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Literature summary for 3.4.21.39 extracted from

  • Akahoshi, F.; Ashimori, A.; Sakashita, H.; Yoshimura, T.; Eda, M.; Imada, T.; Nakajima, M.; Mitsutomi, N.; Kuwahara, S.; Ohtsuka, T.; Fukaya, C.; Miyazaki, M.; Nakamura, N.
    Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase (2001), J. Med. Chem., 44, 1297-1304.
    View publication on PubMed

Inhibitors

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

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
heart
-
Homo sapiens
-
peritoneum
-
Mus musculus
-
peritoneum
-
Rattus norvegicus
-
skin
-
Canis lupus familiaris
-

Substrates and Products (Substrate)

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 [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