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Literature summary for 3.4.21.39 extracted from

  • Akahoshi, F.; Ashimori, A.; Yoshimura, T.; Imada, T.; Nakajima, M.; Mitsutomi, N.; Kuwahara, S.; Ohtsuka, T.; Fukaya, C.; Miyazaki, M.; Nakamura, N.
    Non-peptidic inhibitors of human chymase. Synthesis, structure-activity relationships, and pharmacokinetic profiles of a series of 5-amino-6-oxo-1,6-dihydropyrimidine-containing trifluoromethyl ketones (2001), Bioorg. Med. Chem., 9, 301-315.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(5-Acetylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Amino-6-oxo-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-hydroxypropyl)acetamide
-
Homo sapiens
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(2-phenethyl)acetamide
-
Homo sapiens
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-methylacetamide
-
Homo sapiens
2-(5-Benzenesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Benzoylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Benzyloxycarbonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Mehoxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Methanesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-(5-Oxaloamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[2-(4-Fluorophenyl)-5-hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(3-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-aminophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-hydroxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-2-(4-nitrophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-6-oxo-2-(3-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-6-oxo-2-(4-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
2-[5-Amino-6-oxo-2-(p-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
3-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)propanamide
-
Homo sapiens
L-Valyl-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)-L-prolinamide hydrochloride
-
Homo sapiens
N-(1-Benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
MeO-succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
Homo sapiens MeO-succinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000506
-
2-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.0000656
-
2-(5-Hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.00008
-
L-Valyl-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)-L-prolinamide hydrochloride
-
Homo sapiens
0.000105
-
2-(5-Acetylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.00012
-
2-[5-Amino-2-(4-aminophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000124
-
2-[5-Amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000141
-
2-[5-Amino-2-(3-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000146
-
2-(5-Benzyloxycarbonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000186
-
2-[5-Amino-6-oxo-2-(p-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000229
-
2-(5-Mehoxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000237
-
2-[2-(4-Fluorophenyl)-5-hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000305
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000306
-
2-(5-Benzoylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000369
-
2-(5-Benzenesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000377
-
2-[5-Amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000389
-
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000471
-
2-[5-Amino-2-(4-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000479
-
2-[5-Amino-2-(4-hydroxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000487
-
2-[5-Amino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000547
-
2-[5-Amino-2-(4-nitrophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.000658
-
2-[5-Amino-6-oxo-2-(3-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.00103
-
2-(5-Methanesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.00122
-
2-[5-Amino-6-oxo-2-(4-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.00447
-
2-(5-Oxaloamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.02
-
N-(1-Benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.03
-
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-hydroxypropyl)acetamide
-
Homo sapiens
0.03
-
3-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)propanamide
-
Homo sapiens
0.06
-
2-(5-Amino-6-oxo-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
Homo sapiens
0.08
-
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-methylacetamide
-
Homo sapiens
0.11
-
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(2-phenethyl)acetamide
-
Homo sapiens