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Literature summary for 3.4.21.10 extracted from

  • Zhao, J.; Tian, W.; Qi, J.; Lv, D.; Liu, Y.; Jiang, Y.; Dong, G.; Chen, Q.; Zhou, Y.; Zhu, J.; Wang, H.; Sheng, C.; Lv, J.
    Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 2802-2806.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-aminobenzamidine
-
Homo sapiens
5-(2,4-dichlorophenyl)-1,2-oxazole-3-carbaldehyde
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(1-hydroxypropan-2-yl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2,3-dimethylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2,4-dimethoxyphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2,5-dimethoxyphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2,6-dimethylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2-methoxyphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(2-methylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(3,5-dimethylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(3-chlorophenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(3-methoxyphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(3-methylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-chlorophenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-cyanophenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-ethoxyphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-fluorophenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-methylphenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(4-methylpyridin-2-yl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(naphthalen-1-yl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-(propan-2-yl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-phenyl-1,2-oxazole-3-carboxamide
-
Homo sapiens
5-(4-carbamimidamidophenyl)-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-3-carboxamide hydrochloride
-
Homo sapiens
DV-1006
-
Homo sapiens
ethyl 4-([[5-(4-carbamimidamidophenyl)-1,2-oxazol-3-yl]carbonyl]amino)benzoate hydrochloride
-
Homo sapiens
ethyl 5-[4-(benzoylamino)phenyl]-1,2-oxazole-3-carboxylate
-
Homo sapiens
ethyl 5-[4-[(2-chlorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
-
Homo sapiens
ethyl 5-[4-[(3,4-dichlorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
-
Homo sapiens
ethyl 5-[4-[(4-chlorobenzoyl)amino]phenyl]1,2-oxazole-3-carboxylate
-
Homo sapiens
ethyl 5-[4-[(4-fluorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
-
Homo sapiens
guanidinobenzoate KF950 Homo sapiens
L-1-chloro-3-[4-tosylamido]-7-amino-2-heptanone
-
Homo sapiens
N-(2-bromophenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide
-
Homo sapiens
N-(3-bromophenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide hydrochloride
-
Homo sapiens
N-(4-tert-butylphenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide hydrochloride
-
Homo sapiens
N-(diaminomethylidene)-4-(4-methylanilino)benzene-1-sulfonamide
-
Homo sapiens
phenylpyrazole
-
Homo sapiens
quinazolinone
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Nalpha-benzoyl-L-arginine 4-nitroanilide + H2O
-
Homo sapiens Nalpha-benzoyl-L-arginine + 4-nitroaniline
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0014
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2,4-dimethoxyphenyl)-1,2-oxazole-3-carboxamide
0.0023
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2,5-dimethoxyphenyl)-1,2-oxazole-3-carboxamide
0.0057
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2,6-dimethylphenyl)-1,2-oxazole-3-carboxamide
0.0064
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-ethoxyphenyl)-1,2-oxazole-3-carboxamide
0.0066
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(3-methoxyphenyl)-1,2-oxazole-3-carboxamide
0.0078
-
pH 7.8, 37.8°C Homo sapiens N-(4-tert-butylphenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide hydrochloride
0.0084
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2-methoxyphenyl)-1,2-oxazole-3-carboxamide
0.0093
-
pH 7.8, 37.8°C Homo sapiens ethyl 4-([[5-(4-carbamimidamidophenyl)-1,2-oxazol-3-yl]carbonyl]amino)benzoate hydrochloride
0.0094
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(3-methylphenyl)-1,2-oxazole-3-carboxamide
0.0101
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-methylphenyl)-1,2-oxazole-3-carboxamide
0.0115
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2,3-dimethylphenyl)-1,2-oxazole-3-carboxamide
0.0121
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(3,5-dimethylphenyl)-1,2-oxazole-3-carboxamide
0.0144
-
pH 7.8, 37.8°C Homo sapiens N-(3-bromophenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide hydrochloride
0.0144
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(2-methylphenyl)-1,2-oxazole-3-carboxamide
0.0203
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-3-carboxamide hydrochloride
0.0205
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-fluorophenyl)-1,2-oxazole-3-carboxamide
0.0214
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-methylpyridin-2-yl)-1,2-oxazole-3-carboxamide
0.0239
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-cyanophenyl)-1,2-oxazole-3-carboxamide
0.0246
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-phenyl-1,2-oxazole-3-carboxamide
0.0254
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(3-chlorophenyl)-1,2-oxazole-3-carboxamide
0.0268
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(4-chlorophenyl)-1,2-oxazole-3-carboxamide
0.0279
-
pH 7.8, 37.8°C Homo sapiens N-(2-bromophenyl)-5-(4-carbamimidamidophenyl)-1,2-oxazole-3-carboxamide
0.0299
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(naphthalen-1-yl)-1,2-oxazole-3-carboxamide
0.06
-
pH 7.8, 37.8°C Homo sapiens ethyl 5-[4-[(2-chlorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
0.1
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(propan-2-yl)-1,2-oxazole-3-carboxamide
0.1
-
pH 7.8, 37.8°C Homo sapiens 5-(4-carbamimidamidophenyl)-N-(1-hydroxypropan-2-yl)-1,2-oxazole-3-carboxamide
0.14
-
pH 7.8, 37.8°C Homo sapiens ethyl 5-[4-[(4-fluorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
0.24
-
pH 7.8, 37.8°C Homo sapiens ethyl 5-[4-[(3,4-dichlorobenzoyl)amino]phenyl]-1,2-oxazole-3-carboxylate
0.38
-
pH 7.8, 37.8°C Homo sapiens ethyl 5-[4-[(4-chlorobenzoyl)amino]phenyl]1,2-oxazole-3-carboxylate
0.39
-
pH 7.8, 37.8°C Homo sapiens 5-(2,4-dichlorophenyl)-1,2-oxazole-3-carbaldehyde
0.46
-
pH 7.8, 37.8°C Homo sapiens ethyl 5-[4-(benzoylamino)phenyl]-1,2-oxazole-3-carboxylate