-nitrophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
7-amino-5-(5-nitrothiophen-2-yl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
7-hydroxy-5-methoxy-4-methyl-6-(3-methylbut-2-en-1-yl)-2-benzofuran-1(3H)-one
-
isozyme IMPDH II IC50: 254 nM
7-hydroxy-5-methoxy-4-methyl-6-[(2E)-3-methyl-4-(2lambda~5~-triaza-1,2-dien-2-yl)but-2-en-1-yl]-2-benzofuran-1(3H)-one
-
7-hydroxy-5-methoxy-4-methyl-6-{(2E)-3-methyl-6-[(2R)-oxiran-2-yl]-6-oxohex-2-en-1-yl}-2-benzofuran-1(3H)-one
-
7-hydroxy-5-methoxy-4-methyl-6-{(2E)-3-methyl-6-[(2S)-oxiran-2-yl]-6-oxohex-2-en-1-yl}-2-benzofuran-1(3H)-one
-
7-hydroxy-5-methoxy-6-[(2E)-4-methoxy-3-methylbut-2-en-1-yl]-4-methyl-2-benzofuran-1(3H)-one
-
isozyme IMPDH II IC50: 273 nM
7-hydroxy-6-[(2E)-6-hydroxy-3-methylocta-2,7-dien-1-yl]-5-methoxy-4-methyl-2-benzofuran-1(3H)-one
-
7-methoxy-2,2,3-trimethyl-6-(1,3-oxazol-5-yl)-2,3-dihydroquinazolin-4(1H)-one
-
IC50: 192 nM, isozyme IMPDH II
7-methoxy-2,2-dimethyl-6-(1,3-oxazol-5-yl)-3-(2-pyridin-4-ylethyl)-2,3-dihydroquinazolin-4(1H)-one
-
IC50: 300 nM, isozyme IMPDH II
7-methoxy-2,3-dimethyl-6-(1,3-oxazol-5-yl)-2-[(E)-2-phenylethenyl]-2,3-dihydroquinazolin-4(1H)-one
-
IC50: 49 nM, isozyme IMPDH II
7-methoxy-2-(3-methylphenyl)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
7-methoxy-2-(methylamino)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 220 nM
7-methoxy-2-methyl-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 110 nM
7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 65 nM
7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)quinazoline-2,4(1H,3H)-dione
-
IC50: 104 nM, isozyme IMPDH II
7-methoxy-6-(1,3-oxazol-2-yl)-2-phenylquinolin-4(1H)-one
-
7-methoxy-6-(1,3-oxazol-4-yl)-2-phenylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 210 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-(1,3-thiazol-4-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 34 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenoxyquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 8 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 8 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-2-ylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 43 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-3-ylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 70 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-4-ylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 46 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-2-ylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 63 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-3-ylquinolin-4(1H)-one
-
isozyme IMPDH II IC50: 9 nM
7-methoxy-6-(1,3-oxazol-5-yl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one
-
IC50: 303 nM
7-methoxy-6-(1,3-oxazol-5-yl)-3-(2-pyridin-4-ylethyl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one
-
7-methoxy-6-(1,3-oxazol-5-yl)-3-[2-(pyridin-4-yl)ethyl]-2-sulfanylidene-2,3-dihydroquinazolin-4(1H)-one
-
7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
-
isozyme IMPDH II IC50: 300 nM
8-methoxy-8-oxooctanoic acid
-
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethyl-9H-purin-6-amine
-
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethynyl-9H-purin-6-amine
-
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-phenyl-9H-purin-6-amine
-
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-9H-purin-6-amine
-
9-(5-O-[hydroxy[([hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]oxy)methyl]phosphoryl]-beta-L-ribofuranosyl)-9H-purin-6-amine
allopurinol ribonucleotide
-
-
APAD+
substrate inhibition, uncompetitive substrate inhibition versus IMP
AVN944
induces caspase-independent apoptosis in multiple myeloma cell lines and displays antiproliferative activity against both androgen-dependent and androgen-independent prostate cancer cell lines; induces caspase-independent apoptosis in multiple myeloma cell lines and displays antiproliferative activity against both androgen-dependent and androgen-independent prostate cancer cell lines
beta-difluoromethylene-tiazofurin
-
beta-methylene thiazole 4-carboxamide adenine dinucleotide
beta-methylene-TAD
-
noncompetitive inhibition
beta-methylene-thiazole-4-carboxamide adenine dinucleotide
-
i.e. beta-Me-TAD, enzyme binding structure analysis, the enzyme active site loop is ordered in this complex, and the catalytic Cys319 is 3.6 A from IMP, in the same plane as the hypoxanthine ring, the active site loop forms hydrogen bonds to the carboxamide of beta-Me-TAD, overview
beta-methylene-thiazole-4-carboxyamide-adenine dinucleotide
-
-
beta-methylene-tiazofurin
-
C2-mycophenolic adenine dinucleotide
C4-mycophenolic adenine dinucleotide
-
methylenephosphophosphonate analogue of mycophenolic adenine dinucleotide
CH2-SAD
i.e. 4-carboxamido-2-beta-D-ribofuranosylselenazolyl adenosine methylenediphosphonic acid, an adenine dinucleotide analogue nonhydrolyzable beta-methylene derivative
CH2-TAD
i.e. 4-carboxamido-2-beta-D-ribofuranosylthiazolyl adenosine methylenediphosphonic acid, an adenine dinucleotide analogue nonhydrolyzable beta-methylene derivative
chlorogenic acid
0.1 mM, 30% inhibition
CMP
-
25% inhibition at 0.6 mM
cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone
dimethyl (2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonate
-
isozyme IMPDH II IC50: above 0.001 mM
dimethyl 1-{(2Z)-2-[3,4-bis(benzyloxy)-5-oxofuran-2(5H)-ylidene]ethyl}-4,5-dihydro-1H-imidazole-4,5-dicarboxylate
-
dimethyl 2-amino-5-fluorobenzene-1,4-dicarboxylate
-
dimethyl 2-fluorobenzene-1,4-dicarboxylate
-
dimethyl 4,5-dihydro-1H-imidazole-4,5-dicarboxylate
-
dimethyl [(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphonate
-
isozyme IMPDH II IC50: 289 nM
dithioerythrol
-
inhibits above 1 mM
ellagic acid
0.1 mM, 27% inhibition
epigallocatechin gallate
0.1 mM, 47% inhibition
ethyl (2E)-3-[3-methoxy-4-(1,3-oxazol-5-yl)anilino]-3-phenylprop-2-enoate
-
ethyl (2E)-3-[4-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]prop-2-enoate
-
ethyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoyl carbonate
-
ethyl (S)-2-(3-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)phenoxy)acetate
-
ethyl (S)-2-(4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)phenoxy)acetate
-
ethyl 7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxylate
-
IC50: 0.08 mM, isozyme IMPDH II
ethyl 9-oxo-9,10-dihydroacridine-1-carboxylate
-
Fe3+
-
11% inhibition at 1 nM
HgCl2
-
complete inactivation at 0.5 mM
imidazo[4,5-e][1,4]diazapine
Inosine
-
very weak, non-competitive
Inosine 5'-methylphosphonate
-
very weak, non-competitive
Inosine 5'-phosphite
-
very weak, non-competitive
Inosine 5'-phosphofluoridate
-
very weak, non-competitive
merimepodib
has immunosuppressive activity; has immunosuppressive activity
methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.73 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.73 microM
methyl (S)-4-(5-(2-(2,3-Dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)benzoate
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
methyl methanethiosulfonate
-
-
methyl N-[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoyl]alaninate
-
mizobirine 5'-monophosphate
-
mizoribine 5'-monophosphate
-
mycophenolic 2-ethyladenosin-5'-yl-difluoromethylenebis(phosphonate)
potent, sub-micromolar inhibitor of leukemia K562 cells proliferation, IC50 of 0.45 microM; potent, sub-micromolar inhibitor of leukemia K562 cells proliferation, IC50 of 0.45 microM
mycophenolic 2-ethyladenosin-5'-yl-methylenebis(phosphonate)
inhibition of leukemia K562 cells proliferation, IC50 of 1.0 microM; inhibition of leukemia K562 cells proliferation, IC50 of 1.0 microM
mycophenolic acid glucuronide
-
80% inhibition at 0.2 mM, human plasma or serum reduces the inhibition
mycophenolic acid sodium
-
mycophenolic acid-acyl-glucuronide
mycophenolic adenine dinucleotide
-
-
mycophenolic hydroxamic acid
-
comparison with inhibition of histone deacetylase and K562 cell proliferation
N''-cyano-N-(3'-cyano[1,1'-biphenyl]-3-yl)-N'-(4-cyano-3-methoxyphenyl)guanidine
-
N''-cyano-N-(4'-cyano[1,1'-biphenyl]-3-yl)-N'-(4-cyano-3-methoxyphenyl)guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-(2'-fluoro[1,1'-biphenyl]-3-yl)guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-(3'-fluoro[1,1'-biphenyl]-3-yl)guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-(4'-fluoro[1,1'-biphenyl]-3-yl)guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-[3'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-[3-(1-hydroxyethenyl)phenyl]guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-[3-(2-hydroxyprop-2-en-1-yl)phenyl]guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-[3-(2-methyl-2H-tetrazol-5-yl)phenyl]guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-{3-[(1-methyl-1H-tetrazol-5-yl)methyl]phenyl}guanidine
-
N''-cyano-N-(4-cyano-3-methoxyphenyl)-N'-{3-[(2-methyl-2H-tetrazol-5-yl)methyl]phenyl}guanidine
-
N,7'-dimethoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.079 mM, isozyme IMPDH II
N,N-diethyl-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.045 mM, isozyme IMPDH II
N-(1,4-dinitroacridin-9-yl)methanediamine
-
N-(1-nitroacridin-9-yl)methanediamine
-
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-([4-oxo-2-[2-(thiophen-2-yl)phenyl]-4H-1-benzopyran-3-yl]oxy)acetamide
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
N-(2,3-dichlorophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
poor inhibition of human IMPDH2
N-(2,4-difluorophenyl)-7'-methoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.051 mM, isozyme IMPDH II
N-(2-[3-[(1E)-N-(2-aminoethoxy)ethanimidoyl]phenyl[propan-2-yl)-N'-(4-chloro-3-nitrophenyl)urea
-
P131
N-(2-{2-[3-methoxy-4-(1,3-oxazol-5-yl)anilino]-1,3-oxazol-5-yl}phenyl)-N-methyl-2-(morpholin-4-yl)acetamide
-
N-(2-{3-[(1E)-N-(2-aminoethoxy)ethanimidoyl]phenyl}propan-2-yl)-N'-(4-chloro-3-nitrophenyl)urea
N-(2H-indazol-6-yl)-3,5-dimethyl-1H-pyrazole-4-sulfonamide
N-(4-bromophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
N-(4-bromophenyl)-2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
N-(4-bromophenyl)-2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
N-(4-bromophenyl)-N'-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
P68
N-(4-bromophenyl)-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
P12
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
N-(4-chloro-3-methoxyphenyl)-2-(4-oxo[1]benzopyrano[4,3-c]pyrazol-1(4H)-yl)acetamide
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
N-(4-chlorophenyl)-2-phenoxypropanamide
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
N-(4-fluorophenyl)-4-[(2H-indazol-6-yl)sulfamoyl]-3,5-dimethyl-1H-pyrrole-2-carboxamide
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
N-(4-methoxyphenyl)-2-(naphthalen-1-yl)acetamide
N-(4-methoxyphenyl)-2-naphthalen-1-ylacetamide
binds in the nicotinamide subsite and does not interact with ADP
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
N-(5-phenyl-1,3-oxazol-2-yl)isoquinolin-6-amine
-
N-(naphthalen-1-yl)-2-[(4-oxo-2-phenyl-4H-1-benzopyran-3-yl)oxy]acetamide
N-(naphthalen-1-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
poor inhibition of human IMPDH2
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
N-ethyl-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
-
IC50: 0.119 mM, isozyme IMPDH II
N-ethylmaleimide
-
100% inhibition at 1 mM
N-hydroxy-N'-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]octanediamide
-
comparison with inhibition of histone deacetylase and K562 cell proliferation
N-methyl-N'-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)urea
-
N-methyl-N'-[4-(1,3-oxazol-5-yl)phenyl]-6-phenyl-1,3,5-triazine-2,4-diamine
-
isozyme IMPDH II IC50: 0.005 mM
N-methyl-N'-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-6-phenyl-1,3,5-triazine-2,4-diamine
-
isozyme IMPDH II IC50: 0.005 mM
N-methyl-N-[2-(2-[[3-methyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-morpholin-4-ylpropanamide
-
isozyme IMPDH II IC50: 45 nM
N-naphthalen-2-yl-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
-
-
N-tert-butyl-N'-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]ethanediamide
-
isozyme IMPDH II IC50: 55 nM
N-tert-butyl-N'-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]ethanediamide
-
isozyme IMPDH II IC50: 10 nM
N-tert-butyl-N'-[4-(1,3-oxazol-5-yl)phenyl]ethanediamide
-
isozyme IMPDH II IC50: 0.005 mM
N-tert-butyl-N'-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]ethanediamide
-
isozyme IMPDH II IC50: 0.005 mM
N-[(1R)-1-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]ethyl[-N'-phenylurea
G36
N-[(4-fluorophenyl)(1-methyl-1H-imidazol-2-yl)methyl]-2-methyl-3-(1,2,4-thiadiazol-5-yl)-1H-indole-6-carboxamide
-
N-[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoyl]alanine
-
N-[(Z)-(pyridin-3-ylimino)methyl]-2,3-dihydro-1,4-benzodioxine-2-carboxamide
-
N-[1-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-1-methylethyl]-2-fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide
-
N-[2-(2-[[3-(chloromethyl)-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
-
isozyme IMPDH II IC50: 47 nM
N-[2-(2-[[3-bromo-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
-
isozyme IMPDH II IC50: 28 nM
N-[2-(2-[[3-bromo-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
-
isozyme IMPDH II IC50: 21 nM
N-[2-(2-[[3-chloro-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
-
isozyme IMPDH II IC50: 48 nM
N-[2-(2-[[3-ethyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
-
isozyme IMPDH II IC50: 310 nM
N-[2-(2-[[3-ethyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
-
isozyme IMPDH II IC50: 21 nM
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-2-morpholin-4-ylacetamide
-
isozyme IMPDH II IC50: 91 nM
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-2-morpholin-4-ylacetamide
-
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
-
isozyme IMPDH II IC50: 16 nM
N-[2-(4-cyanophenyl)-1,3-benzoxazol-5-yl]-N2-(2,3-dichlorophenyl)-L-alaninamide
-
N-[2-(4-cyanophenyl)-1,3-benzoxazol-5-yl]-N2-(2,3-difluorophenyl)-L-alaninamide
-
N-[2-(hydroxymethyl)cyclopentyl]-N'-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]propanediamide
-
N-[2-chloro-3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[2-chloro-5-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.0016 mM
N-[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenyl]-beta-D-xylofuranosylamine
N-[2-chloro-5-[([2-[3-(propan-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenyl]-?-D-ribofuranosylamine
P176
N-[2-fluoro-5-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[3-bromo-4-(1,3-oxazol-5-yl)phenyl]-N'-tert-butylethanediamide
-
isozyme IMPDH II IC50: 50 nM
N-[3-chloro-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 88 nM
N-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
-
isozyme IMPDH II IC50: 340 nM
N-[3-ethoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.010 mM
N-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 190 nM
N-[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 57 nM
N-[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
-
isozyme IMPDH II IC50: 0.0016 mM
N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 20 nM
N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
-
isozyme IMPDH II IC50: 76 nM
N-[3-methoxy-4-(1H-1,2,4-triazol-1-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 410 nM
N-[3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.002 mM
N-[3-methoxy-4-(4-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[3-methyl-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[4-(1-benzyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl]acetamide
N-[4-(2,4-dimethyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.002 mM
N-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
-
isozyme IMPDH II IC50: 0.005 mM
N-[4-chloro-3-(alpha-D-ribofuranosyloxy)phenyl]-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
N-[4-chloro-3-(morpholine-4-carbonyl)phenyl]-N'-(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
noncompetitive with respect to NAD+, displays submicromolar activity in a Toxoplasma gondii model of Cryptosporidium parvum infection and displays good stability in mouse liver microsome. No antiparasitic activity is observed in mouse with once per day oral dosing of 250 mg/kg for 7 days
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
N-[4-chloro-3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]phenyl]-N'-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
N-{2-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]propan-2-yl}-2-fluoro-9-oxo-4a,9,9a,10-tetrahydroacridine-3-carboxamide
-
N-{2-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]propan-2-yl}-2-fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide
-
N1-methyl-N~2~-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethanediamide
-
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
NADPH
-
50% inhibition at 0.14 mM
NH4+
-
25% inhibition at 2.12 M
nicotinic acid
-
inhibitory analog of NAD+, non-competitive with respect to IMP and K+
N~1~-hydroxy-N~8~-phenyloctanediamide
-
N~1~-hydroxy-N~8~-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]octanediamide
-
N~2~-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]alaninamide
-
olaparib
-
about 70% inhibition at 8 mM
oxolan-3-yl {[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]methyl}carbamate
-
p-hydroxymercuribenzoate
-
97% inactivation at 1 mM
P1-(7-hydroxy-6-(ethyl-2-yl)-5-methoxy-4-methylphthalan-1-one)methylenephospho-P2-(adenosin-5'-yl)phosphonate
-
-
P1-(adenosine-5'-yl)methylenephospho-P2-(7-hydroxy-6-(ethyl-2-yl)-5-methoxy-4-methylphthalan-1-one)phosphonate
-
-
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
P1-(tiazofurin-5'-yl)-P2-(2-aminoadenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-(tiazofurin-5'-yl)-P2-(2-ethyladenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-(tiazofurin-5'-yl)-P2-(2-ethynyladenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-(tiazofurin-5'-yl)-P2-(2-iodoadenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-(tiazofurin-5'-yl)-P2-(2-phenyladenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-(tiazofurin-5'-yl)-P2-(adenosin-5'-yl) diphosphate
-
comparison with inhibition of alcohol dehydrogenase, malate dehydrogenase, lactate dehydrogenase and K562 cell proliferation
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-phenyladenosin-5'-yl)methylenebis(phosphonate)
-
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(adenosin-5'-yl)methylenebis(phosphonate)
-
phenyl N'-cyano-N-(3-[cyano[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamimidamido]benzyl)imidocarbamate
-
phosphate
-
mixed inhibition kinetics
prop-2-yn-1-yl (S)-2-(4-(5-(2-(2,3-dichlorophenoxy)-propanamido)benzo[d]oxa-zol-2-yl)phenoxy)acetate
-
propan-2-yl {3-[N''-cyano-N'-(4-cyano-3-methoxyphenyl)carbamimidamido]phenoxy}acetate
-
quinazolinedione derivatives
-
several derivatives, synthesis and inhibitory values, overview
-
quinazolinethione derivatives
-
several derivatives, synthesis and inhibitory values, overview
-
ribavirin 5'-monophosphate
ribose 5-phosphate
-
non-competitive
S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate
S-[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-en-1-yl] ethanethioate
-
SAD
i.e. selenazole-4-carboxamido adenine diphosphonic acid, an adenine dinucleotide analogue
selenazole adenine dinucleotide
-
-
selenazole-4-carboxyamide-adenine dinucleotide
-
Sesquiterpene lactones
-
a class of anti-neoplastic drugs, overview
-
TAD
i.e. thiazole-4-carboxamide adenine dinucleotide, an adenine dinucleotide analogue
tert-butyl 7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxylate
-
IC50: 104 nM, isozyme IMPDH II
tert-butyl methyl (1S,4S)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1'H-spiro[cyclopentane-1,2'-quinazoline]-3,4-dicarboxylate
-
tetrasodium 6,6'-[(3,3'-dimethoxy[1,1'-biphenyl]-4,4'-diyl)bis[(E)-diazene-2,1-diyl]]bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate)
thiazofurin-5'-yl-2-ethyladenosin-5'-yl-difluromethylene bis(phosphonate)
inhibition of leukemia K562 cells proliferation, IC50 of 4.7 microM; inhibition of leukemia K562 cells proliferation, IC50 of 4.7 microM
thiazole-4-carboxamide 2-ethyladenine dinucleotide
-
thiazole-4-carboxamide adenine dinucleotide
TMP
-
25% inhibition at 0.6 mM
UMP
-
25% inhibition at 0.6 mM
Urea
-
inactive at 3 M but regains activity after dialysis
VCC234718
-
uncompetitive inhibition with respect to IMP and NAD+
Zn2+
-
complete inhibition at 1 nM
[(1E,3E)-5-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpenta-1,3-dien-1-yl]phosphonic acid
-
isozyme IMPDH II IC50: 506 nM
[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphonic acid
-
isozyme IMPDH II IC50: 168 nM
[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphoramidic acid
-
isozyme IMPDH II IC50: above 0.001 mM
[(2S,5R)-5-(6-amino-7,8-dihydro-9H-purin-9-yl)oxolan-2-yl]methyl cyanate
-
[(3E)-5-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpent-3-en-1-yl]phosphonic acid
-
isozyme IMPDH II IC50: 96 nM
[(3E)-5-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpent-3-en-1-yl]phosphonic acid
-
isozyme IMPDH II IC50: 20 nM
[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-en-1-yl]phosphonic acid
-
isozyme IMPDH II IC50: 86 nM
[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenoxy]acetic acid
{3-[N''-cyano-N'-(4-cyano-3-methoxyphenyl)carbamimidamido]phenoxy}acetic acid
-
(1H-naphtho[2,3-d]imidazol-2-yl)methyl 4-aminobenzoate
-
-
(1H-naphtho[2,3-d]imidazol-2-yl)methyl 4-aminobenzoate
-
-
(1H-naphtho[2,3-d]imidazol-2-yl)methyl 4-aminobenzoate
-
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
-
isozyme IMPDH II IC50: 28 nM
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
-
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
-
-
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
-
(2R)-2-[(naphthalen-1-yl)oxy]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Q21
(2R)-2-[(naphthalen-1-yl)oxy]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
Q21
(2R)-2-[(naphthalen-1-yl)oxy]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Q21
(2S)-2-(2,3-dichloroanilino)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
potent inhibitor
(2S)-2-(2,3-dichloroanilino)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Q67
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
-
(3S)-oxolan-3-yl {[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]methyl}carbamate
i.e. VX-148, structure-activity relationship analysis, overview
(3S)-oxolan-3-yl {[3-({[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoyl}amino)phenyl]methyl}carbamate
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
-
-
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
-
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
-
-
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
-
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
derivative of mycophenolic acid. IC50 value for K562 cells proliferation 2.1 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 2.1 microM
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
-
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide
14.50% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide
4.59% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide
-
29.44% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide
46.13% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide
98.87% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide
-
42.79% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide
22.99% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide
3.59% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide
-
19.94% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide
14.29% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide
4.65% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide
-
32.43% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide
7.83% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide
2.36% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide
-
16.66% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide
22.27% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide
1.45% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide
-
17.11% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid
11.56% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid
3.03% inhibition at 0.001 mg
(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid
-
13.61% inhibition at 0.001 mg
(E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide
5.24% inhibition at 0.001 mg
(E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide
94.46% inhibition at 0.001 mg
(E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide
-
14.21% inhibition at 0.001 mg
(R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
9.03% inhibition at 0.001 mg
(R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
3.15% inhibition at 0.001 mg
(R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
-
9.49% inhibition at 0.001 mg
(S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
9.28% inhibition at 0.001 mg
(S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
0.06% inhibition at 0.001 mg
(S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one
-
11.99% inhibition at 0.001 mg
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
0.1% inhibition at 0.01 mM
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
0.1% inhibition at 0.01 mM
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
0.1% inhibition at 0.01 mM
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
0.1% inhibition at 0.01 mM
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
30.66% inhibition at 0.01 mM
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
-
-
1-[(3-methoxyphenyl)methyl]-4-[[(naphthalen-2-yl)oxy]methyl]-1H-1,2,3-triazole
24.94% inhibition at 0.01 mM
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
-
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
binds in the nicotinamide subsite and does not interact with ADP
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
not inhibitory to wild-type
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
-
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
-
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
-
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
-
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
-
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
-
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
-
-
2-([2-[2-(furan-2-yl)phenyl]-4-oxo-4H-1-benzopyran-3-yl]oxy)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
2-([2-[2-(furan-2-yl)phenyl]-4-oxo-4H-1-benzopyran-3-yl]oxy)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
0.1% inhibition at 0.01 mM
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
noncompetitive inhibitor, that has similar affinity to both E-IMP and E-XMP, enzyme binding structure analysis, overview
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
-
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
-
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
-
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
-
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
-
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
-
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
antagonizes ADP binding
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
-
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
not inhibitory to wild-type
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
-
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
-
2-[4-([1-[(3,4-dichlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
-
-
2-[4-([1-[(3,4-dichlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
0.1% inhibition at 0.01 mM
2-[4-([1-[(3-chlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
-
-
2-[4-([1-[(3-chlorophenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
0.1% inhibition at 0.01 mM
2-[4-([1-[(3-methoxyphenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
-
-
2-[4-([1-[(3-methoxyphenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
0.1% inhibition at 0.01 mM
2-[[2-(2-chlorophenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
2-[[2-(2-chlorophenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
0.1% inhibition at 0.01 mM
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
34.45% inhibition at 0.01 mM
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
-
-
2-[[2-(3,4-dimethoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
0.1% inhibition at 0.01 mM
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
56.81% inhibition at 0.01 mM
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
-
-
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(naphthalen-1-yl)acetamide
2.1% inhibition at 0.01 mM
2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
0.1% inhibition at 0.01 mM
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
-
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
-
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
-
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
-
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
-
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
-
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
not inhibitory to wild-type
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
-
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
-
3-(2-[[(4-chlorophenyl)carbamoyl]amino]propan-2-yl)-N-hydroxybenzene-1-carboximidamide
P200
3-(2-[[(4-chlorophenyl)carbamoyl]amino]propan-2-yl)-N-hydroxybenzene-1-carboximidamide
P200
3-(2-[[(4-chlorophenyl)carbamoyl]amino]propan-2-yl)-N-hydroxybenzene-1-carboximidamide
P200
3-(4-chlorophenyl)-4-(4-ethoxyphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
3-(4-chlorophenyl)-4-(4-ethoxyphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
-
-
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
-
4-(3-bromo-4-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
4-(3-bromo-4-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
4-(4-acetamidophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
4-(4-acetamidophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
4-(4-acetamidophenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
4-(4-acetamidophenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
4-(5-bromo-2-fluorophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
4-(5-bromo-2-fluorophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
4-(5-bromo-2-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
-
4-(5-bromo-2-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
-
4-acetyl-N-(3-chloro-4-fluorophenyl)-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
-
4-acetyl-N-(3-chloro-4-fluorophenyl)-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
-
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinolin-2(1H)-one
A110
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinolin-2(1H)-one
A110
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
Q81W29
-
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
-
-
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
-
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
-
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
-
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
-
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
-
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
-
uncompetitive versus IMP
6-Chloro-9-beta-D-ribofuranosylpurine 5 '-phosphate
-
covalent modification of the enzyme, total inactivation after 15 min at 0.01 mg/ml Cl-IMP, activity can be restored with 2-mercaptoethanol
6-Chloro-9-beta-D-ribofuranosylpurine 5 '-phosphate
-
50% inactivation after 90 min at 0.00012 mM Cl-IMP
6-Chloro-9-beta-D-ribofuranosylpurine 5 '-phosphate
-
-
6-Chloro-9-beta-D-ribofuranosylpurine 5 '-phosphate
-
acts at the IMP binding site
6-chloroinosine 5'-phosphate
-
-
6-chloroinosine 5'-phosphate
-
-
6-chloroinosine 5'-phosphate
-
6-Chloropurine ribonucleoside 5'-phosphate
-
inosine 5'-phosphate and guanosine 5'-phosphate retard inactivation
6-Chloropurine ribonucleoside 5'-phosphate
-
-
6-thioinosine 5'-phosphate
-
complete inactivation after 10 min preincubation at a concentration of 0.001 mM; in absence of glutathione
6-thioinosine 5'-phosphate
-
in absence of glutathione
7-amino-5-(4-chlorophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
-
7-amino-5-(4-chlorophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
7-amino-5-(4-nitrophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
-
7-amino-5-(4-nitrophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
7-amino-5-(5-nitrothiophen-2-yl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
-
7-amino-5-(5-nitrothiophen-2-yl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
-
9-(5-O-[hydroxy[([hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]oxy)methyl]phosphoryl]-beta-L-ribofuranosyl)-9H-purin-6-amine
inhibition of leukemia K562 cells proliferation, IC50 of 71.3 microM
9-(5-O-[hydroxy[([hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]oxy)methyl]phosphoryl]-beta-L-ribofuranosyl)-9H-purin-6-amine
homology modeling; homology modeling
ADP
multiple inhibition with tiazofurin, competitive versus NAD+
ADP
binds in the adenosine portion, tiazofurin and ADP are strongly synergistic inhibitors, a conformational change occurs upon the binding of one inhibitor that increases the affinity of the second inhibitor
AMP
-
-
AMP
-
20% inhibition at high concentrations
ATP
-
at high concentration of IMP and KCl
benzamide riboside
-
NAD+ binding site inhibitor
benzamide riboside
displays skeletal muscle toxicity in preclinical trials, which limits its utility; displays skeletal muscle toxicity in preclinical trials, which limits its utility
benzamide riboside
inhibitory activity is higher than tiazofurin and lower than selenazofurin; inhibitory activity is higher than tiazofurin and lower than selenazofurin
beta-methylene thiazole 4-carboxamide adenine dinucleotide
-
i.e. beta-Me-TAD or CH2-TAD
beta-methylene thiazole 4-carboxamide adenine dinucleotide
-
i.e. beta-Me-TAD
BMS-337197
-
isozyme IMPDH II IC50: 16 nM
BMS-337197
-
i.e. BMS-337197
BMS-337197
-
IC50: 0.0082 mM
BMS-337197
-
is a potent IMPDH inhibitor, shows in vivo activity for inhibition of antibody production in mice
BMS-337197
-
is a potent IMPDH inhibitor, shows in vivo activity for inhibition of antibody production in the adjuvant-induced arthritis model in rats
C2-mycophenolic adenine dinucleotide
-
methylenephosphophosphonate analogue of mycophenolic adenine dinucleotide
C2-mycophenolic adenine dinucleotide
-
-
Ca2+
-
competitive inhibition with respect to both K+ and NAD+
Ca2+
-
29% inactivation in the presence of 0.1M K+
curcumin
-
significantly reduces the level of GTP and reduces the rate of cell growth
curcumin
0.1 mM, 68% inhibition, both competitive and uncompetitive
cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone
-
uncompetitive inhibition with respect to IMP and NAD+
cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone
VCC234718
EICARMP
-
-
eicosadienoic acid
competitive inhibitor versus IMPDH; competitive inhibitor versus IMPDH
eicosadienoic acid
-
competitive to inosine 5'-phosphate
GDP
-
GDP
-
45% inhibition at 0.6 mM
GMP
-
GMP
-
competitive, 58% inhibition at 0.5 mM
GMP
-
competitive with respect to IMP
GMP
-
competitive with respect to IMP and non competitive with respect to NAD+
GMP
-
competitive with respect to IMP
GMP
-
weak and competitive inhibition, strong binding, dissociation by 3 M urea
GMP
-
competitive with respect to IMP
GMP
-
competitive with respect to IMP, non competitive with respect to NAD+ and K+
GMP
-
competitive with respect to IMP
GMP
-
feedback inhibitor; feed-back inhibitor eliciting 'allosteric' kinetics of the enzyme, determination of the GMP binding site
GMP
-
55% inhibition at 0.6 mM
GTP
-
-
GTP
-
45% inhibition at 0.6 mM
imidazo[4,5-e][1,4]diazapine
-
-
imidazo[4,5-e][1,4]diazapine
-
fat base nucleotide, inosine 5'-phosphate but not NAD+ protects against inhibition
imidazo[4,5-e][1,4]diazapine
-
-
imidazo[4,5-e][1,4]diazapine
fat base nucleotide, inosine 5'-phosphate but not NAD+ protects against inhibition; fat base nucleotide, inosine 5'-phosphate but not NAD+ protects against inhibition
iodoacetate
-
-
iodoacetate
-
98% inhibition at 10 mM
Li+
-
Li+
-
competitive inhibition with respect to both K+ and NAD+
Li+
-
inhibits stimulatory effect of K+
linoleic acid
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
antagonizes ADP binding
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
not inhibitory to wild-type
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
-
Mg2+
-
inhibits K+ activation
Mg2+
-
competitive inhibition with respect to both K+ and NAD+
Mg2+
-
inhibits K+ activation
Mg2+
-
inhibits K+ activation
mizoribine
-
-
mizoribine
competitive inhibitor
mizoribine 5'-phosphate
competitive versus NAD+, slow tight-binding, the mutant A251T is 20fold more sesitive
mizoribine 5'-phosphate
-
complexes the enzyme
mizoribine monophosphate
-
-
mizoribine monophosphate
-
-
mizoribine monophosphate
-
-
mizoribine monophosphate
-
-
mizoribine monophosphate
-
-
mycophenolate mofetil
-
NAD+ binding site inhibitor
mycophenolate mofetil
-
-
mycophenolate mofetil
-
prodrug of mycophenolic acid, treatment of diet-induced obese mice with mycophenolate mofetil for 28 days does not affect food intake or lean body mass but reduces body fat content (by 36%), adipocyte size and number and the appearance of hepatic steatosis
Mycophenolic acid
inhibitory to enzyme, also inhibits growth of Babesia gibsoni cells. The treated parasite cultures have predominantly single Babesia cells as opposed to untreated cells that have both single and dividing forms as observed on day two
Mycophenolic acid
Q81W29
noncompetitive with regard to inosine monophosphate and NAD+
Mycophenolic acid
-
uncompetitive with respect to IMP and NAD+
Mycophenolic acid
inhibition of the wild-type enzyme uncompetitively versus NAD+, the mutant A251T enzyme is 4fold more resistant to mycophenolic acid
Mycophenolic acid
-
uncompetitive
Mycophenolic acid
subtype MMRL2651 of Cryptococcus gattii is naturally resistant to inhibition by mycophenolic acid
Mycophenolic acid
-
50% inhibition at 0.0003 mM, reversible by guanine
Mycophenolic acid
-
50% inhibition at 0.00025 mM, human plasma or serum reduces the inhibition
Mycophenolic acid
-
mutants have increased Ki for MPA
Mycophenolic acid
-
type II enzyme is 4.8fold more sensitive than type I
Mycophenolic acid
-
key binding interactions for the benzofuranone residue mycophenolic acid and the N-[3-methoxy-4-(5-oxazolyl)phenyl] fragment of VX-497, the benzofuranone ring mycophenolic acid binds in a spatially restricted region of the NAD+ binding site packing with the hypoxanthine ring xanthosine 5'-phosphate, the carbonyl oxygen and hydroxy residues are involved in a hydrogen bond array that involves Gly326, Thr333 and Gln441, the appending methyl substituent of the benzofuranone system, resides in a small hydrophobic pocket defined by the planes of Asn303 amide and Arg322 guanidine, the phenyl oxazole moiety of VX-497 binds in the same region as the benzofuranone ring of mycophenolic acid, forming hydrogen bonds between the oxazole nitrogen and oxygen with Gly326 and possibly Thr333, respectively, the methoxy residue binds in the same pocket as the benzofuranone methyl in mycophenolic acid
Mycophenolic acid
-
isozyme IMPDH II IC50: 15 nM
Mycophenolic acid
-
potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil, isozyme IMPDH II IC50: 14 nM
Mycophenolic acid
-
potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil
Mycophenolic acid
-
isozyme IMPDH II IC50: 11 nM, potent, uncompetitive inhibition, immunosuppressive drug, prodrug is mycophenolate mofetil
Mycophenolic acid
-
enzyme inhibition by mycophenolic acid impairs maturation and function of dendritic cells
Mycophenolic acid
-
traps the reaction intermediate E-XMP, the human enzyme is sensitive to the inhibitor due to its open dehydrogenase conformation
Mycophenolic acid
-
uncompetitive inhibition, the interaction with the enzyme, inducing striking conformational changes and aggregation, is regulated by GTP, GTP reverses the enzyme aggregation by inhibitor mycophenolic acid, the inhibitor is part of an immunosuppressive drug
Mycophenolic acid
-
IC50: 99.2 nM with umbilical vein endothelial cells, 128 nM with Jurkat cells, inhibits the enzyme in vivo and in vitro, mycophenolic acid inhibits tumor-associated angiogenesis and is used as clinical drug in immunosuppression
Mycophenolic acid
-
exerts immunosuppression through inhibition of the enzyme in lymphocytes, inhibitory potency in vivo, overview, prodrug is mycophenolate mofetil
Mycophenolic acid
-
comparison with inhibition of histone deacetylase and K562 cell proliferation
Mycophenolic acid
-
biphasic concentration-dependent influence on inosine 5'-phosphate dehydrogenase basal activity. At concentrations around or below IC50 value, mycophenolic acid increases the basal enzymic activity, associated with elevated expression of isoform IMPDH2. Despite increased expression, the basal enzyme activity decreases following exposure to high mycophenolic acid concentrations
Mycophenolic acid
-
uncompetitive inhibition
Mycophenolic acid
-
IMPDH activity in erythrocytes is inhibited at the peak plasma concentration of mycophenolic acid in initial kidney transplant recipients. Reduction does not coincide with the peak of the plasma concentration of phenolic and acyl glucuronides of mycophenolic acid
Mycophenolic acid
is a uncompetitive inhibitor of IMPDH with respect to both inosine 5'-phosphate and NAD+, inhibits IMPDH by trapping the covalent intermediate. It it is easily converted to mycophenolic acid-7-O-glucuronide, which limits the inhibitory efficacy and higher doses are therefore needed in order to maintain appropriate therapeutic levels; is a uncompetitive inhibitor of IMPDH with respect to both inosine 5'-phosphate and NAD+, inhibits IMPDH by trapping the covalent intermediate. It it is easily converted to mycophenolic acid-7-O-glucuronide, which limits the inhibitory efficacy and higher doses are therefore needed in order to maintain appropriate therapeutic levels
Mycophenolic acid
-
new enzymatic mycophenolic acid assay, cross-reactivity by mycophenolic acid-acyl-glucuronide is less than 5%, thus interference is expected to be clinically irrelevant
Mycophenolic acid
inhibition of leukemia K562 cells proliferation, IC50 of 7.7 microM; inhibition of leukemia K562 cells proliferation, IC50 of 7.7 microM
Mycophenolic acid
a natural product and a reversible, potent and uncompetitive inhibitor of IMPDH
Mycophenolic acid
reversible, potent, uncompetitive inhibitor, 99.9% inhibition at 0.01 mM
Mycophenolic acid
-
mixed type inhibition
Mycophenolic acid
-
in 3T3-L1 preadipocytes inhibition of IMPDH with mycophenolic acid reduces intracellular GTP levels by 60% (p <0.05) and blocks adipogenesis. Co-treatment with guanosine restores GTP levels and adipogenesis
Mycophenolic acid
complete inhibition at 0.01 mM, 83% inhibition at 0.05 mM
Mycophenolic acid
-
50% inhibition at 0.024 mM
Mycophenolic acid
-
IMD2 imparts mycophenolic acid resistance due to A253S as a critical amino acid substitution
Mycophenolic acid
uncompetitive to NAD+
Mycophenolic acid
-
i.e. MPA, slight inhibition, microbial IMPDHs differ from mammalian enzymes in their lower affinity for inhibitors such as mycophenolic acid and thiazole-4-carboxamide adenine dinucleotide, part of this resistance is determined by the coupling between nicotinamide and adenosine subsites in the NAD+ binding site that is postulated to involve an active site flap
Mycophenolic acid
82.99% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity
Mycophenolic acid
99.60% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity
Mycophenolic acid
-
90.53% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity
mycophenolic acid-acyl-glucuronide
-
uncompetitive inhibition, is a weaker inhibitor of IMPDH II than mycophenolic acid. When coincubated with mycophenolic acid, mycophenolic acid-acyl-glucuronide activity is negligible at pharmacological concentrations
mycophenolic acid-acyl-glucuronide
-
cross-reactivity by mycophenolic acid is less than 5%, thus interference is expected to be clinically irrelevant
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-([4-oxo-2-[2-(thiophen-2-yl)phenyl]-4H-1-benzopyran-3-yl]oxy)acetamide
-
-
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-([4-oxo-2-[2-(thiophen-2-yl)phenyl]-4H-1-benzopyran-3-yl]oxy)acetamide
0.1% inhibition at 0.01 mM
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
-
-
N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
0.1% inhibition at 0.01 mM
N-(2-{3-[(1E)-N-(2-aminoethoxy)ethanimidoyl]phenyl}propan-2-yl)-N'-(4-chloro-3-nitrophenyl)urea
an inhibitor with in vivo anticryptosporidial activity, binding structure determination and analysi, P131 contains two aromatic groups, one of which interacts with the hypoxanthine ring of IMP, while the second interacts with the aromatic ring of a tyrosine in the adjacent subunit. In addition, the amine and NO2 moieties bind in hydrated cavities, forming water-mediated hydrogen bonds to the proteins. The oxime group of P131 lies across the hypoxanthine ring of IMP, while the N5 amine forms hydrogen bonds to the main chain carbonyl O atom of Gly212 and N3 of IMP in all of the subunits
N-(2-{3-[(1E)-N-(2-aminoethoxy)ethanimidoyl]phenyl}propan-2-yl)-N'-(4-chloro-3-nitrophenyl)urea
-
P131
N-(2H-indazol-6-yl)-3,5-dimethyl-1H-pyrazole-4-sulfonamide
TBK6
N-(2H-indazol-6-yl)-3,5-dimethyl-1H-pyrazole-4-sulfonamide
TBK6
N-(4-bromophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
crystallization data. Poor inhibition of human IMPDH2
N-(4-bromophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
-
N-(4-bromophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(4-bromophenyl)-2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
-
-
N-(4-bromophenyl)-2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
0.1% inhibition at 0.01 mM
N-(4-bromophenyl)-2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
-
-
N-(4-bromophenyl)-2-[[2-(4-methylphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]acetamide
0.1% inhibition at 0.01 mM
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
-
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
-
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
-
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
-
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
-
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
-
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
-
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
-
N-(4-chloro-3-methoxyphenyl)-2-(4-oxo[1]benzopyrano[4,3-c]pyrazol-1(4H)-yl)acetamide
-
N-(4-chloro-3-methoxyphenyl)-2-(4-oxo[1]benzopyrano[4,3-c]pyrazol-1(4H)-yl)acetamide
-
-
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
-
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
N-(4-chlorophenyl)-2-phenoxypropanamide
antagonizes ADP binding
N-(4-chlorophenyl)-2-phenoxypropanamide
-
-
N-(4-chlorophenyl)-2-phenoxypropanamide
-
-
N-(4-chlorophenyl)-2-phenoxypropanamide
-
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
-
-
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
binds in the nicotinamide subsite and does not interact with ADP
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
not inhibitory to wild-type
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(naphthalen-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(naphthalen-1-yl)acetamide
-
-
N-(4-methoxyphenyl)-2-(naphthalen-1-yl)acetamide
-
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
binds in the nicotinamide subsite and does not interact with ADP
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
not inhibitory to wild-type
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-1-yl)-2-[(4-oxo-2-phenyl-4H-1-benzopyran-3-yl)oxy]acetamide
-
-
N-(naphthalen-1-yl)-2-[(4-oxo-2-phenyl-4H-1-benzopyran-3-yl)oxy]acetamide
0.1% inhibition at 0.01 mM
N-(naphthalen-1-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
-
-
N-(naphthalen-1-yl)-2-[[4-oxo-2-(3,4,5-trimethoxyphenyl)-4H-1-benzopyran-3-yl]oxy]acetamide
16.54% inhibition at 0.01 mM
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
poor inhibition of human IMPDH2
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Q81W29
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
C91
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
C91
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
C91
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
C91, 0.197% inhibition at 0.01 mM
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
not inhibitory to wild-type
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
-
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
-
N-[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenyl]-beta-D-xylofuranosylamine
P176; P221
N-[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenyl]-beta-D-xylofuranosylamine
P176; P221
N-[4-(1-benzyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl]acetamide
-
-
N-[4-(1-benzyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl]acetamide
-
N-[4-chloro-3-(alpha-D-ribofuranosyloxy)phenyl]-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
P178
N-[4-chloro-3-(alpha-D-ribofuranosyloxy)phenyl]-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
P178
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
-
N-[4-chloro-3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]phenyl]-N'-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
P182
N-[4-chloro-3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]phenyl]-N'-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
P182
N-[4-chloro-3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]phenyl]-N'-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
P182
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
a competitive inhibitor versus NAD+, that has a strong preference for E-IMP, enzyme binding structure analysis, overview
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
-
Na+
-
Na+
-
competitive inhibition with respect to both K+ and NAD+
NAD+
Q81W29
-
NAD+
-
substrate inhibition
NAD+
-
substrate inhibition at high concentration
NAD+
-
substrate inhibition
NAD+
-
substrate inhibition
NAD+
substrate inhibition
NAD+
-
at high concentration, inhibition of canonical isoform. No inhibition of retinal-specific isoforms
NAD+
-
substrate inhibition at high concentration
NAD+
low substrate inhibition
NAD+
substrate inhibition
NAD+
-
substrate inhibition at high concentration
NAD+
-
50% inhibition at 0.62 mM
NAD+
-
44% inhibition at 1.5 M
NAD+
substrate inhibition
NAD+
-
substrate inhibition
NADH
-
-
NADH
-
mixed inhibition type versus inosine 5'-phosphate and NAD+
NADH
-
non competitive with respect to K+, IMP and NAD
NADH
-
poor inhibitor, product inhibition, non competitive
NADH
-
non competitive with respect to NAD+
NADH
product inhibition, noncompetitive versus IMP, NAD+, and K+
NADH
-
uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+
oxanosine monophosphate
potent reversible competitive inhibitor
oxanosine monophosphate
-
oxanosine monophosphate
potent reversible competitive inhibitor
oxanosine monophosphate
-
potent reversible competitive inhibitor
oxanosine monophosphate
potent reversible competitive inhibitor
oxanosine monophosphate
-
potent reversible competitive inhibitor
p-chloromercuribenzoate
-
100% inhibition at 0.021 mM
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
inhibition can be restored by addition of DTT
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
-
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
-
-
Pentamidine
complete inhibition at 500 ng/ml
Pentamidine
complete inhibition at 500 ng/ml
Pentamidine
-
complete inhibition at 500 ng/ml
ribavirin
-
-
ribavirin
1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide, a prodrug of corresponding 5-monophosphate, which as a competitive inhibitor interacts with the IMP domain of IMPDH; 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide, a prodrug of corresponding 5-monophosphate, which as a competitive inhibitor interacts with the IMP domain of IMPDH
ribavirin
competitive inhibitor
ribavirin
Parainfluenza virus
-
potent competitive inhibition, shows anti-viral activity in vivo, detailed overview
ribavirin
-
potent competitive inhibition, shows anti-viral activity in vivo, detailed overview
ribavirin 5'-monophosphate
-
-
ribavirin 5'-monophosphate
-
competitive with respect to IMP
ribavirin 5'-monophosphate
-
-
ribavirin 5'-monophosphate
-
ribavirin 5'-monophosphate
-
ribavirin 5'-phosphate
-
-
ribavirin 5'-phosphate
-
-
ribavirin monophosphate
-
-
ribavirin monophosphate
-
-
ribavirin monophosphate
-
ribavirin monophosphate
-
-
ribavirin monophosphate
-
-
ribavirin monophosphate
-
-
S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate
16.47% inhibition at 0.001 mg
S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate
6.51% inhibition at 0.001 mg
S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate
-
12.79% inhibition at 0.001 mg
Selenazofurin
-
inhibition (in vivo) by the NAD analog formed intracellularly
Selenazofurin
Parainfluenza virus
-
potent competitive inhibition, shows anti-viral activity in vivo, detailed overview, a complete reversal of the antiviral activity of selenazofurin was obtained by addition of guanosine and selenazofurin at varying concentrations
Selenazofurin
-
potent competitive inhibition, shows anti-viral activity in vivo, detailed overview
tetrasodium 6,6'-[(3,3'-dimethoxy[1,1'-biphenyl]-4,4'-diyl)bis[(E)-diazene-2,1-diyl]]bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate)
-
-
tetrasodium 6,6'-[(3,3'-dimethoxy[1,1'-biphenyl]-4,4'-diyl)bis[(E)-diazene-2,1-diyl]]bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate)
-
thiazole-4-carboxamide adenine dinucleotide
-
uncompetitive with respect to IMP and NAD
thiazole-4-carboxamide adenine dinucleotide
-
-
thiazole-4-carboxamide adenine dinucleotide
-
inhibition is strong and not reversible by NAD+; thiazole-4-carboxamide adenine dinucleotide acts non competitive
thiazole-4-carboxamide adenine dinucleotide
-
reversible inhibition
thiazole-4-carboxamide adenine dinucleotide
-
i.e. TAD, mixed inhibition type versus inosine 5'-phosphate and NAD+
thiazole-4-carboxamide adenine dinucleotide
-
inhibitory mechanism
thiazole-4-carboxamide adenine dinucleotide
-
i.e. TAD, synthesis, noncompetitive inhibition, conformational analysis, and biological activity of inhibitor analogues, overview, TAD binds to the NAD+ binding site with out isozyme specificity, mechanism and molecular modeling using the enzyme crystal structure, overview, cytotoxic against K562 tumor cells
thiazole-4-carboxamide adenine dinucleotide
inhibition of leukemia K562 cells proliferation, IC50 of 3.7 microM; inhibition of leukemia K562 cells proliferation, IC50 of 3.7 microM
thiazole-4-carboxamide adenine dinucleotide
-
-
thiazole-4-carboxamide adenine dinucleotide
-
i.e. TAD, uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+
thiazole-4-carboxamide adenine dinucleotide
-
i.e. TAD, slight inhibition, microbial IMPDHs differ from mammalian enzymes in their lower affinity for inhibitors such as mycophenolic acid and thiazole-4-carboxamide adenine dinucleotide, part of this resistance is determined by the coupling between nicotinamide and adenosine subsites in the NAD+ binding site that is postulated to involve an active site flap
tiazofurin
multiple inhibition with ADP, noncompetitive versus NAD+
tiazofurin
-
decrease of cell growth
tiazofurin
-
i.e. 2-beta-D-ribofuranosyl-thiazole-4-carboxamide, overview: clinical and molecular impact of inhibition; the drug is tested in clinical use to treat acute myelocytic leukemia, AML, detailed overview, tiazofurin treatment may result in induced differentiation of leukemic leukocytes in patients, incubation of K-562 cells with tiazofurin produces inhibition of IMP DH and decreases GTP concentration, these biochemical alterations are followed by a decrease in the expression of as proto-oncogene which is followed by induced differentiation of these cells, biochemical mechanism, overview
tiazofurin
-
noncompetitive inhibition, cytotoxic against K562 tumor cells
tiazofurin
competitive inhibitor
tiazofurin
Parainfluenza virus
-
-
tiazofurin
-
inhibits cell proliferation of hepatoma cells, overview
tiazofurin
binds in the nicotinamide portion of the dinucleotide site, tiazofurin and ADP are strongly synergistic inhibitors, a conformational change occurs upon the binding of one inhibitor that increases the affinity of the second inhibitor
VX-148
-
isozyme IMPDH II IC50: 6 nM
VX-148
has immunosuppressive activity; has immunosuppressive activity
VX-497
-
key binding interactions for the benzofuranone residue mycophenolic acid and the N-[3-methoxy-4-(5-oxazolyl)phenyl] fragment of VX-497, the benzofuranone ring mycophenolic acid binds in a spatially restricted region of the NAD+ binding site packing with the hypoxanthine ring xanthosine 5'-phosphate, the carbonyl oxygen and hydroxy residues are involved in a hydrogen bond array that involves Gly326, Thr333 and Gln441, the appending methyl substituent of the benzofuranone system, resides in a small hydrophobic pocket defined by the planes of Asn303 amide and Arg322 guanidine, the phenyl oxazole moiety of VX-497 binds in the same region as the benzofuranone ring of mycophenolic acid, forming hydrogen bonds between the oxazole nitrogen and oxygen with Gly326 and possibly Thr333, respectively, the methoxy residue binds in the same pocket as the benzofuranone methyl in mycophenolic acid
VX-497
-
isozyme IMPDH II IC50: 11 nM
xanthosine 5'-phosphate
Q81W29
competitive with regard to inosine monophosphate
xanthosine 5'-phosphate
-
39% competitive, inhibition at 0.5 mM
xanthosine 5'-phosphate
-
competitive with respect to IMP
xanthosine 5'-phosphate
-
-
xanthosine 5'-phosphate
-
competitive versus inosine 5'-phosphate but noncompetitive versus NAD+
xanthosine 5'-phosphate
-
-
xanthosine 5'-phosphate
-
competitive with respect to IMP
xanthosine 5'-phosphate
-
-
xanthosine 5'-phosphate
-
non-competitive with respect to NAD
xanthosine 5'-phosphate
-
competitive with respect to IMP, non competitive with respect to NAD and K+
xanthosine 5'-phosphate
-
product inhibitor
xanthosine 5'-phosphate
-
competitive inhibition
xanthosine 5'-phosphate
-
competitive with respect to IMP
xanthosine 5'-phosphate
-
competitive inhibition
xanthosine 5'-phosphate
-
competitive versus inosine 5'-phosphate but noncompetitive versus NAD+
xanthosine 5'-phosphate
-
-
xanthosine 5'-phosphate
-
-
XMP
product inhibition
XMP
product inhibition, competitive versus IMP, noncompetitive versus NAD+ and K+
[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenoxy]acetic acid
P225
[2-chloro-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]phenoxy]acetic acid
P225
additional information
-
the enzyme is not inhibited by mycophenolic acid
-
additional information
-
inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variants, overview
-
additional information
-
-
-
additional information
-
overview
-
additional information
-
inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variant, overview
-
additional information
-
inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variant, overview
-
additional information
-
1,2,3-triazole containing ether IMPDH inhibitors, small alkyl group on the alpha-position of the ether is required, with the (R)-enantiomer significantly more active than the (S)-enantiomer. Electron-withdrawing groups in the 3- and/or 4-positions of the pendent phenyl ring are best, and conversion of the quinoline containing inhibitors to quinoline-N-oxides retains inhibitory activity both in the presence and absence of bovine serum albumin
-
additional information
-
overview
-
additional information
-
dinucleotide analogs of NAD
-
additional information
-
overview
-
additional information
-
no enzyme inhibition by nucleic acids
-
additional information
-
compounds are not inhibitory to Escherichia coli, Tritrichomonas foetus, and Leishmania donovani IMPDH. Susceptible enzymes are defined by structural motif A165/Y358, Cryptosporidium parvum numbering
-
additional information
-
inhibition by purine and pyrimidine compounds
-
additional information
-
mycophenolic acid and it's nuclear variants
-
additional information
-
-
-
additional information
-
overview
-
additional information
-
6-ethoxycarbonyl-3,3-disubstituted-1,5-diazabicyclo[3.1.0.]hexane-2,4-diones inhibit type II enzyme
-
additional information
-
no enzyme inhibition by nucleic acids
-
additional information
-
determination and analysis of structure-activity relationships of the different inhibitor molecules, overview
-
additional information
-
development and synthesis of inhibitors, determination and analysis of structure-activity relationships of the different inhibitor molecules with isozyme IMPDH II, overview
-
additional information
-
optimization of nitrile containing drugs, such as VX-148, by combining them with an oxazole moiety which is very reactive in inhibition, overview
-
additional information
-
synthesis, inhibitory potency, and structure-activity relationship of enzyme with phosphonic acid-containing analogues of mycophenolic acid inhibitors, IC50 values, overview
-
additional information
-
the enzyme is resistant to mizoribine 5'-phosphate due to its open dehydrogenase conformation in opposite to the bacterial enzyme which has a closed hydrolase conformation
-
additional information
-
inhibitor development and synthesis, overview
-
additional information
-
inhibition of the enzyme in K562 cells sensitizes the before resistant cells to methotrexate
-
additional information
-
retinal isoforms do not bind significant fractions of a random pool of oligonucleotides
-
additional information
IMPDH2 interacts with protein kinase B/Akt via its plekstrin homology domain, the resulting phosphorylation reduces activity
-
additional information
IMPDH2 interacts with protein kinase B/Akt via its plekstrin homology domain, the resulting phosphorylation reduces activity
-
additional information
-
mycophenolic acid-phenyl-glucuronide has no effect
-
additional information
involvement of three conserved water molecules (W(L), W(M), and W(C)) in the recognition of catalytic residues (R 322, D 364, and N 303) to inhibitor
-
additional information
-
involvement of three conserved water molecules (W(L), W(M), and W(C)) in the recognition of catalytic residues (R 322, D 364, and N 303) to inhibitor
-
additional information
-
IMPDH activity decreases more than 10% with increasing contamination by erythrocytes due to increasing AMP and protein content. Storage of lithium heparin blood samples at room temperature for 24 hours before peripheral blood mononuclear cell isolation does not lead to any significant changes in the IMPDH activity, when the activity is normalized to the AMP concentration
-
additional information
synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH; synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH
-
additional information
synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH; synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH
-
additional information
-
tacrolimus, cyclosporine and prednisolone do not affect IMPDH activity
-
additional information
structure- and ligand-based IMPDH inhibitor development, molecular modeling studies, overview
-
additional information
-
structure- and ligand-based IMPDH inhibitor development, molecular modeling studies, overview
-
additional information
inhibitor synthesis, analysis and comparison of potencies against isozymes IMPDH1 and IMPDH2, overview; inhibitor synthesis, analysis and comparison of potencies against isozymes IMPDH1 and IMPDH2, overview
-
additional information
inhibitor synthesis, analysis and comparison of potencies against isozymes IMPDH1 and IMPDH2, overview; inhibitor synthesis, analysis and comparison of potencies against isozymes IMPDH1 and IMPDH2, overview
-
additional information
enzyme cytoophidia are catalytically active and resistant to GDP allosteric inhibition
-
additional information
-
enzyme cytoophidia are catalytically active and resistant to GDP allosteric inhibition
-
additional information
-
-
-
additional information
no inhibition by tiazofurin and benzamide
-
additional information
-
no inhibition by tiazofurin and benzamide
-
additional information
-
-
-
additional information
-
not inhibitory: linoelaidic acid, methyl linoleate, cis-9-octadecen-1-ol
-
additional information
not inhibitory: resveratrol, genistein, eugenol, gingerol, naringenin, naringin, caffeic acid, morin, kaempferol, hesperidin, rosmarinic acid
-
additional information
IMPDH has multiple active site states that can be targeted for inhibitor design, and both the IMP/XMP and cofactor binding sites are exploited for that purpose, inhibitor screening of compounds with antitubercular activity, overview. Mechanism of MtbIMPDH2DELTACBS enzyme mutant inhibition
-
additional information
-
IMPDH has multiple active site states that can be targeted for inhibitor design, and both the IMP/XMP and cofactor binding sites are exploited for that purpose, inhibitor screening of compounds with antitubercular activity, overview. Mechanism of MtbIMPDH2DELTACBS enzyme mutant inhibition
-
additional information
several inhibitors compete with the flap for the vacant NADH site, thus preventing the hydrolysis of E-XMP* reaction intermediate
-
additional information
-
the enzyme is not inhibited by mycophenolic acid
-
additional information
-
inhibition by products and antimetabolites
-
additional information
-
overview
-
additional information
no inhibition by tiazofurin and seleno-thiazofurin
-
additional information
-
no inhibition by tiazofurin and seleno-thiazofurin
-
additional information
-
-
-
additional information
-
overview
-
additional information
-
no enzyme inhibition by nucleic acids
-
additional information
-
structural basis of the drug selectivity, overview
-
additional information
becomes resistant to IMPDH inhibitors by rearranging its purine salvage pathways to rely on xanthine instead of hypoxanthine
-
additional information
-
inhibitor synthesis, overview
-
additional information
-
the enzyme is not affected by allantoin, allantoic acid, uric acid, inosine, xanthosine, and xanthosine 5'-phosphate
-
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0.00048 - 0.00055
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
0.00044
(2R)-2-phenyl-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.000014
(2S)-2-(2,3-dichloroanilino)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000096
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(2-hydroxyphenyl)-1,3-benzoxazol-5-yl]propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000076
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
0.00004
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-6-yl]propanamide
pH 8.0, 22°C
0.000039
(2S)-2-(2,3-dichlorophenoxy)-N-[2-[4-(N'-hydroxycarbamimidoyl)phenyl]-1,3-benzoxazol-5-yl]propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00062
(2S)-2-(2,3-dimethoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.00013
(2S)-2-(2-chloro-3-nitrophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.0001
(2S)-2-(2-chlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.000151 - 0.0004
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
0.000681
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.000041 - 0.00034
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.000046 - 0.00035
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.000042 - 0.00013
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00087
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
-
at pH 8.0 and 25°C
0.00011 - 0.00035
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00018 - 0.00027
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.0017
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.000016 - 0.00023
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.0004 - 0.0011
(5E)-N-hydroxy-7-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-5-methylhept-5-enamide
0.000012
(S)-2-(2,3-dichlorophenoxy)-N-(2-(2-methoxypyridin-4-yl)benzo-[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00022
(S)-2-(2,3-dichlorophenoxy)-N-(2-(2-oxo-1,2-dihydropyridin-4-yl)benzo[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000085
(S)-2-(2,3-dichlorophenoxy)-N-(2-(3-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000046
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl)benzo-[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.0000023
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl)benzo[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000049
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(hydrazinecarbonyl)phenyl)-benzo[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.0000043
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-(trifluoromethoxy)phenyl)-benzo[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000035
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-fluorophenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00005
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.0000069
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000027
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanethioamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00016
(S)-2-(2,3-dichlorophenoxy)-N-(2-(4-methoxyphenyl)imidazo-[1,2-a]pyridin-6-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00002
(S)-2-(2,3-dichlorophenoxy)-N-(2-(6-methoxypyridin-3-yl)benzo-[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00004
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-fluorophenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000121
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-hydroxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000019
(S)-2-(2,3-difluorophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000042
(S)-2-(2,3-difluorophenoxy)-N-(2-(6-methoxypyridin-3-yl)benzo-[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000055
(S)-2-(2,3-difluorophenoxy)-N-(2-(pyridin-4-yl)benzo[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000023
(S)-2-(2-(aminomethyl)phenoxy)-N-(2-(4-methoxyphenyl)benzo-[d]oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00043
(S)-2-(2-(benzyloxy)phenoxy)-N-(2-(4-cyanophenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00004
(S)-2-(2-cyano-3-fluorophenoxy)-N-(2-(pyridin-4-yl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000033
(S)-2-(2-cyanophenoxy)-N-(2-(4-methoxyphenyl)benzo[d]-oxazol-5-yl)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000076
(S)-2-(2-cyanophenoxy)-N-(2-(pyridin-4-yl)benzo[d]oxazol-5-yl)-propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000055
(S)-2-(3-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]-oxazol-2-yl)phenoxy)acetic acid
isoform IMPDH2, at pH 8.0 and 37°C
0.000018
(S)-2-(4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]-oxazol-2-yl)phenoxy)acetic acid
isoform IMPDH2, at pH 8.0 and 37°C
0.00063
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)-N-hydroxybenzamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000064
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)benzamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00036
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)benzoic acid
isoform IMPDH2, at pH 8.0 and 37°C
0.00007
(S)-4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo[d]oxazol-2-yl)pyridine-1-oxide
isoform IMPDH2, at pH 8.0 and 37°C
0.00129
(S)-N-(2-(2,3-dichlorophenoxy)propyl)-2-(4-methoxyphenyl)-benzo[d]oxazol-5-amine
isoform IMPDH2, at pH 8.0 and 37°C
0.000051
(S)-N-(2-(4-(1H-tetrazol-5-yl)phenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00024
(S)-N-(2-(4-(aminomethyl)phenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.00037
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-((1-hydroxy-1,3-dihydrobenzo-[c][1,2]oxaborol-7-yl)oxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000009
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-((2,3-dichlorophenyl)amino)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000022
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3,4-trifluorophenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000012
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3-dichlorophenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.0000072
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2,3-difluorophenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000036
(S)-N-(2-(4-cyanophenyl)benzo[d]oxazol-5-yl)-2-(2-hydroxyphenoxy)propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.0011 - 0.0014
2'-methylthiazole-4-carboxamide adenine dinucleotide
0.002
2-(2,4-dichlorophenoxy)-N-[2-(pyridin-2-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.00024
2-(2-chlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.00015
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
0.115
2-beta-D-ribofuranosylthiazole-4-carboxamide 5'-phosphate
-
pH 7.4, 37°C
0.000013
2-chloro-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]-N,N-dimethylbenzamide
pH 8.0, 22°C
0.000158
2-chloro-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]benzamide
pH 8.0, 22°C
0.000035
2-chloro-N,N-diethyl-5-[[(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)carbamoyl]amino]benzamide
pH 8.0, 22°C
0.000017
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
0.00065
2-phenoxy-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.001
2-[2-(Z)-fluorovinyl]-inosine 5'-phosphate
-
-
0.00052 - 0.00066
3'-methylthiazole-4-carboxamide adenine dinucleotide
0.000405 - 0.00087
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
0.00158
5'-O-([1-[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]-1H-1,2,3-triazol-4-yl]methyl)adenosine
pH 8.0, 22°C
0.000034 - 0.000077
6-((E)-4-(((1-(50-deoxy-adenosin-50-yl)-1H-1,2,3-triazol-4-yl)-methyl)amino)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
0.000044 - 0.0015
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
0.078
6-chloroinosine 5'-phosphate
-
0.000007
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one
-
-
0.44 - 0.82
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethyl-9H-purin-6-amine
0.18 - 0.52
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethynyl-9H-purin-6-amine
0.31 - 0.66
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-phenyl-9H-purin-6-amine
0.17 - 0.35
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-9H-purin-6-amine
0.25 - 0.33
C2-mycophenolic adenine dinucleotide
-
pH 8.0, 25°C
0.38 - 0.52
C4-mycophenolic adenine dinucleotide
-
pH 8.0, 25°C
0.00038
CH2-SAD
pH 8.0, 37°C, recombinant enzyme
0.00098
CH2-TAD
pH 8.0, 37°C, recombinant enzyme
0.0997
curcumin
pH not specified in the publication, temperature not specified in the publication
0.0001
cyclohexyl[4-(isoquinoline-5-sulfonyl)piperazin-1-yl]methanone
-
pH and temperature not specified in the publication
0.003 - 0.0031
eicosadienoic acid
0.000023
ethyl (S)-2-(3-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)phenoxy)acetate
isoform IMPDH2, at pH 8.0 and 37°C
0.0000066
ethyl (S)-2-(4-(5-(2-(2,3-dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)phenoxy)acetate
isoform IMPDH2, at pH 8.0 and 37°C
0.000001 - 0.00005
imidazo[4,5-e][1,4]diazapine
4.5
inosine 5'-phosphate
pH 8.0, 37°C, recombinant enzyme
0.000096
methyl (S)-4-(5-(2-(2,3-Dichlorophenoxy)propanamido)benzo-[d]oxazol-2-yl)benzoate
isoform IMPDH2, at pH 8.0 and 37°C
0.0000005 - 0.000008
mizoribine
0.0033
mizoribine 5'-monophosphate
pH 8.0, 25°C
0.00000001 - 0.0000002
mizoribine 5'-phosphate
0.0005 - 0.0115
mizoribine monophosphate
0.0000002 - 10
Mycophenolic acid
0.000382 - 0.000511
mycophenolic acid-acyl-glucuronide
0.00003 - 0.00007
mycophenolic hydroxamic acid
0.0008 - 0.0028
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
0.00029 - 0.00045
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
0.0017 - 0.005
N-hydroxy-N'-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]octanediamide
0.0001
N-[2-(4-cyanophenyl)-1,3-benzoxazol-5-yl]-N2-(2,3-dichlorophenyl)-L-alaninamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000018
N-[2-(4-cyanophenyl)-1,3-benzoxazol-5-yl]-N2-(2,3-difluorophenyl)-L-alaninamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000037
N-[4-chloro-3-(morpholine-4-carbonyl)phenyl]-N'-(2-[3-[(1Z)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
pH 8.0, 22°C
0.0000032
N-[4-chloro-3-(trifluoromethyl)phenyl]-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
pH not specified in the publication, temperature not specified in the publication
0.000066 - 0.00046
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
0.00057 - 0.0014
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
0.00006
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
-
at pH 8.0 and 25°C
0.000014
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
0.00004
N~2~-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]alaninamide
pH 8.0, 22°C
0.000013 - 0.00034
oxanosine monophosphate
0.02 - 0.037
P1-(7-hydroxy-6-(ethyl-2-yl)-5-methoxy-4-methylphthalan-1-one)methylenephospho-P2-(adenosin-5'-yl)phosphonate
-
pH 8.0, 25°C
0.06 - 0.087
P1-(adenosine-5'-yl)methylenephospho-P2-(7-hydroxy-6-(ethyl-2-yl)-5-methoxy-4-methylphthalan-1-one)phosphonate
-
pH 8.0, 25°C
0.000095 - 0.0085
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
0.000007 - 0.000027
P1-(tiazofurin-5'-yl)-P2-(2-aminoadenosin-5'-yl) diphosphate
0.000001 - 0.000014
P1-(tiazofurin-5'-yl)-P2-(2-ethyladenosin-5'-yl) diphosphate
0.00001 - 0.000049
P1-(tiazofurin-5'-yl)-P2-(2-ethynyladenosin-5'-yl) diphosphate
0.000019 - 0.000084
P1-(tiazofurin-5'-yl)-P2-(2-iodoadenosin-5'-yl) diphosphate
0.00002 - 0.000143
P1-(tiazofurin-5'-yl)-P2-(2-phenyladenosin-5'-yl) diphosphate
0.00011
P1-(tiazofurin-5'-yl)-P2-(adenosin-5'-yl) diphosphate
0.02 - 0.04
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
0.07 - 0.11
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-phenyladenosin-5'-yl)methylenebis(phosphonate)
0.25 - 0.33
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(adenosin-5'-yl)methylenebis(phosphonate)
0.000012
prop-2-yn-1-yl (S)-2-(4-(5-(2-(2,3-dichlorophenoxy)-propanamido)benzo[d]oxa-zol-2-yl)phenoxy)acetate
isoform IMPDH2, at pH 8.0 and 37°C
0.00025 - 0.0032
ribavirin 5'-monophosphate
0.000065 - 0.006
ribavirin monophosphate
0.0018
SAD
pH 8.0, 37°C, recombinant enzyme
0.00002 - 0.00003
Selenazofurin
0.0018
TAD
pH 8.0, 37°C, recombinant enzyme
0.000058 - 0.0013
thiazole-4-carboxamide adenine dinucleotide
0.0001
VCC234718
-
pH and temperature not specified in the publication
0.000006 - 0.000014
VX-148
0.000007 - 0.00001
VX-497
0.03 - 0.32
xanthosine 5'-phosphate
additional information
additional information
-
0.00048
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
-
at pH 8.0 and 25°C
0.00055
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
at pH 8.0 and 25°C
0.000076
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.000076
(2S)-2-(2,3-dichlorophenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000151
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
-
at pH 8.0 and 25°C
0.0004
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
at pH 8.0 and 25°C
0.000041
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00034
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.000046
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00035
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.000042
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00013
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.00011
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00035
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.00018
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00027
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.000016
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
at pH 8.0 and 25°C
0.00023
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
at pH 8.0 and 25°C
0.0004
(5E)-N-hydroxy-7-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-5-methylhept-5-enamide
-
isoform IMPDH1, pH 8.0, 25°C
0.0011
(5E)-N-hydroxy-7-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-5-methylhept-5-enamide
-
isoform IMPDH2, pH 8.0, 25°C
0.0011
2'-methylthiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH I
0.0014
2'-methylthiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH II
0.00015
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
pH 8.0, 22°C
0.00015
2-(4-methoxyphenoxy)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
isoform IMPDH2, at pH 8.0 and 37°C
0.000017
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
pH 8.0, 22°C
0.000017
2-chloro-N,N-dimethyl-5-[([2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]carbamoyl)amino]benzamide
pH and temperature not specified in the publication
0.00052
3'-methylthiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH I
0.00066
3'-methylthiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH II
0.000405
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
-
at pH 8.0 and 25°C
0.00087
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
at pH 8.0 and 25°C
0.000034
6-((E)-4-(((1-(50-deoxy-adenosin-50-yl)-1H-1,2,3-triazol-4-yl)-methyl)amino)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
pH 8.0, 25°C
0.000077
6-((E)-4-(((1-(50-deoxy-adenosin-50-yl)-1H-1,2,3-triazol-4-yl)-methyl)amino)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
pH 8.0, 25°C
0.000044
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
pH 8.0, 25°C
0.00007
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
pH 8.0, 25°C
0.0015
6-((E)-4-(4-(adenosin-50-yl)methyl-1H-1,2,3-triazol-1-yl)-3-methylbut-2-en-1-yl)-7-hydroxy-5-methoxy-4-methylisobenzofuran-1(3H)-one
-
pH 8.0, 25°C
0.44
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethyl-9H-purin-6-amine
isoform IMPDH2, pH 8.0, 25°C
0.82
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethyl-9H-purin-6-amine
isoform IMPDH1, pH 8.0, 25°C
0.18
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethynyl-9H-purin-6-amine
isoform IMPDH2, pH 8.0, 25°C
0.52
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-ethynyl-9H-purin-6-amine
isoform IMPDH1, pH 8.0, 25°C
0.31
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-phenyl-9H-purin-6-amine
isoform IMPDH2, pH 8.0, 25°C
0.66
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-2-phenyl-9H-purin-6-amine
isoform IMPDH1, pH 8.0, 25°C
0.17
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-9H-purin-6-amine
isoform IMPDH2, pH 8.0, 25°C
0.35
9-(5-deoxy-5-([(([2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]sulfonyl)methyl)sulfonyl]amino)-b-L-ribofuranosyl)-9H-purin-6-amine
isoform IMPDH1, pH 8.0, 25°C
2 - 5
ADP
-
mutant E323A, pH 8.0, 25°C
7
ADP
-
mutant Q324A, pH 8.0, 25°C
16
ADP
pH 8.0, 25°C, recombinant mutant A251T
17
ADP
-
mutant R322A, pH 8.0, 25°C
31
ADP
-
wild-type, pH 8.0, 25°C
34
ADP
pH 8.0, 25°C, recombinant wild-type enzyme
50
ADP
-
mutant R322E, pH 8.0, 25°C
0.282
AMP
-
-
0.002
EICARMP
-
-
0.003
eicosadienoic acid
-
0.0031
eicosadienoic acid
-
pH 8.0, 37°C
0.038
FFAD
with inosine 5'-phosphate as substrate
0.056
FFAD
with inosine 5'-phosphate as substrate
0.008
GMP
at pH 8.0 and 25°C
0.021
GMP
-
at pH 8.0 and 25°C
0.024
GMP
-
at pH 8.0 and 25°C
0.037
GMP
at pH 8.0 and 25°C
0.115
GMP
at pH 8.0 and 25°C
0.000001
imidazo[4,5-e][1,4]diazapine
-
0.00005
imidazo[4,5-e][1,4]diazapine
-
IMPDH2
0.0000005
mizoribine
-
-
0.00000001
mizoribine 5'-phosphate
pH 8.0, 25°C, recombinant mutant A251T
0.0000002
mizoribine 5'-phosphate
pH 8.0, 25°C, recombinant wild-type enzyme
0.0005
mizoribine monophosphate
-
-
0.0005
mizoribine monophosphate
-
-
0.0039
mizoribine monophosphate
-
type 2 isozyme
0.0082
mizoribine monophosphate
-
type 1 isozyme
0.0115
mizoribine monophosphate
-
-
0.0000002
Mycophenolic acid
-
-
0.0000011
Mycophenolic acid
pH 8.0, 25°C, recombinant wild-type enzyme
0.000002
Mycophenolic acid
-
for the competitive component
0.0000044
Mycophenolic acid
pH 8.0, 25°C, recombinant mutant A251T
0.000007
Mycophenolic acid
against type II isoform
0.000007
Mycophenolic acid
isoform IMPDH2, at pH 8.0 and 25°C
0.000008
Mycophenolic acid
-
for the non-competitive component
0.000009
Mycophenolic acid
-
-
0.00001
Mycophenolic acid
-
isoform IMPDH2, pH 8.0, 25°C
0.00002
Mycophenolic acid
-
-
0.00002
Mycophenolic acid
against IMPDH in general
0.000025
Mycophenolic acid
-
pH 7.5, 25°C
0.00003
Mycophenolic acid
pH 8.0, 37°C, recombinant enzyme
0.0000321
Mycophenolic acid
pH 8.0, 28°C, recombinant enzyme
0.000033
Mycophenolic acid
type I isoform
0.00004
Mycophenolic acid
-
isoform IMPDH1, pH 8.0, 25°C
0.0000508
Mycophenolic acid
-
in the presence of NAD+
0.0000577
Mycophenolic acid
-
in the presence of inosine 5'-phosphate
0.000071
Mycophenolic acid
-
at a fixed concentration of 0.5 mM NAD+ and 0.03 mM IMP
0.000178
Mycophenolic acid
-
at a fixed concentration of 0.5 mM NAD+
0.00069
Mycophenolic acid
-
-
0.00069
Mycophenolic acid
-
at a fixed concentration of 0.03 mM IMP
0.0011
Mycophenolic acid
-
type 1 isozyme
0.0039
Mycophenolic acid
Q81W29
substrate NAD+, pH 8.0, 22°C
0.0048
Mycophenolic acid
Q81W29
substrate inosine monophosphate, pH 8.0, 22°C
0.006
Mycophenolic acid
-
type 2 isozyme
0.0093
Mycophenolic acid
-
at pH 8.0 and 25°C
0.01
Mycophenolic acid
isoform IMPDH2, pH 8.0, 25°C
0.011
Mycophenolic acid
-
wild-type, 37°C, pH 8.0
0.0182
Mycophenolic acid
-
mutant L263F, 37°C, pH 8.0
0.021
Mycophenolic acid
pH 8.0, 25°C
0.021
Mycophenolic acid
pH 8.0, 25°C
0.04
Mycophenolic acid
isoform IMPDH1, pH 8.0, 25°C
0.000382
mycophenolic acid-acyl-glucuronide
-
in the presence of NAD+
0.000511
mycophenolic acid-acyl-glucuronide
-
in the presence of inosine 5'-phosphate
0.00003
mycophenolic hydroxamic acid
-
isoform IMPDH2, pH 8.0, 25°C
0.00007
mycophenolic hydroxamic acid
-
isoform IMPDH1, pH 8.0, 25°C
0.0008
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
at pH 8.0 and 25°C
0.0028
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
at pH 8.0 and 25°C
0.00029
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
at pH 8.0 and 25°C
0.00045
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
-
at pH 8.0 and 25°C
0.0017
N-hydroxy-N'-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]octanediamide
-
isoform IMPDH2, pH 8.0, 25°C
0.005
N-hydroxy-N'-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]octanediamide
-
isoform IMPDH1, pH 8.0, 25°C
0.000066
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
at pH 8.0 and 25°C
0.00046
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
at pH 8.0 and 25°C
0.00057
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
at pH 8.0 and 25°C
0.0014
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
at pH 8.0 and 25°C
0.000014
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
pH 8.0, 22°C
0.000014
N2-(2,3-dichlorophenyl)-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]-L-alaninamide
pH and temperature not specified in the publication
0.6
NAD+
absence of K+, pH 8.0, 25°C
1
NAD+
pH 8.0, 37°C, recombinant mutant R224P
1.5
NAD+
presence of 1 mM K+, pH 8.0, 25°C
2
NAD+
pH 8.0, 37°C, recombinant wild-type enzyme
2.9
NAD+
-
pH 8.0, 25°C, recombinant alphabeta core domain, in presence of 100 mM KCl
3.6
NAD+
recombinant wild-type enzyme, pH 8.0, 28°C
3.8
NAD+
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
3.9
NAD+
Q81W29
pH 8.0, 22°C
3.9
NAD+
-
pH 8.0, 25°C, recombinant wild-type enzyme
4
NAD+
pH 8.0, 37°C, recombinant mutants D226N and V268I
4.5
NAD+
recombinant AgIMPDH-DELTABateman mutant enzyme, pH 8.0, 28°C
4.9
NAD+
presence of 100 mM K+, pH 8.0, 25°C
5
NAD+
recombinant wild-type enzyme, pH 8.0, 22°C
5.3
NAD+
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
6.3
NAD+
recombinant enzyme, pH 8.5, 37°C
6.4
NAD+
-
pH 8.0, 25°C, recombinant wild-type enzyme
6.8
NAD+
-
pH 8.0, 25°C, recombinant full-length enzyme, in presence of 100 mM KCl
9
NAD+
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant ClpIMPDHDELTAL
13
NAD+
-
pH 8.0, 25°C, recombinant wild-type enzyme
13
NAD+
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
13
NAD+
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant VcIMPDHDELTAL
16
NAD+
recombinant MtbIMPDH2DELTACBS mutant enzyme, pH 8.0, 22°C
0.094
NADH
-
-
0.21
NADH
-
versus inosine 5'-phosphate
0.23
NADH
-
versus inosine 5'-phosphate
0.000013
oxanosine monophosphate
at pH 8.0 and 25°C
0.000017
oxanosine monophosphate
-
at pH 8.0 and 25°C
0.000051
oxanosine monophosphate
at pH 8.0 and 25°C
0.00009
oxanosine monophosphate
-
at pH 8.0 and 25°C
0.00034
oxanosine monophosphate
at pH 8.0 and 25°C
0.000095
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
type 1 isozyme
0.00014
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
type 2 isozyme
0.0015
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
0.0016
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
0.0023
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
0.0085
P1-(thiazofurin-5'-yl)-P2-(adenosyl-5'-yl)-alpha,beta-methylene diphosphate
-
-
0.000007
P1-(tiazofurin-5'-yl)-P2-(2-aminoadenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.000027
P1-(tiazofurin-5'-yl)-P2-(2-aminoadenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.000001
P1-(tiazofurin-5'-yl)-P2-(2-ethyladenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.000014
P1-(tiazofurin-5'-yl)-P2-(2-ethyladenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.00001
P1-(tiazofurin-5'-yl)-P2-(2-ethynyladenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.000049
P1-(tiazofurin-5'-yl)-P2-(2-ethynyladenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.000019
P1-(tiazofurin-5'-yl)-P2-(2-iodoadenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.000084
P1-(tiazofurin-5'-yl)-P2-(2-iodoadenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.00002
P1-(tiazofurin-5'-yl)-P2-(2-phenyladenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.000143
P1-(tiazofurin-5'-yl)-P2-(2-phenyladenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.00011
P1-(tiazofurin-5'-yl)-P2-(adenosin-5'-yl) diphosphate
-
isoform IMPDH1, pH 8.0, 25°C
0.00011
P1-(tiazofurin-5'-yl)-P2-(adenosin-5'-yl) diphosphate
-
isoform IMPDH2, pH 8.0, 25°C
0.02
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH1, pH 8.0, 25°C
0.04
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
-
isoform IMPDH2, pH 8.0, 25°C
0.04
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-ethyladenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH2, pH 8.0, 25°C
0.07
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-phenyladenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH1, pH 8.0, 25°C
0.11
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(2-phenyladenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH2, pH 8.0, 25°C
0.25
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(adenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH2, pH 8.0, 25°C
0.33
P1-[7-hydroxy-6-(hydroxyethyl)-5-methoxy-4-methylphthtalan-1-one-2-yl]-P2-(adenosin-5'-yl)methylenebis(phosphonate)
isoform IMPDH1, pH 8.0, 25°C
0.00025
ribavirin 5'-monophosphate
-
-
0.00058
ribavirin 5'-monophosphate
-
-
0.0008
ribavirin 5'-monophosphate
-
-
0.0032
ribavirin 5'-monophosphate
pH 8.0, 25°C
0.000065
ribavirin monophosphate
-
-
0.00039
ribavirin monophosphate
-
type 2 isozyme
0.00065
ribavirin monophosphate
-
type 1 isozyme
0.006
ribavirin monophosphate
-
-
0.006
ribavirin monophosphate
-
-
0.00002
Selenazofurin
with inosine 5'-phosphate as substrate
0.00003
Selenazofurin
with inosine 5'-phosphate as substrate
0.00058
SFAD
with inosine 5'-phosphate as substrate
0.0011
SFAD
with inosine 5'-phosphate as substrate
0.00043
TFAD
with inosine 5'-phosphate as substrate
0.0007
TFAD
with inosine 5'-phosphate as substrate
0.000058
thiazole-4-carboxamide adenine dinucleotide
-
pH 7.4, 37°C
0.000075
thiazole-4-carboxamide adenine dinucleotide
-
-
0.000123
thiazole-4-carboxamide adenine dinucleotide
-
chemically synthesized thiazole-4-carboxamide adenine dinucleotide
0.00019
thiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH I
0.000226
thiazole-4-carboxamide adenine dinucleotide
-
enzymatically synthesized thiazole-4-carboxamide adenine dinucleotide
0.00024
thiazole-4-carboxamide adenine dinucleotide
-
isozyme IMPDH II
0.00029
thiazole-4-carboxamide adenine dinucleotide
-
versus inosine 5'-phosphate
0.00031
thiazole-4-carboxamide adenine dinucleotide
-
versus inosine 5'-phosphate
0.000345
thiazole-4-carboxamide adenine dinucleotide
-
ex vivo thiazole-4-carboxamide adenine dinucleotide
0.00058
thiazole-4-carboxamide adenine dinucleotide
-
-
0.00073
thiazole-4-carboxamide adenine dinucleotide
-
versus NAD+
0.00074
thiazole-4-carboxamide adenine dinucleotide
-
versus NAD+
0.0013
thiazole-4-carboxamide adenine dinucleotide
-
-
0.00043
tiazofurin
with inosine 5'-phosphate as substrate
0.0007
tiazofurin
with inosine 5'-phosphate as substrate
26
tiazofurin
pH 8.0, 25°C, recombinant wild-type enzyme
40
tiazofurin
pH 8.0, 25°C, recombinant mutant A251T
69
tiazofurin
-
wild-type, pH 8.0, 25°C
90
tiazofurin
-
mutant Q324A, pH 8.0, 25°C
91
tiazofurin
-
mutant R322A, pH 8.0, 25°C
200
tiazofurin
-
mutant R322E, pH 8.0, 25°C
300
tiazofurin
-
mutant E323A, pH 8.0, 25°C
0.000006
VX-148
-
0.000007
VX-497
type I isoform
0.00001
VX-497
against type II isoform
0.03
xanthosine 5'-phosphate
-
-
0.085
xanthosine 5'-phosphate
-
-
0.085
xanthosine 5'-phosphate
-
-
0.109
xanthosine 5'-phosphate
-
-
0.118
xanthosine 5'-phosphate
-
versus inosine 5'-phosphate
0.136
xanthosine 5'-phosphate
-
-
0.136
xanthosine 5'-phosphate
-
versus inosine 5'-phosphate
0.218
xanthosine 5'-phosphate
Q81W29
pH 8.0, 22°C
0.28
xanthosine 5'-phosphate
-
versus NAD+
0.32
xanthosine 5'-phosphate
-
versus NAD+
0.026
XMP
-
pH 7.5, 25°C
0.2083
XMP
pH 8.0, 28°C, recombinant enzyme
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
various inhibitors
-
additional information
additional information
-
Ki over the range of pH 7.3 to 8.5
-
additional information
additional information
-
inhibition by purine nucleotides
-
additional information
additional information
-
wild type and mutants
-
additional information
additional information
-
wild type and mutants
-
additional information
additional information
-
wild type and mutants
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
inhibition kinetics, structure-inhibitory potency relationship, overview
-
additional information
additional information
-
inhibition kinetics, structure-inhibitory potency relationship, overview
-
additional information
additional information
-
inhibition patterns, isozymes I and II
-
additional information
additional information
-
multi-inhibitor kinetics
-
additional information
additional information
-
mycophenolic acid inhibition kinetics
-
additional information
additional information
inhibition kinetic analysis, detailed overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0001
(1H-naphtho[2,3-d]imidazol-2-yl)methyl 4-aminobenzoate
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.000785
(2-[acetyl[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 785 nM
0.000749
(2-[formyl[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 749 nM
0.001
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: above 0.001 mM
0.000498
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methylsulfonyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 498 nM
0.000093
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](sulfamoyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 93 nM
0.000499
(2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 499 nM
0.000132
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 132 nM
0.000068
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](methylsulfonyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 68 nM
0.000024
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl](sulfamoyl)amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 24 nM
0.000013
(2-[[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 13 nM
0.000028
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
0.002
(2E)-3-furan-2-yl-N-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]prop-2-enamide
Homo sapiens
-
isozyme IMPDH II IC50: 0.002 mM
0.000014
(2S)-2-[(1-naphthyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Cryptosporidium parvum
pH 8.0, 25°C
0.0000005
(2S)-2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Cryptosporidium parvum
pH 8.0, 25°C
0.00015 - 0.00017
(4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
0.00082
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2R)-2-phenylpropyl]hex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.0005
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(2-methylphenyl)ethyl]hex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.0006
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(4-methylphenyl)ethyl]hex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.00033
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-[2-(4-methoxyphenyl)ethyl]-4-methylhex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.0041
(4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoic acid
Homo sapiens
pH 7.4, 37°C
0.00035 - 0.00042
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00048
(4E)-N-[(4-butylphenyl)methyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.00073
(4E)-N-[2-(2-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.00051
(4E)-N-[2-(2H-1,3-benzodioxol-5-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.00057
(4E)-N-[2-(4-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
isoform IMPDH2, at pH 8.6 and 37°C
0.000246
([[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]oxy]methyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 246 nM
0.000023
([[(2E)-4-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]oxy]methyl)phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 23 nM
0.0019
1,4-dimethyl-6-nitro-2H-cyclopenta[d]pyridazine
Homo sapiens
-
0.094
1-(2,2-dimethylpropanoyl)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1'H-spiro[pyrrolidine-3,2'-quinazolin]-4'(3'H)-one
Homo sapiens
-
IC50: 0.094 mM, isozyme IMPDH II
0.0000009
1-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)-3-quinolin-7-ylurea
Cryptosporidium parvum
pH 8.0, 25°C
0.00064
1-(3-methylphenyl)-3-[4-(1,3-oxazol-5-yl)phenyl]urea
Homo sapiens
-
isozyme IMPDH II IC50: 640 nM
0.00000066
1-(4-chloro-5-nitrocyclohexa-1,5-dien-1-yl)-3-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
Cryptosporidium parvum
pH 8.0, 25°C
0.000076
1-(benzyloxy)-3-(3-pyridin-4-yl-1H-indol-6-yl)urea
Homo sapiens
-
0.000033
1-methyl-6-[(5-phenyl-1,3-oxazol-2-yl)amino]-1H-indole-3-carbonitrile
Homo sapiens
-
0.000035
1-tert-butyl 5-methyl (3R,5R)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
Homo sapiens
-
IC50: 35 nM, isozyme IMPDH II
0.000948
1-tert-butyl 5-methyl (3R,5S)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
Homo sapiens
-
IC50: 948 nM, isozyme IMPDH II
0.000035
1-tert-butyl 5-methyl (3S,5R)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1,5-dicarboxylate
Homo sapiens
-
IC50: 35 nM, isozyme IMPDH II
0.00127
1-[(3,4-dichlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
Helicobacter pylori
-
at pH 7.6 and 37°C
0.0021
1-[(3-chlorophenyl)methyl]-4-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazole
Helicobacter pylori
-
at pH 7.6 and 37°C
0.0000008
1-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]-3-quinolin-7-ylurea
Cryptosporidium parvum
pH 8.0, 25°C
0.000043
1-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
Homo sapiens
-
isozyme IMPDH II IC50: 43 nM
0.000019
1-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
Homo sapiens
-
isozyme IMPDH II IC50: 19 nM
0.0005
1-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-3-(3-methylphenyl)urea
Homo sapiens
-
isozyme IMPDH II IC50: 500 nM
0.00002
14,16-dihydroxy-3,8-dimethyl-3,4,5,6,9,10-hexahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione
Homo sapiens
pH 8.0, 25°C
0.00022 - 0.00055
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
0.0016
2-(1,3-oxazol-5-yl)-5-[(5-phenyl-1,3-oxazol-2-yl)amino]phenol
Homo sapiens
-
isozyme IMPDH II IC50: 0.0016 mM
0.00003
2-(1-benzothiophen-3-yl)-6-methoxy-5-(1,3-oxazol-5-yl)-1H-indole-3-carbaldehyde
Homo sapiens
-
0.000013 - 0.000095
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
0.0062
2-(4-benzoylphenyl)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)propanamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.00304
2-(4-fluoronaphthalen-1-yl)-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0002
2-(dimethylamino)-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 200 nM
0.00018
2-benzyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 180 nM
0.00001 - 0.000092
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
0.00024
2-cyano-1-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-3-phenylguanidine
Homo sapiens
-
isozyme IMPDH II IC50: 240 nM
0.000073 - 0.000099
2-ethyl-9-[5-O-[hydroxy(2-[hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]ethyl)phosphoryl]-beta-L-ribofuranosyl]-9H-purin-6-amine
0.000032
2-furan-3-yl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 32 nM
0.000041
2-hydroxy-N-[2-(2-[[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methylacetamide
Homo sapiens
-
isozyme IMPDH II IC50: 41 nM
0.000343
2-methyl-3-(pyrid-4-yl)indole
Homo sapiens
-
IC50: 343 nM
0.01
2-tert-butyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 0.01 mM
0.000002
2-[(3,4-dichlorophenyl)amino]-N-[2-(pyridin-4-yl)-1,3-benzoxazol-5-yl]propanamide
Cryptosporidium parvum
pH 8.0, 25°C
0.0008 - 0.013
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
0.00406
2-[4-([1-[(3-methoxyphenyl)methyl]-1H-1,2,3-triazol-4-yl]methoxy)phenyl]-5-methyl-1,3,4-oxadiazole
Helicobacter pylori
-
at pH 7.6 and 37°C
0.000007
2-[methyl[2-(2-[[3-(1,3-oxazol-5-yl)-1H-indol-6-yl]amino]-1,3-oxazol-5-yl)phenyl]amino]-2-oxoethyl acetate
Homo sapiens
-
0.00188
2-[[2-(4-methoxyphenyl)-4-oxo-4H-1-benzopyran-3-yl]oxy]-N-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
Helicobacter pylori
-
at pH 7.6 and 37°C
0.07
2264A
Homo sapiens
-
0.000169 - 0.0034
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
0.00086 - 0.0012
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
0.0183
3-(4-chlorophenyl)-4-(4-ethoxyphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.000033 - 0.00042
3-cyanoindole-based inhibitors
Homo sapiens
-
synthesis and initial structureactivity relationships of 3-cyanoindole-based inhibitors with isozyme IMPDH II, IC50: 33-420 nM, comparison to other inhibitor structural classes, overview
-
0.0001
3-hydroxy-N-methyl-N-[2-(2-[[3-methyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]propanamide
Homo sapiens
-
isozyme IMPDH II IC50: 100 nM
0.000021
3-hydroxy-N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 21 nM
0.000005 - 0.00016
3-phenyl quinolone derivatives
Homo sapiens
-
several, isozyme IMPDH II IC50: 5-160 nM, overview
-
0.0117
4-(3-bromo-4-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.019
4-(4-acetamidophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.023
4-(4-acetamidophenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.0074
4-(5-bromo-2-fluorophenyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.0117
4-(5-bromo-2-methoxyphenyl)-3-(4-methylphenyl)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.017
4-acetyl-N-(3-chloro-4-fluorophenyl)-3,4-dihydro-2H-1,4-benzoxazine-7-sulfonamide
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.00115
4-pyridylindole
Homo sapiens
-
IC50: 0.00115 mM
0.000057 - 0.00012
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
0.000043 - 0.000364
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
0.1747
4-[(5-[[(naphthalen-1-yl)oxy]methyl]-1H-1,2,3-triazol-1-yl)methyl]benzonitrile
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000018
4-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-6-phenyl-1,3,5-triazin-2-ol
Homo sapiens
-
0.000004
5-([[2-([1,1'-biphenyl]-3-yl)propan-2-yl]carbamoyl]amino)-2-chlorobenzamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.0005
5-bromoisoquinolin-6-amine
Homo sapiens
-
0.00076
5-chloro-1,4-dimethyl-2H-cyclopenta[d]pyridazine-6-carbonitrile
Homo sapiens
-
0.000328
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1'H-spiro[cyclopentane-1,2'-quinazolin]-4'(3'H)-one
Homo sapiens
-
IC50: 328 nM, isozyme IMPDH II
0.068
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-1-(piperidin-1-ylcarbonyl)-1'H-spiro[pyrrolidine-3,2'-quinazolin]-4'(3'H)-one
Homo sapiens
-
IC50: 0.068 mM, isozyme IMPDH II
0.000526
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-2,3,5,6-tetrahydro-1'H-spiro[pyran-4,2'-quinazolin]-4'(3'H)-one
Homo sapiens
-
IC50: 526 nM, isozyme IMPDH II
0.393
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-N-phenyl-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.393 mM, isozyme IMPDH II
0.000096
7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4,6-dihydro-1'H-spiro[cyclopenta[b]thiophene-5,2'-quinazolin]-4'(3'H)-one
Homo sapiens
-
IC50: 96 nM, isozyme IMPDH II
0.071
7'-methoxy-3'-methyl-N,N-bis(1-methylethyl)-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.071 mM, isozyme IMPDH II
0.064
7'-methoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-N-phenyl-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.064 mM, isozyme IMPDH II
0.004
7-amino-5-(4-chlorophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.007
7-amino-5-(4-nitrophenyl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.004
7-amino-5-(5-nitrothiophen-2-yl)-2,4-dioxo-1,3,4,5-tetrahydro-2H-pyrano[2,3-d]pyrimidine-6-carbonitrile
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.000254
7-hydroxy-5-methoxy-4-methyl-6-(3-methylbut-2-en-1-yl)-2-benzofuran-1(3H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 254 nM
0.000273
7-hydroxy-5-methoxy-6-[(2E)-4-methoxy-3-methylbut-2-en-1-yl]-4-methyl-2-benzofuran-1(3H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 273 nM
0.000192
7-methoxy-2,2,3-trimethyl-6-(1,3-oxazol-5-yl)-2,3-dihydroquinazolin-4(1H)-one
Homo sapiens
-
IC50: 192 nM, isozyme IMPDH II
0.0003
7-methoxy-2,2-dimethyl-6-(1,3-oxazol-5-yl)-3-(2-pyridin-4-ylethyl)-2,3-dihydroquinazolin-4(1H)-one
Homo sapiens
-
IC50: 300 nM, isozyme IMPDH II
0.000049
7-methoxy-2,3-dimethyl-6-(1,3-oxazol-5-yl)-2-[(E)-2-phenylethenyl]-2,3-dihydroquinazolin-4(1H)-one
Homo sapiens
-
IC50: 49 nM, isozyme IMPDH II
0.000005
7-methoxy-2-(3-methylphenyl)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
0.00022
7-methoxy-2-(methylamino)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 220 nM
0.00011
7-methoxy-2-methyl-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 110 nM
0.000065
7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 65 nM
0.000104
7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)quinazoline-2,4(1H,3H)-dione
Homo sapiens
-
IC50: 104 nM, isozyme IMPDH II
0.00021
7-methoxy-6-(1,3-oxazol-4-yl)-2-phenylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 210 nM
0.000034
7-methoxy-6-(1,3-oxazol-5-yl)-2-(1,3-thiazol-4-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 34 nM
0.000008
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenoxyquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 8 nM
0.000008
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 8 nM
0.000043
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-2-ylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 43 nM
0.00007
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-3-ylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 70 nM
0.000046
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-4-ylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 46 nM
0.000063
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-2-ylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 63 nM
0.000009
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-3-ylquinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 9 nM
0.000303
7-methoxy-6-(1,3-oxazol-5-yl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one
Homo sapiens
-
IC50: 303 nM
0.000013
7-methoxy-6-(1,3-oxazol-5-yl)-3-(2-pyridin-4-ylethyl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one
Homo sapiens
-
0.0003
7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one
Homo sapiens
-
isozyme IMPDH II IC50: 300 nM
0.000037
9-(5-O-[hydroxy[([hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]oxy)methyl]phosphoryl]-beta-L-ribofuranosyl)-9H-purin-6-amine
Homo sapiens
pH 8.0, 25°C
0.000016 - 0.0082
BMS-337197
0.001
dimethyl (2-[[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]amino]ethyl)phosphonate
Homo sapiens
-
isozyme IMPDH II IC50: above 0.001 mM
0.000289
dimethyl [(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphonate
Homo sapiens
-
isozyme IMPDH II IC50: 289 nM
0.0161
eicosadienoic acid
Mus musculus
-
pH 8.0, 37°C
0.08
ethyl 7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxylate
Homo sapiens
-
IC50: 0.08 mM, isozyme IMPDH II
0.00073
ethyl 9-oxo-9,10-dihydroacridine-1-carboxylate
Homo sapiens
-
0.0014 - 0.0015
methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
0.0009 - 0.015
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
0.000005 - 0.000024
mycophenolic 2-ethyladenosin-5'-yl-difluoromethylenebis(phosphonate)
0.000016 - 0.000038
mycophenolic 2-ethyladenosin-5'-yl-methylenebis(phosphonate)
0.000007 - 0.0272
Mycophenolic acid
0.079
N,7'-dimethoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.079 mM, isozyme IMPDH II
0.045
N,N-diethyl-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.045 mM, isozyme IMPDH II
0.000018
N-(2,3-dichlorophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
Cryptosporidium parvum
pH not specified in the publication, temperature not specified in the publication
0.051
N-(2,4-difluorophenyl)-7'-methoxy-N,3'-dimethyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.051 mM, isozyme IMPDH II
0.000028
N-(4-bromophenyl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
Cryptosporidium parvum
pH not specified in the publication, temperature not specified in the publication
0.000015 - 0.000067
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
0.000006 - 0.000066
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
0.0033
N-(4-chlorophenyl)-2-phenoxypropanamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.0017 - 0.049
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
0.0016
N-(4-methoxyphenyl)-2-(naphthalen-1-yl)acetamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.0006 - 0.07
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
0.000005
N-(5-phenyl-1,3-oxazol-2-yl)isoquinolin-6-amine
Homo sapiens
-
0.000008
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-2-yl)-1H-benzimidazol-1-yl]acetamide
Cryptosporidium parvum
pH not specified in the publication, temperature not specified in the publication
0.000007
N-(naphthalen-2-yl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Cryptosporidium parvum
pH not specified in the publication, temperature not specified in the publication
0.000042 - 0.00057
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
0.0000011 - 0.0000054
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
0.119
N-ethyl-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxamide
Homo sapiens
-
IC50: 0.119 mM, isozyme IMPDH II
0.005
N-methyl-N'-[4-(1,3-oxazol-5-yl)phenyl]-6-phenyl-1,3,5-triazine-2,4-diamine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.005
N-methyl-N'-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-6-phenyl-1,3,5-triazine-2,4-diamine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.000045
N-methyl-N-[2-(2-[[3-methyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-morpholin-4-ylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 45 nM
0.0000021
N-naphthalen-2-yl-N'-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]urea
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.000055
N-tert-butyl-N'-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]ethanediamide
Homo sapiens
-
isozyme IMPDH II IC50: 55 nM
0.00001
N-tert-butyl-N'-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]ethanediamide
Homo sapiens
-
isozyme IMPDH II IC50: 10 nM
0.005
N-tert-butyl-N'-[4-(1,3-oxazol-5-yl)phenyl]ethanediamide
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.005
N-tert-butyl-N'-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]ethanediamide
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.000017
N-[1-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]-1-methylethyl]-2-fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide
Homo sapiens
-
0.000047
N-[2-(2-[[3-(chloromethyl)-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 47 nM
0.000028
N-[2-(2-[[3-bromo-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 28 nM
0.000021
N-[2-(2-[[3-bromo-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 21 nM
0.000048
N-[2-(2-[[3-chloro-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 48 nM
0.00031
N-[2-(2-[[3-ethyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-3-hydroxy-N-methylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 310 nM
0.000021
N-[2-(2-[[3-ethyl-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 21 nM
0.000091
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-2-morpholin-4-ylacetamide
Homo sapiens
-
isozyme IMPDH II IC50: 91 nM
0.000012
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-2-morpholin-4-ylacetamide
Homo sapiens
-
0.000016
N-[2-(2-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]amino]-1,3-oxazol-5-yl)phenyl]-N-methyl-3-morpholin-4-ylpropanamide
Homo sapiens
-
isozyme IMPDH II IC50: 16 nM
0.000018
N-[2-(hydroxymethyl)cyclopentyl]-N'-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]propanediamide
Homo sapiens
-
0.005
N-[2-chloro-3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.0016
N-[2-chloro-5-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.0016 mM
0.005
N-[2-fluoro-5-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.00005
N-[3-bromo-4-(1,3-oxazol-5-yl)phenyl]-N'-tert-butylethanediamide
Homo sapiens
-
isozyme IMPDH II IC50: 50 nM
0.005
N-[3-chloro-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.000088
N-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 88 nM
0.00034
N-[3-chloro-4-(1,3-oxazol-5-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
Homo sapiens
-
isozyme IMPDH II IC50: 340 nM
0.01
N-[3-ethoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.010 mM
0.00019
N-[3-methoxy-4-(1,3-oxazol-2-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 190 nM
0.000057
N-[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 57 nM
0.0016
N-[3-methoxy-4-(1,3-oxazol-4-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
Homo sapiens
-
isozyme IMPDH II IC50: 0.0016 mM
0.00002
N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 20 nM
0.000076
N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]-N'-methyl-6-phenyl-1,3,5-triazine-2,4-diamine
Homo sapiens
-
isozyme IMPDH II IC50: 76 nM
0.00041
N-[3-methoxy-4-(1H-1,2,4-triazol-1-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 410 nM
0.002
N-[3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.002 mM
0.005
N-[3-methoxy-4-(4-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.005
N-[3-methyl-4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.005
N-[4-(1,3-oxazol-4-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.005
N-[4-(1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.0028
N-[4-(1-benzyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl]acetamide
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.002
N-[4-(2,4-dimethyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.002 mM
0.005
N-[4-(4-methyl-1,3-oxazol-5-yl)phenyl]-5-phenyl-1,3-oxazol-2-amine
Homo sapiens
-
isozyme IMPDH II IC50: 0.005 mM
0.001
pellynic acid
Homo sapiens
-
0.000016
phenyl N'-cyano-N-(3-[cyano[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamimidamido]benzyl)imidocarbamate
Homo sapiens
-
0.000104
tert-butyl 7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1H,1'H-spiro[pyrrolidine-3,2'-quinazoline]-1-carboxylate
Homo sapiens
-
IC50: 104 nM, isozyme IMPDH II
0.000035
tert-butyl methyl (1S,4S)-7'-methoxy-3'-methyl-6'-(1,3-oxazol-5-yl)-4'-oxo-3',4'-dihydro-1'H-spiro[cyclopentane-1,2'-quinazoline]-3,4-dicarboxylate
Homo sapiens
-
0.0016
tetrasodium 6,6'-[(3,3'-dimethoxy[1,1'-biphenyl]-4,4'-diyl)bis[(E)-diazene-2,1-diyl]]bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate)
Pseudomonas aeruginosa
pH and temperature not specified in the publication
0.000013 - 0.00003
thiazofurin-5'-yl-2-ethyladenosin-5'-yl-difluromethylene bis(phosphonate)
0.000001 - 0.000014
thiazole-4-carboxamide 2-ethyladenine dinucleotide
0.00011
thiazole-4-carboxamide adenine dinucleotide
Homo sapiens
pH 8.0, 25°C
0.000006
VX-148
Homo sapiens
-
isozyme IMPDH II IC50: 6 nM
0.000011
VX-497
Homo sapiens
-
isozyme IMPDH II IC50: 11 nM
0.000506
[(1E,3E)-5-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpenta-1,3-dien-1-yl]phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 506 nM
0.000168
[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 168 nM
0.001
[(2E)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-2-methylbut-2-en-1-yl]phosphoramidic acid
Homo sapiens
-
isozyme IMPDH II IC50: above 0.001 mM
0.000096
[(3E)-5-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpent-3-en-1-yl]phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 96 nM
0.00002
[(3E)-5-(6-ethyl-4-hydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-3-methylpent-3-en-1-yl]phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 20 nM
0.000086
[(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-en-1-yl]phosphonic acid
Homo sapiens
-
isozyme IMPDH II IC50: 86 nM
additional information
additional information
Vibrio cholerae serotype O1
-
the inhibitors all exhibit inhibitory potencies with IC50 values of over 0.005 mM with wild-type and truncation mutant
-
0.000028
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
Homo sapiens
-
0.000028
(2E)-3-furan-2-yl-N-[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]prop-2-enamide
Homo sapiens
-
isozyme IMPDH II IC50: 28 nM
0.00015
(4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
Homo sapiens
pH 7.4, 37°C
0.00017
(4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
Homo sapiens
pH 7.4, 37°C
0.00035
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
pH 7.4, 37°C
0.00042
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
Homo sapiens
pH 7.4, 37°C
0.00022
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0003
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
Helicobacter pylori
-
pH 8.0, 25°C
0.0004
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.00055
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
Streptococcus pyogenes
-
pH 8.0, 25°C
0.000013
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000019
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.000023
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000027
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.000038
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.000054
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000095
2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.00001
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.000022
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000034
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000039
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.00004
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.000047
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000092
2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.000073
2-ethyl-9-[5-O-[hydroxy(2-[hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]ethyl)phosphoryl]-beta-L-ribofuranosyl]-9H-purin-6-amine
Homo sapiens
pH 8.0, 25°C
0.000099
2-ethyl-9-[5-O-[hydroxy(2-[hydroxy[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)ethoxy]phosphoryl]ethyl)phosphoryl]-beta-L-ribofuranosyl]-9H-purin-6-amine
Homo sapiens
pH 8.0, 25°C
0.0008
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0011
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
Helicobacter pylori
-
pH 8.0, 25°C
0.0011
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.0014
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.013
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
Streptococcus pyogenes
-
pH 8.0, 25°C
0.000169
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.0002
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant3 CjIMPDHDELTAS
0.00067
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.0007
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.0008
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant3 BaIMPDHDELTAS
0.0017
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.0034
3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.00086
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
Streptococcus pyogenes
-
pH 8.0, 25°C
0.0009
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0009
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.001
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.0012
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
Helicobacter pylori
-
pH 8.0, 25°C
0.000057
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
Bacillus anthracis
Q81W29
pH 8.0, 22°C
0.00012
4-[(1R)-1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl]ethoxy]quinoline 1-oxide
Campylobacter jejuni
-
pH 8.0, 22°C
0.000043
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.000063
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000074
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000107
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.000137
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.00014
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000364
4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.000016
BMS-337197
Homo sapiens
-
isozyme IMPDH II IC50: 16 nM
0.0082
BMS-337197
Homo sapiens
-
IC50: 0.0082 mM
0.0014
methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
Homo sapiens
pH 7.4, 37°C
0.0015
methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
Homo sapiens
pH 7.4, 37°C
0.0009
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0015
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
Helicobacter pylori
-
pH 8.0, 25°C
0.0016
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.0018
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.015
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
Streptococcus pyogenes
-
pH 8.0, 25°C
0.000005
mycophenolic 2-ethyladenosin-5'-yl-difluoromethylenebis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.000024
mycophenolic 2-ethyladenosin-5'-yl-difluoromethylenebis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.000016
mycophenolic 2-ethyladenosin-5'-yl-methylenebis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.000038
mycophenolic 2-ethyladenosin-5'-yl-methylenebis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.000007
Mycophenolic acid
Homo sapiens
pH 8.0, 25°C
0.000011
Mycophenolic acid
Homo sapiens
-
isozyme IMPDH II IC50: 11 nM, potent, uncompetitive inhibition, immunosuppressive drug, prodrug is mycophenolate mofetil
0.000012
Mycophenolic acid
Homo sapiens
pH 7.4, 37°C
0.000014
Mycophenolic acid
Homo sapiens
-
potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil, isozyme IMPDH II IC50: 14 nM
0.000015
Mycophenolic acid
Homo sapiens
-
isozyme IMPDH II IC50: 15 nM
0.000019
Mycophenolic acid
Homo sapiens
pH 7.4, 37°C
0.000033
Mycophenolic acid
Homo sapiens
pH 8.0, 25°C
0.0000992
Mycophenolic acid
Homo sapiens
-
IC50: 99.2 nM with umbilical vein endothelial cells, 128 nM with Jurkat cells, inhibits the enzyme in vivo and in vitro, mycophenolic acid inhibits tumor-associated angiogenesis and is used as clinical drug in immunosuppression
0.000128
Mycophenolic acid
Homo sapiens
-
IC50: 99.2 nM with umbilical vein endothelial cells, 128 nM with Jurkat cells, inhibits the enzyme in vivo and in vitro, mycophenolic acid inhibits tumor-associated angiogenesis and is used as clinical drug in immunosuppression
0.0272
Mycophenolic acid
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000015
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000019
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000036
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000044
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.000065
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.000067
N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.000006
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.00002
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000024
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000028
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.000029
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000046
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.000066
N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.0017
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0023
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.003
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
Helicobacter pylori
-
pH 8.0, 25°C
0.0054
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.049
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
Streptococcus pyogenes
-
pH 8.0, 25°C
0.0006
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Helicobacter pylori
-
pH 8.0, 25°C
0.0006
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Borreliella burgdorferi
-
pH 8.0, 25°C
0.0006
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.0012
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Cryptosporidium parvum
-
pH and temperature not specified in the publication
0.07
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
Streptococcus pyogenes
-
pH 8.0, 25°C
0.000042
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS
0.000051
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Campylobacter jejuni
-
pH 8.0, 22°C
0.000051
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Campylobacter jejuni
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000057
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Bacillus anthracis
Q81W29
pH 8.0, 22°C
0.000067
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.000072
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL
0.0001
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Bacillus anthracis
-
pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS
0.00045
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL
0.00057
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
Clostridium perfringens
-
pH 8.0, 25°C, recombinant wild-type enzyme
0.0000011
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
Helicobacter pylori
-
pH 8.0, 25°C
0.0000019
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
Escherichia coli
-
mutant S250A/L444Y, pH 8.0, 25°C
0.0000054
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
Streptococcus pyogenes
-
pH 8.0, 25°C
0.000013
thiazofurin-5'-yl-2-ethyladenosin-5'-yl-difluromethylene bis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.00003
thiazofurin-5'-yl-2-ethyladenosin-5'-yl-difluromethylene bis(phosphonate)
Homo sapiens
pH 8.0, 25°C
0.000001
thiazole-4-carboxamide 2-ethyladenine dinucleotide
Homo sapiens
pH 8.0, 25°C
0.000014
thiazole-4-carboxamide 2-ethyladenine dinucleotide
Homo sapiens
pH 8.0, 25°C
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