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((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide
-
-
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide
0.2 mM, 82.04% inhibition
-
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 9.89% inhibition
-
(2E)-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 11.75% inhibition
-
(2E)-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide
0.2 mM, 69.3% inhibition
-
(2E)-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide
0.2 mM, 1.17% inhibition; 0.2 mM, 1.35% inhibition; 0.2 mM, 6.68% inhibition
-
(2E)-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[[4-(trifluoromethyl)phenyl]methylidene]hydrazine-1-carbothioamide
0.2 mM, 12.27% inhibition; 0.2 mM, 61.99% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide
0.2 mM, 74.8% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 11.94% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[(2-fluorophenyl)(imino)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 14.91% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 30.59% inhibition; 0.2 mM, 51.84% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide
0.2 mM, 60.45% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 28.54% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 7.4% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[(2-fluorophenyl)(imino)methyl]hydrazine-1-carbothioamide
0.2 mM, 23.95% inhibition
-
(2E)-2-[(4-chlorophenyl)methylidene]-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]hydrazine-1-carbothioamide
0.2 mM, 19.65% inhibition; 0.2 mM, 81.81% inhibition
-
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 7.72% inhibition
-
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 13.65% inhibition
-
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[(piperazin-1-yl)methyl]hydrazine-1-carbothioamide
0.2 mM, 72.01% inhibition
-
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 10.34% inhibition
-
(2E)-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]-N-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]hydrazine-1-carbothioamide
0.2 mM, 10.14% inhibition
-
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-1-[(2-fluorophenyl)(imino)methyl]-2-[(4-fluorophenyl)methylidene]hydrazine-1-carbothioamide
0.2 mM, 75.66% inhibition
-
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[(4-fluorophenyl)methylidene]-1-[imino(3,4,5-trimethoxy-2-nitrophenyl)methyl]hydrazine-1-carbothioamide
0.2 mM, 6.22% inhibition; 0.2 mM, 78.38% inhibition
-
(2E)-N-[[4-(4,6-dimethylpyrimidin-2-yl)piperazin-1-yl]methyl]-2-[(4-fluorophenyl)methylidene]-1-[imino(phenyl)methyl]hydrazine-1-carbothioamide
0.2 mM, 8.19% inhibition
-
(E)-[6-(4-fluorophenyl)-2-sulfanylidene-1,6-dihydropyrimidin-5(2H)-ylidene](4-methylphenyl)methanolate
-
-
1,1-cyclopropanedicarboxylic acid
-
i.e. CPCA, inhibition in vivo, effect on pea root length, shoot length, and fermentative metabolism, effects of KARI inhibition effects on other enzymes, such as alcohol dehydrogenase, EC 1.1.1.1, pyruvate dehydrogenase, EC 4.1.1.1, lactate dehydrogenase, EC 1.1.1.27, and alanine aminotransferase, EC 2.6.1.2, overview
1-aminocarbonyl-cyclopropane carboxylate
-
-
1-aminocarbonylcyclopropanecarboxylate
-
1-carbamoylcyclopropanecarboxylic acid
-
-
1-cyano-cyclopropane carboxylate
-
-
1-cyano-cyclopropane-1-carboxylate
-
-
1-cyano-N-(2,4,5-trichlorophenyl)cyclopropanecarboxamide
-
inhibition rate: 0%
1-cyano-N-(2,4-dichlorophenyl)cyclopropanecarboxamide
-
inhibition rate: 97.04%
1-cyano-N-(2-hydroxyethyl)cyclopropanecarboxamide
-
inhibition rate: 98.92%
1-cyano-N-(2-methylphenyl)cyclopropanecarboxamide
-
inhibition rate: 100%
1-cyano-N-(4-methoxyphenyl)cyclopropanecarboxamide
-
inhibition rate: 3.95%
1-cyano-N-(4-methylphenyl)cyclopropanecarboxamide
-
inhibition rate: 61.21%
1-cyano-N-phenylcyclopropanecarboxamide
-
inhibition rate: 77.23%
1-cyano-N-[(E)-(3,3-dichloroprop-1-yn-1-yl)diazenyl]sulfanylcyclopropanecarboxamide
-
inhibition rate: 100%
1-cyano-N-[2-(trifluoromethyl)phenyl]cyclopropanecarboxamide
-
inhibition rate: 0%
1-cyano-N-[3-(trifluoromethyl)phenyl]cyclopropanecarboxamide
-
inhibition rate: 0%
1-cyano-N-[4-(trifluoromethyl)phenyl]cyclopropanecarboxamide
-
inhibition rate: 0%
1-cyano-N-[[(3-methylcyclopropa-1,2-dien-1-yl)amino]sulfanyl]cyclopropanecarboxamide
-
inhibition rate: 69.81%
1-cyanocyclopropanecarboxylate
-
1-cyanocyclopropanecarboxylic acid
1-hydroxycyclopropanecarboxylate
-
11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-one
-
-
2,3-dihydroxy-3-isovalerate
-
-
2,3-dihydroxy-3-methylbutanoic acid
-
linear noncompetitive inhibitor of both 2-acetolactate and NADPH
2,3-dihydroxy-3-methylbutyrate
-
-
2-(4-benzylpiperazin-1-yl)-N-(3,4-dichlorophenyl)acetamide
2-(4-benzylpiperazin-1-yl)-N-arylacetamide
-
-
2-(4-methoxybenzamido)benzoic acid
-
-
2-dimethylphosphinoyl-2-hydroxyacetate
2-dimethylphosphinoyl-2-hydroxyacetic acid
2-dimethylphosphoryl-2-hydroxy-acetic acid
-
2-hydroxy-2-methyl-3-oxopentanoate
-
-
2-Hydroxy-2-methylbutyrate
-
0.01 M 45% inhibition
2-Hydroxybutyrate
-
0.01 M, 48% inhibition
2-Oxo-3-hydroxyisovalerate
-
0.001 mM, 58% inhibition
2-oxoisovalerate
-
0.01 M, 21% inhibition
2-[2-(4-morpholino)]acetamido-4-methylthiazole
-
-
2-[[(4-methoxyphenyl)carbonyl]amino]benzoic acid
3-aminopyridine-NADP+
-
-
3-hydroxy-2-oxobutanoic acid
3-hydroxy-3-methyl-2-oxobutanoic acid
4,4'-(pentamethylenedioxy)dibenzamidne bis(2-hydroxyethanesulfonate)
4-(2,4-dichlorophenoxy)benzenecarboximidamide
-
-
4-(2-fluorophenoxy)benzenecarboximidamide
-
-
4-(3-chlorophenoxy)benzenecarboximidamide
-
-
4-(4-chlorophenoxy)benzenecarboximidamide
-
-
4-phenoxybenzenecarboximidamide
-
-
6-hydroxy-2-methylthiazolo[4,5-d]pyrimidine-5,7(4H,6H)-dione
NSC116565, potent time-dependent inhibitor. The inhibitor binds to Mycobacterium tuberculosis KARI in the presence and absence of the cofactor, NADPH. Inhibits the growth of Mycobacterium tuberculosis H37Ra strain with MIC50 value of 0.00293 mM; NSC116565, potent time-dependent inhibitor. The inhibitor binds to Mycobacterium tuberculosis KARI in the presence and absence of the cofactor, NADPH. Inhibits the growth of Mycobacterium tuberculosis H37Rv strain with MIC50 value of 0.00606 mM
-
arsenite
-
slight inhibition
ascorbic acid
-
slight inhibition with 2-acetolactate as substrate
cyclopropane-1,1-dicarboxylate
cyclopropane-1,1-dicarboxylic acid
-
-
dimethylmalonate
slow-binding inhibitor
ethyl 1-cyanocyclopropanecarboxylate
-
inhibition rate: 0%
ethyl 3-hydroxy-2-oxobutanoate
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
ethyl [(2-chlorophenyl)(hydroxy)amino](oxo)acetate
-
-
ethyl [hydroxy(2-methylphenyl)amino](oxo)acetate
-
-
ethyl [hydroxy(4-methylphenyl)amino](oxo)acetate
-
-
ethyl [[4-(cyanomethyl)phenyl](hydroxy)amino](oxo)acetate
-
-
ethylene glycol
exhibits competitive and uncompetitive inhibition
hydroxy(methyl)propanedioic acid
-
-
L-ascorbic acid
-
slightly inhibitory with alpha-acetolactate as substrate
methyl [hydroxy(1-methylethyl)amino](oxo)acetate
-
-
Mn2+
-
with acetolactate as substrate, Mn2+ behaves as a competitive inhibitor in presence of Mg2+
N'-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(2-fluorophenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(2-methyl-phenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(3-methyl-phenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(3-pyridinyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-(4-nitrophenyl)-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-butyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-ethyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-furan-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-heptyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-iso-propyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-isopropyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-methyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
-
N'-(5-octyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-pentyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-phenyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N'-(5-propyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea
-
-
N-(2-(piperidin-1-yl)ethyl)phthalimide
-
-
N-(3-bromophenyl)-1-cyanocyclopropanecarboxamide
-
inhibition rate: 17.25%
N-(3-chlorophenyl)-1-cyanocyclopropanecarboxamide
-
inhibition rate: 0%
N-(4-bromophenyl)-1-cyanocyclopropanecarboxamide
-
inhibition rate: 32.23%
N-(4-chlorophenyl)-1-cyanocyclopropanecarboxamide
-
inhibition rate: 93.92%
N-(4-chlorophenyl)-N'-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]thiourea
low toxicity against HEK 293T cell lines
-
N-(4-methoxyphenyl)-N'-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]thiourea
low toxicity against HEK 293T cell lines
-
N-(4-methoxyphenyl)-N'-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]thiourea
low toxicity against HEK 293T cell lines
-
N-(5-substituted-1,3,4-thiadiazol-2-yl)-N-cyclopropylformyl-thiourea
-
-
N-Hydroxy-N-isopropyloxamate
N-isopropyloxalyl hydroxamate
-
N-[(4-methoxyphenyl)carbamoyl]-5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-aminide
-
-
1-cyanocyclopropanecarboxylic acid
-
-
1-cyanocyclopropanecarboxylic acid
-
inhibition rate: 100%
2-(4-benzylpiperazin-1-yl)-N-(3,4-dichlorophenyl)acetamide
-
72.6% inhibition at 100 microg/ml
2-(4-benzylpiperazin-1-yl)-N-(3,4-dichlorophenyl)acetamide
-
28.3% inhibition at 100 microg/ml
2-(4-benzylpiperazin-1-yl)-N-(3,4-dichlorophenyl)acetamide
-
48.1% inhibition at 200 microg/ml
2-dimethylphosphinoyl-2-hydroxyacetate
-
i.e. Hoe 704, potent competitive inhibitor in vitro but weak in vivo
2-dimethylphosphinoyl-2-hydroxyacetate
-
i.e. Hoe 704, potent competitive inhibitor in vitro but weak in vivo
2-dimethylphosphinoyl-2-hydroxyacetic acid
-
competitive, reversible
2-dimethylphosphinoyl-2-hydroxyacetic acid
-
nearly irreversible; reversible, strong competitive inhibition
2-dimethylphosphinoyl-2-hydroxyacetic acid
-
i.e. HOE 704, inhibition in vivo, effect on pea root length, shoot length, and fermentative metabolism, effects of KARI inhibition on other enzymes, such as alcohol dehydrogenase, EC 1.1.1.1, pyruvate dehydrogenase, EC 4.1.1.1, lactate dehydrogenase, EC 1.1.1.27, and alanine aminotransferase, EC 2.6.1.2, overview
2-dimethylphosphinoyl-2-hydroxyacetic acid
-
nearly irreversible; reversible, strong competitive inhibition
2-dimethylphosphinoyl-2-hydroxyacetic acid
-
nearly irreversible; reversible, strong competitive inhibition
2-dimethylphosphoryl-2-hydroxy-acetic acid
-
i.e. Hoe 704, reversible inhibitor
-
2-dimethylphosphoryl-2-hydroxy-acetic acid
i.e. Hoe 704, reversible inhibitor
-
2-Hydroxyisovalerate
-
0.01 M, 38% inhibition
2-Hydroxyisovalerate
-
noncompetitive
2-Methyllactate
-
uncompetitive; uncompetitive with respect to NADPH
2-Methyllactate
-
competitive
2-Methyllactate
-
0.001 M, 61% inhibition; competitive
2-[[(4-methoxyphenyl)carbonyl]amino]benzoic acid
-
52% inhibition at 100 microg/ml
2-[[(4-methoxyphenyl)carbonyl]amino]benzoic acid
-
25.9% inhibition at 100 microg/ml
2-[[(4-methoxyphenyl)carbonyl]amino]benzoic acid
-
57.4% inhibition at 200 microg/ml
3-hydroxy-2-oxobutanoic acid
-
-
3-hydroxy-2-oxobutanoic acid
-
-
3-hydroxy-2-oxobutanoic acid
-
-
3-hydroxy-2-oxobutanoic acid
-
-
3-hydroxy-2-oxobutanoic acid
-
-
3-hydroxy-3-methyl-2-oxobutanoic acid
-
-
3-hydroxy-3-methyl-2-oxobutanoic acid
-
-
3-hydroxy-3-methyl-2-oxobutanoic acid
-
-
3-hydroxy-3-methyl-2-oxobutanoic acid
-
-
3-hydroxy-3-methyl-2-oxobutanoic acid
-
-
4,4'-(pentamethylenedioxy)dibenzamidne bis(2-hydroxyethanesulfonate)
-
binding structure and inhibition mechanism, overview
4,4'-(pentamethylenedioxy)dibenzamidne bis(2-hydroxyethanesulfonate)
-
binding structure and inhibition mechanism, overview
chlorsulfuron
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herbicide
chlorsulfuron
-
herbicide
chlorsulfuron
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herbicide
chlorsulfuron
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herbicide
chlorsulfuron
-
herbicide
cyclopropane-1,1-dicarboxylate
-
reversible inhibitor
cyclopropane-1,1-dicarboxylate
reversible inhibitor
cyclopropane-1,1-dicarboxylate
a competitive slow-, tight-binding inhibitor
cyclopropane-1,1-dicarboxylate
-
-
cyclopropane-1,1-dicarboxylate
0.2 mM, 100% inhibition
cyclopropane-1,1-dicarboxylate
binds in a competitively and in multi-dentate manner to the enzyme; the compounds bind competitively and in multi-dentate manner to the enzyme
ethyl 3-hydroxy-2-oxobutanoate
-
-
ethyl 3-hydroxy-2-oxobutanoate
-
-
ethyl 3-hydroxy-2-oxobutanoate
-
-
ethyl 3-hydroxy-2-oxobutanoate
-
-
ethyl 3-hydroxy-2-oxobutanoate
-
-
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
-
-
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
-
-
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
-
-
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
-
-
ethyl 3-methyl-3-hydroxy-2-oxobutanoate
-
-
HOE 704
-
i.e. 2-dimethylphosphinoyl-2-hydroxyacetic acid, competitive inhibitor, potent in vitro, weak as in vivo herbicide
HOE 704
-
i.e. 2-dimethylphosphinoyl-2-hydroxyacetic acid, competitive inhibitor, potent in vitro, weak as in vivo herbicide
HOE 704
-
i.e. 2-dimethylphosphinoyl-2-hydroxyacetic acid, competitive inhibitor, potent in vitro, weak as in vivo herbicide
HOE 704
-
i.e. 2-dimethylphosphinoyl-2-hydroxyacetic acid, competitive inhibitor, potent in vitro, weak as in vivo herbicide
HOE 704
-
i.e. 2-dimethylphosphinoyl-2-hydroxyacetic acid, competitive inhibitor, potent in vitro, weak as in vivo herbicide
IpOHA
-
competitive inhibitor, potent in vitro, weak as in vivo herbicide
IpOHA
-
competitive inhibitor, potent in vitro, weak as in vivo herbicide
IpOHA
-
competitive inhibitor, potent in vitro, weak as in vivo herbicide
IpOHA
-
competitive inhibitor, potent in vitro, weak as in vivo herbicide
IpOHA
-
competitive inhibitor, potent in vitro, weak as in vivo herbicide
metsulfuron-methyl
-
herbicide
metsulfuron-methyl
-
herbicide
metsulfuron-methyl
-
herbicide
metsulfuron-methyl
-
herbicide
metsulfuron-methyl
-
herbicide
MMV553002
i.e. 3-((methylsulfonyl)methyl)-2H-benzo[b][1,4]oxazin-2-one
-
MMV553002
i.e. 3-((methylsulfonyl)methyl)-2H-benzo[b][1,4]oxazin-2-one
-
MMV688271
-
-
N-Hydroxy-N-isopropyloxamate
-
irreversible
N-Hydroxy-N-isopropyloxamate
-
very strong, nearly irreversible inhibition, inhibition also with N-alkyl substituted derivates, tightest binding in presence of Mg2+ and NADPH
N-Hydroxy-N-isopropyloxamate
-
nearly irreversible, competitive; nearly irreversible, poor herbicidal action
N-Hydroxy-N-isopropyloxamate
-
N-Hydroxy-N-isopropyloxamate
-
-
N-Hydroxy-N-isopropyloxamate
-
-
N-Hydroxy-N-isopropyloxamate
-
i.e. IpOHA, potent competitive inhibitor in vitro but weak in vivo
N-Hydroxy-N-isopropyloxamate
-
-
N-Hydroxy-N-isopropyloxamate
-
nearly irreversible, competitive; nearly irreversible, poor herbicidal action
N-Hydroxy-N-isopropyloxamate
-
nearly irreversible, competitive; nearly irreversible, poor herbicidal action
N-Hydroxy-N-isopropyloxamate
-
competitive
N-Hydroxy-N-isopropyloxamate
-
-
N-Hydroxy-N-isopropyloxamate
-
i.e. IpOHA, potent competitive inhibitor in vitro but weak in vivo
N-isopropyloxalyl hydroxamate
0.2 mM, 100% inhibition
-
N-isopropyloxalyl hydroxamate
binds slowly to the enzyme, binds in a competitively and in multi-dentate manner to the enzyme. The observation that the inhibitor is processed to its deoxygenated form in crystallo provides an alternative explanation for the relatively weak herbicidal/antimicrobial activity affordsed by N-isopropyloxalyl hydroxamate despite its low Ki value; the compounds bind competitively and in multi-dentate manner to the enzyme. Binds slowly to the enzyme. Intact N-isopropyloxalyl hydroxamate is present in only 25% of binding sites, whereas its deoxygenated form is present in the remaining sites. This deoxy form of N-isopropyloxalyl hydroxamate binds rapidly to the enzyme, but with much weaker affinity (Ki: 0.021 mM)
-
NADP+
-
-
NADP+
-
linear non-competitive with respect to 2-acetolactate, linear competitive inhibitor of NADPH
NADP+
-
competitive with NADPH
NADP+
-
product inhibition
additional information
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herbicidal effect of inhibitors, overview
-
additional information
-
herbicidal effect of inhibitors, overview
-
additional information
-
herbicidal effect of inhibitors, overview
-
additional information
-
herbicidal effect of inhibitors, overview
-
additional information
-
computer-aided drug design, overview
-
additional information
-
herbicidal effect of inhibitors, overview
-
additional information
no inhibition by 1-aminocyclopropanecarboxylate, 1-methylcyclopropanecarboxylate, 2-methylcyclopropanecarboxylate, cyclopropane-1,2-dicarboxylate, and cyclopropanecarboxylate dimethyl ester
-
additional information
-
computer-aided drug design, overview
-
additional information
-
no inhibition by N'-(5-methyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea, N'-(5-ethyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea, and N'-(5-propyl-1,3,4-thiadiazol-2-yl)-N-cyclopropyformyl-thiourea; structure-activity relationship
-
additional information
-
high throughput receptor-based virtual screening of the ZINC/drug like database based on the crystal structure of ketol-acid reductoisomerase/N-hydroxy-N-isopropyloxamate complex, PDB entry 1YVE
-
additional information
-
computer-aided drug design, overview
-
additional information
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molecular design of KARI inhibitors, and synthesis, overview. Structure-function relationship, analysis by computational docking of inhibitor molecules to cyrstal structure. No inhibition by 5-[(4-morpholino/piperidin-1-yl)acetyl]-10
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additional information
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no inhibition with p-mercuribenzoate, cysteine, 2-mercaptoethanol
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