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Literature summary for 3.4.21.117 extracted from

  • Arama, D.; Soualmia, F.; Lisowski, V.; Longevial, J.; Bosc, E.; Maillard, L.; Martinez, J.; Masurier, N.; El Amri, C.
    Pyrido-imidazodiazepinones as a new class of reversible inhibitors of human kallikrein 7 (2015), Eur. J. Med. Chem., 93, 203-213.
No PubMed abstract available
Search for more literature for 3.4.21.117

Inhibitors

Inhibitors Comment Organism Structure
(4R)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-(1-naphthyl)methyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-(4-benzyloxy)benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-(4-hydroxyphenyl)-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(2,4-dimethylphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one cytotoxic effect Homo sapiens
(4S)-4-benzyl-2-(2,5-dihydroxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(2,5-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one cytotoxic effect Homo sapiens
(4S)-4-benzyl-2-(2-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(2-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(2-methylpropyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(3,4,5-trimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one cytotoxic effect Homo sapiens
(4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one mechanism of inhibition, modeling, overview. Cytotoxic effect Homo sapiens
(4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-4,5-dihydro-3H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-ol
-
 Homo sapiens
(4S)-4-benzyl-2-(3-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(3-methoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(3-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(4-bromophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(4-nitrophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-(pyridin-3-yl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-2-phenyl-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyl-3,4-dihydro-1H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepine-2,5-dione
-
 Homo sapiens
(4S)-4-benzyloxymethyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-benzyloxymethyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido [10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-hydroxymethyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2] imi-dazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-methyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]-imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(4S)-4-methyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
-
 Homo sapiens
(S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3-methyl-3H-pyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5(4H)-one
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-1H-pyrrole-2-carboxamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-methylbenzamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-phenylacetamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3,4-dimethoxybenzamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-3-phenylpropanamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)benzamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)cinnamamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)isonicotinamide
-
 Homo sapiens
(S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)picolinamide
-
 Homo sapiens
additional information usage of the pyridoimidazodiazepinone core as a potential scaffold to develop selective and competitive reversible inhibitors, analysis of structure-activity relationships, inhibition mechanisms, and selectivity as well as cytotoxicity against selected three human cancer cell lines, i.e. the HeLa cells, prostatic PC-3 cell line, and colorectal adenocarcinoma SW-620 cells, structure-based molecular docking, overview. No inhibition by 1b, 1f, 1g, 1h, 1i, 1j, 1l, 1m, 1q, 1r, 1s, 1t, 1u, 1v, 1w, 1x, 1z, 1aa, 1ab, 1ac, 1ad, 2a, 2b, 2c, 2d, 2f, 2h, and 2i Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens succinyl-Leu-Leu-Val-Tyr + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
kallikrein-7
-
 Homo sapiens
KLK7
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0335
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(3,4-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
0.0557
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(3,4,5-trimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2] imidazo[4,5-d][1,3]diazepin-5-one
0.057
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
0.068
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
0.072
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one
0.0809
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(2,5-dimethoxyphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
0.0839
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(2,4-dimethylphenyl)-3,4-dihydro-5Hpyrido[10,20:1,2]imidazo [4,5-d][1,3]diazepin-5-one
0.0959
-
 pH 8..0, 37°C Homo sapiens (4R)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo[4,5-d][1,3]diazepin-5-one
0.1248
-
 pH 8..0, 37°C Homo sapiens (4S)-4-benzyl-2-(3-hydroxyphenyl)-3,4-dihydro-5H-pyrido[10,20:1,2]imidazo-[4,5-d][1,3]diazepin-5-one
0.1354
-
 pH 8..0, 37°C Homo sapiens (S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-methylbenzamide
0.1492
-
 pH 8..0, 37°C Homo sapiens (S)-N-(1-(2-amino-imidazo[1,2-a]pyridin-3-yl)-1-oxo-3-phenylpropan-2-yl)-2-phenylacetamide

General Information

General Information Comment Organism
evolution human tissue kallikrein-7 is a chymotryptic serine protease member of tissue kallikrein family. Homo sapiens
physiological function the enzyme is involved in skin homeostasis and inflammation. Excess of enzyme activity is also associated with tumor metastasis processes, especially in ovarian carcinomas, prostatic and pancreatic cancers Homo sapiens