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Literature summary extracted from

  • Miyazaki, M.; Takai, S.; Jin, D.; Muramatsu, M.
    Pathological roles of angiotensin II produced by mast cell chymase and the effects of chymase inhibition in animal models (2006), Pharmacol. Ther., 112, 668-676.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.39 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide NK3201 Canis lupus familiaris
3.4.21.39 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide NK3201 Homo sapiens
3.4.21.39 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide NK3201 Mesocricetus auratus
3.4.21.39 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid TY-1184 Canis lupus familiaris
3.4.21.39 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid TY-1184 Homo sapiens
3.4.21.39 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid TY-1184 Mesocricetus auratus
3.4.21.39 3[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione N-C8257 Canis lupus familiaris
3.4.21.39 3[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione N-C8257 Homo sapiens
3.4.21.39 3[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione N-C8257 Mesocricetus auratus
3.4.21.39 4-[1-[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy-benzoic acid BCEAB Canis lupus familiaris
3.4.21.39 4-[1-[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy-benzoic acid BCEAB Homo sapiens
3.4.21.39 4-[1-[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy-benzoic acid BCEAB Mesocricetus auratus
3.4.21.39 chymostatin
-
 Canis lupus familiaris
3.4.21.39 chymostatin
-
 Homo sapiens
3.4.21.39 chymostatin
-
 Mesocricetus auratus
3.4.21.39 Suc-Val-Pro-PheP-(OPh)2 noncompetitive inhibitor Canis lupus familiaris
3.4.21.39 Suc-Val-Pro-PheP-(OPh)2 noncompetitive inhibitor Homo sapiens
3.4.21.39 Suc-Val-Pro-PheP-(OPh)2 noncompetitive inhibitor Mesocricetus auratus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.39 Canis lupus familiaris
-
-
-
3.4.21.39 Homo sapiens
-
-
-
3.4.21.39 Mesocricetus auratus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.39 mast cell
-
 Homo sapiens
-
3.4.21.39 mast cell
-
 Canis lupus familiaris
-
3.4.21.39 mast cell
-
 Mesocricetus auratus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.39 angiotensin I + H2O
-
 Homo sapiens angiotensin II + ?
-
 ?
3.4.21.39 angiotensin I + H2O
-
 Canis lupus familiaris angiotensin II + ?
-
 ?
3.4.21.39 angiotensin I + H2O
-
 Mesocricetus auratus angiotensin II + ?
-
 ?
3.4.21.39 latent transforming growth factor-beta + H2O
-
 Homo sapiens active transforming growth factor-beta + ?
-
 ?
3.4.21.39 latent transforming growth factor-beta + H2O
-
 Canis lupus familiaris active transforming growth factor-beta + ?
-
 ?
3.4.21.39 latent transforming growth factor-beta + H2O
-
 Mesocricetus auratus active transforming growth factor-beta + ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.39 alpha-chymase
-
 Homo sapiens
3.4.21.39 alpha-chymase
-
 Canis lupus familiaris
3.4.21.39 alpha-chymase
-
 Mesocricetus auratus
3.4.21.39 mast cell protease
-
 Homo sapiens
3.4.21.39 mast cell protease
-
 Canis lupus familiaris
3.4.21.39 mast cell protease
-
 Mesocricetus auratus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.39 0.0000028
-
-
 Homo sapiens Suc-Val-Pro-PheP-(OPh)2
3.4.21.39 0.0000054
-
-
 Homo sapiens 4-[1-[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy-benzoic acid
3.4.21.39 0.000012
-
-
 Canis lupus familiaris 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide
3.4.21.39 0.000025
-
-
 Homo sapiens 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide
3.4.21.39 0.000037
-
-
 Homo sapiens 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid
3.4.21.39 0.000058
-
-
 Canis lupus familiaris 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid
3.4.21.39 0.000128
-
-
 Mesocricetus auratus 2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid
3.4.21.39 0.00028
-
-
 Mesocricetus auratus 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide
3.4.21.39 0.00031
-
-
 Homo sapiens 3-[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione
3.4.21.39 0.00068
-
-
 Mesocricetus auratus 3-[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione