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Literature summary for 3.4.21.39 extracted from
- Endothelin-1 (1-31): from chymase-dependent synthesis to cardiovascular pathologies (2008), Vascul. Pharmacol., 49, 51-62.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | chymase is upregulated in atherosclerotic conditions | Homo sapiens |
| medicine | chymase, is upregulated in atherosclerotic conditions | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide | NK3201 | Homo sapiens |  |
| 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide | NK3201 | Mus musculus | |
| 3-[(3,4-dimethoxyphenyl)sulfonyl]-1-(3,4-dimethylphenyl)imidazoline-2,4-dione | C41 | Homo sapiens | |
| 3-[(3,4-dimethoxyphenyl)sulfonyl]-1-(3,4-dimethylphenyl)imidazoline-2,4-dione | C41 | Mus musculus | |
| 4-[1-(naphthylmethyl)benzimidazol-2-ylthio]butanoic acid | TEI-E548 | Homo sapiens | |
| 4-[1-(naphthylmethyl)benzimidazol-2-ylthio]butanoic acid | TEI-E548 | Mus musculus | |
| 4-[1-[[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy]-benzoic acid | - |
Homo sapiens | |
| 4-[1-[[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy]-benzoic acid | - |
Mus musculus | |
| chymostatin | i.e. (S)-1-carboxy-2-(phenylethyl)-carbamoyl-alpha-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal | Homo sapiens | |
| chymostatin | i.e. (S)-1-carboxy-2-(phenylethyl)-carbamoyl-alpha-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal | Mus musculus | |
| JNJ-10311795 | - |
Homo sapiens | |
| JNJ-10311795 | - |
Mus musculus | |
| N-tosyl-L-phenylalanyl-chloromethyl ketone | - |
Homo sapiens | |
| N-tosyl-L-phenylalanyl-chloromethyl ketone | - |
Mus musculus | |
| RWJ-355871 | - |
Homo sapiens | |
| RWJ-355871 | - |
Mus musculus | |
| succinyl-Val-Pro-PheP(OPh)2 | - |
Homo sapiens | |
| succinyl-Val-Pro-PheP(OPh)2 | - |
Mus musculus | |
| succinyl-Val-Pro-PheP-(OPh)2 | highly specific and metabolically stable chymase inhibitor with a biological half-life of more than 20 h | Homo sapiens | |
| succinyl-Val-Pro-PheP-(OPh)2 | highly-specific and metabolically stable chymase inhibitor with a biological half-life of more than 20 h | Mus musculus | |
| SUN-C8007 | i.e. 3-(3-aminophenylsulfonyl)-7-chloroquinazorine-2,4(1H,3H)-dione | Homo sapiens | |
| SUN-C8007 | i.e. 3-(3-aminophenylsulfonyl)-7-chloroquinazorine-2, 4(1H,3H)-dione | Mus musculus | |
| SUN-C8257 | i.e. 3-[(3-amino-4-carboxy)phenylsulfonyl]-7-chloroquinazorine 2,4(1H,3H)-dione | Homo sapiens | |
| SUN-C8257 | i.e. 3-[(3-amino-4-carboxy)phenylsulfonyl]-7-chloroquinazorine 2,4(1H,3H)-dione | Mus musculus | |
| suramin | i.e. 8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid | Homo sapiens | |
| suramin | i.e. 8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid | Mus musculus | |
| TY-51184 | highly-specific and orally active chymase inhibitor; i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamide-3-methanesulfonylphenyl]oxazole-4-carboxylic acid | Homo sapiens | |
| TY-51184 | highly-specific and orally-active chymase inhibitor; i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamide-3-methanesulfonylphenyl]oxazole-4-carboxylic acid | Mus musculus | |
| TY-51469 | i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamido-3-methanesulfonylphenyl]thiazole-4-carboxylic acid; inhibitor with very high affinity (IC50 0.1 nmol/kg) against chymase | Homo sapiens | |
| TY-51469 | i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamido-3-methanesulfonylphenyl]thiazole-4-carboxylic acid; inhibitor with very high affinity against chymase | Mus musculus | |
| Y-40018 | i.e. 4-[5-amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidin-1-ylacetamido]-N-benzyl-2,2-difluoro-3-oxo-5-phenylpentanamide | Homo sapiens | |
| Y-40018 | i.e. 4-[5-amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidin-1-ylacetamido]-N-benzyl-2,2-difluoro-3-oxo-5-phenylpentanamide | Mus musculus | |
| Y-40079 | i.e. 2-[2-[2-[5-amino-2-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-1-yl]acetamido]-3-phenylpropionyl]benzoxazole-5-carboxylic acid methyl ester | Homo sapiens | |
| Y-40079 | i.e. 2-[2-[2-[5-amino-2-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-1-yl]acetamido]-3-phenylpropionyl]benzoxazole-5-carboxylic acid methyl ester | Mus musculus | |
| Z-Ile-Glu-Pro-Phe-CO2Me | - |
Homo sapiens | |
| Z-Ile-Glu-Pro-Phe-CO2Me | - |
Mus musculus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| mast cell granule | - |
Mus musculus | 42629 | - |
| mast cell granule | - |
Homo sapiens | 42629 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| angiotensin I + H2O | Mus musculus | - |
angiotensin II + His-Leu | - |
? | |
| angiotensin I + H2O | Homo sapiens | - |
angiotensin II + His-Leu | - |
? | |
| big-endothelin-1 (1-38) + H2O | Mus musculus | chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38) | endothelin-1 (1-31) + ? | - |
? | |
| big-endothelin-1 (1-38) + H2O | Homo sapiens | chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38) | endothelin-1 (1-31) + ? | - |
? | |
| Fibronectin + H2O | Mus musculus | - |
? | - |
? | |
| Fibronectin + H2O | Homo sapiens | - |
? | - |
? | |
| plasmin + H2O | Mus musculus | - |
? | - |
? | |
| plasmin + H2O | Homo sapiens | - |
? | - |
? | |
| promatrix metalloproteinase-2 + H2O | Mus musculus | - |
matrix metalloproteinase-2 | - |
? | |
| promatrix metalloproteinase-2 + H2O | Homo sapiens | - |
matrix metalloproteinase-2 | - |
? | |
| promatrix metalloproteinase-9 + H2O | Mus musculus | - |
matrix metalloproteinase-9 | - |
? | |
| promatrix metalloproteinase-9 + H2O | Homo sapiens | - |
matrix metalloproteinase-9 | - |
? | |
| thrombin + H2O | Mus musculus | - |
? | - |
? | |
| thrombin + H2O | Homo sapiens | - |
? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| mast cell | - |
Mus musculus | - |
| mast cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| angiotensin I + H2O | - |
Mus musculus | angiotensin II + His-Leu | - |
? | |
| angiotensin I + H2O | - |
Homo sapiens | angiotensin II + His-Leu | - |
? | |
| big-endothelin-1 (1-38) + H2O | chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38) | Mus musculus | endothelin-1 (1-31) + ? | - |
? | |
| big-endothelin-1 (1-38) + H2O | chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38) | Homo sapiens | endothelin-1 (1-31) + ? | - |
? | |
| Fibronectin + H2O | - |
Mus musculus | ? | - |
? | |
| Fibronectin + H2O | - |
Homo sapiens | ? | - |
? | |
| plasmin + H2O | - |
Mus musculus | ? | - |
? | |
| plasmin + H2O | - |
Homo sapiens | ? | - |
? | |
| promatrix metalloproteinase-2 + H2O | - |
Mus musculus | matrix metalloproteinase-2 | - |
? | |
| promatrix metalloproteinase-2 + H2O | - |
Homo sapiens | matrix metalloproteinase-2 | - |
? | |
| promatrix metalloproteinase-9 + H2O | - |
Mus musculus | matrix metalloproteinase-9 | - |
? | |
| promatrix metalloproteinase-9 + H2O | - |
Homo sapiens | matrix metalloproteinase-9 | - |
? | |
| thrombin + H2O | - |
Mus musculus | ? | - |
? | |
| thrombin + H2O | - |
Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Chy | - |
Mus musculus |
| Chy | - |
Homo sapiens |
| MCP-4 | - |
Mus musculus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000023 | - |
- |
Homo sapiens | JNJ-10311795 | |
| 0.0000025 | - |
- |
Homo sapiens | 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide | |
| 0.00000262 | - |
- |
Homo sapiens | Y-40018 | |
| 0.00000485 | - |
- |
Homo sapiens | Y-40079 | |
| 0.0000054 | - |
- |
Homo sapiens | 4-[1-[[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy]-benzoic acid | |
| 0.0000062 | - |
- |
Homo sapiens | 4-[1-(naphthylmethyl)benzimidazol-2-ylthio]butanoic acid | |
| 0.000007 | - |
- |
Homo sapiens | TY-51469 | |
| 0.000037 | - |
- |
Homo sapiens | TY-51184 | |
| 0.00006 | - |
- |
Homo sapiens | 3-[(3,4-dimethoxyphenyl)sulfonyl]-1-(3,4-dimethylphenyl)imidazoline-2,4-dione | |
| 0.00013 | - |
- |
Homo sapiens | SUN-C8257 | |
| 0.00024 | - |
- |
Homo sapiens | chymostatin | |
| 0.00036 | - |
- |
Homo sapiens | SUN-C8007 | |
| 0.12 | - |
- |
Homo sapiens | suramin | |
| 8 | - |
- |
Homo sapiens | N-tosyl-L-phenylalanyl-chloromethyl ketone | |
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