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Literature summary for 3.4.21.39 extracted from

  • Akahoshi, F.; Ashimori, A.; Sakashita, H.; Yoshimura, T.; 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 alpha-keto heterocycles as novel inhibitors of human chymase (2001), J. Med. Chem., 44, 1286-1296.
    View publication on PubMed
Search for more literature for 3.4.21.39

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-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase 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-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
-
 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
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-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase Canis lupus familiaris
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 i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase Mus musculus
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 i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase Rattus norvegicus
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
-
 Canis lupus familiaris
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-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
 Mus musculus
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
-
 Rattus norvegicus
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxazolo[4,5-b]pyridin-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-thiazol-2-yl-ethyl)-acetamide
-
 Homo sapiens
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(2-benzothiazol-2-yl-1-benzyl-2-oxo-ethyl)-acetamide
-
 Homo sapiens
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(4,5-dihydro-oxazol-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-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-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
chymostatin
-
 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-nitroanilide + H2O
-
 Homo sapiens ?
-
 ?
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
-
 Rattus norvegicus ?
-
 ?
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
-
 Canis lupus familiaris ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000112
-
 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
-
 Canis lupus familiaris
0.00000368
-
 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
-
 Canis lupus familiaris
0.00000557
-
 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
0.0000056
-
 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
0.0000131
-
 chymostatin
-
 Homo sapiens
0.0000143
-
 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
0.0000226
-
 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
0.000026
-
 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
0.0000261
-
 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
0.00003
-
 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
0.0000404
-
 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
-
 Mus musculus
0.0000418
-
 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
0.0000435
-
 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
0.0000442
-
 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
0.0000485
-
 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 i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase Homo sapiens
0.0000563
-
 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
0.0000595
-
 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
0.0000606
-
 2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxazolo[4,5-b]pyridin-2-yl-2-oxo-ethyl)-acetamide
-
 Homo sapiens
0.0000639
-
 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
-
 Mus musculus
0.0000686
-
 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
0.0000733
-
 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
0.0000774
-
 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
-
 Homo sapiens
0.0000821
-
 1-(2-Amino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid (1-benzyl-3,3,3-trifluoro-2-oxo-propyl)-amide
-
 Homo sapiens
0.0000866
-
 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
-
 Rattus norvegicus
0.0000931
-
 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
0.000094
-
 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
0.000103
-
 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
-
 Rattus norvegicus
0.000125
-
 2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(2-benzoxazolyl)carbonyl]-2-phenylethyl]-acetamide
-
 Homo sapiens
0.000174
-
 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
0.000182
-
 2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(2-benzothiazol-2-yl-1-benzyl-2-oxo-ethyl)-acetamide
-
 Homo sapiens
0.000183
-
 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
0.00076
-
 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
0.00212
-
 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
0.00385
-
 2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxo-2-thiazol-2-yl-ethyl)-acetamide
-
 Homo sapiens
0.00589
-
 2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(4,5-dihydro-oxazol-2-yl)-2-oxo-ethyl]-acetamide
-
 Homo sapiens