Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(2-Amino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid (1-benzyl-3,3,3-trifluoro-2-oxo-propyl)-amide | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(3-amino-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid diethylamide | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethylamide | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-6-carboxylic acid methyl ester | - |
Homo sapiens | |
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-[2-[2-[5-amino-2-(3-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-[2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-fluoro-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-methoxy-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-oxo-2-(5-phenyl-benzooxazol-2-yl)-ethyl]-acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(2-benzoxazolyl)carbonyl]-2-phenylethyl]-acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-aminobenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carbamoylbenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carboxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | - |
Homo sapiens | |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-hydroxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | - |
Homo sapiens | |
2-{2-[2-(5-Amino-6-oxo-2-m-tolyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-{2-[2-(5-Amino-6-oxo-2-phenyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
2-{2-[2-(5-Amino-6-oxo-2-pyridin-3-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester | novel, potent, and orally active inhibitor. Rapidly after oral administration and has satisfactory bioavailability | Homo sapiens | |
2-{2-[2-(5-Amino-6-oxo-2-pyridin-4-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester | - |
Homo sapiens | |
chymostatin | - |
Homo sapiens | |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | novel, potent, and orally active inhibitor. Rapidly after oral administration and has satisfactory bioavailability, 32% | Canis lupus familiaris | |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | novel, potent, and orally active inhibitor. Rapidly after oral administration and has satisfactory bioavailability | Mus musculus | |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | novel, potent, and orally active inhibitor. Rapidly after oral administration and has satisfactory bioavailability, 17% | Rattus norvegicus | |
[1-[(1-Benzyl-2-hydroxy-2-oxazolo[5,4-b]pyridin-2-yl-ethylcarbamoyl)-methyl]-2-(4-fluoro-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Canis lupus familiaris | - |
- |
- |
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
heart | - |
Homo sapiens | - |
peritoneum | - |
Mus musculus | - |
peritoneum | - |
Rattus norvegicus | - |
skin | - |
Canis lupus familiaris | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O | - |
Mus musculus | succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline | - |
? | |
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O | - |
Homo sapiens | succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline | - |
? | |
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O | - |
Rattus norvegicus | succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline | - |
? | |
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O | - |
Canis lupus familiaris | succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00000262 | - |
2-[2-[2-(5-amino-6-oxo-2-pyridin-3-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.00000356 | - |
2-[2-[2-(5-amino-6-oxo-2-phenyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.000005 | - |
1-(2-Amino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid (1-benzyl-3,3,3-trifluoro-2-oxo-propyl)-amide | pH 7.5, 37°C | Homo sapiens | |
0.00000771 | - |
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethylamide | pH 7.5, 37°C | Homo sapiens | |
0.00000932 | - |
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid diethylamide | pH 7.5, 37°C | Homo sapiens | |
0.0000097 | - |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-hydroxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0000097 | - |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-oxo-2-(5-phenyl-benzooxazol-2-yl)-ethyl]-acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0000102 | - |
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000102 | - |
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-6-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.000012 | - |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carbamoylbenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0000131 | - |
chymostatin | pH 7.5, 37°C | Homo sapiens | |
0.0000133 | - |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(2-benzoxazolyl)carbonyl]-2-phenylethyl]-acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0000138 | - |
2-[2-[2-(5-amino-6-oxo-2-pyridin-4-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000157 | - |
2-[2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000166 | - |
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000169 | - |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carboxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0000169 | - |
2-[2-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000185 | - |
2-[2-[2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.000028 | - |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | pH 7.5, 37°C | Canis lupus familiaris | |
0.0000289 | - |
2-[2-[2-(5-amino-6-oxo-2-m-tolyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000325 | - |
2-[2-[2-[5-amino-2-(3-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000506 | - |
[1-[(1-Benzyl-2-hydroxy-2-oxazolo[5,4-b]pyridin-2-yl-ethylcarbamoyl)-methyl]-2-(4-fluoro-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester | pH 7.5, 37°C | Homo sapiens | |
0.0000907 | - |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-fluoro-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide | pH 7.5, 37°C | Homo sapiens | |
0.0004 | - |
2-[2-[2-[5-amino-2-(3-amino-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester | pH 7.5, 37°C | Homo sapiens | |
0.000489 | - |
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-methoxy-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide | pH 7.5, 37°C | Homo sapiens | |
0.000489 | - |
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-aminobenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide | pH 7.5, 37°C | Homo sapiens | |
0.00126 | - |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | pH 7.5, 37°C | Mus musculus | |
0.00424 | - |
N-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetyl]-N,N'-dibenzyl-2,2-difluoro-malonamide | pH 7.5, 37°C | Rattus norvegicus |