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chymase 1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2340

Nomenclature: chymase 1

Family: S1: Chymotrypsin

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 247 14q12 CMA1 chymase 1
Mouse - 247 14 28.19 cM Cma1 chymase 1, mast cell
Rat - 247 15p13 Cma1 chymase 1
Previous and Unofficial Names Click here for help
alpha-chymase | chymase 1, mast cell | mast cell protease 3 | mast cell protease 5 | mast cell protease I | mast cell protease III | MCP3P | Mcp5
Database Links Click here for help
Specialist databases
MEROPS S01.140 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Human chymase in complex with 7-oxo-3-(phenoxyimino)-1,4-diazepane derivative (compound 7f).
Ligand:  compound 7f [PMID: 29191554]
Resolution:  1.9Å
Species:  Human
References:  1
Enzyme Reaction Click here for help
EC Number:

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Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
NK3201 Small molecule or natural product Hs Inhibition 8.6 pIC50 8
pIC50 8.6 (IC50 2.5x10-9 M) [8]
JNJ-10311795 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 2
pIC50 8.3 (IC50 4.5x10-9 M) [2]
TY-51469 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 5,7
pIC50 8.1 (IC50 7x10-9 M) [5,7]
compound 7f [PMID: 29191554] Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 1
pIC50 8.1 (IC50 8.9x10-9 M) [1]
Immunopharmacology Comments
Chymase is a chymotrypsin-like serine protease that is expressed by mast cells. Amongst its activities, chymase is involved in the conversion of angiotensin (AT) I to ATII, its protease activity cleaves latent TGFβ1 and IL-1β in the cellular environment to generate the active cytokines, and it can further stimulate mast cell degranulation in a self-amplification loop. The potential of chymase as a drug target for inflammatory and gastrointestinal disorders is reviewed by Heuston and Hyland (2012) [3]. Chymase inhibitors are being investigated for anti-inflammatory potential [4,7] (and cardiovascular disease [10]).
Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  Chymase is present in mast cell secretory granules.
References:  6,9
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling


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1. Futamura-Takahashi J, Tanaka T, Sugawara H, Iwashita S, Imajo S, Oyama Y, Muto T. (2018) Structure-based design, synthesis, and binding mode analysis of novel and potent chymase inhibitors. Bioorg Med Chem Lett, 28 (2): 188-192. [PMID:29191554]

2. Greco MN, Hawkins MJ, Powell ET, Almond Jr HR, de Garavilla L, Hall J, Minor LK, Wang Y, Corcoran TW, Di Cera E et al.. (2007) Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem, 50 (8): 1727-30. [PMID:17361995]

3. Heuston S, Hyland NP. (2012) Chymase inhibition as a pharmacological target: a role in inflammatory and functional gastrointestinal disorders?. Br J Pharmacol, 167 (4): 732-40. [PMID:22646261]

4. Liu WX, Wang Y, Sang LX, Zhang S, Wang T, Zhou F, Gu SZ. (2016) Chymase inhibitor TY-51469 in therapy of inflammatory bowel disease. World J Gastroenterol, 22 (5): 1826-33. [PMID:26855541]

5. Palaniyandi SS, Nagai Y, Watanabe K, Ma M, Veeraveedu PT, Prakash P, Kamal FA, Abe Y, Yamaguchi K, Tachikawa H et al.. (2007) Chymase inhibition reduces the progression to heart failure after autoimmune myocarditis in rats. Exp Biol Med (Maywood), 232 (9): 1213-21. [PMID:17895529]

6. Schwartz LB, Austen KF. (1980) Enzymes of the mast cell granule. J Invest Dermatol, 74 (5): 349-53. [PMID:6771334]

7. Takato H, Yasui M, Ichikawa Y, Waseda Y, Inuzuka K, Nishizawa Y, Tagami A, Fujimura M, Nakao S. (2011) The specific chymase inhibitor TY-51469 suppresses the accumulation of neutrophils in the lung and reduces silica-induced pulmonary fibrosis in mice. Exp Lung Res, 37 (2): 101-8. [PMID:21128860]

8. Tsunemi K, Takai S, Nishimoto M, Jin D, Sakaguchi M, Muramatsu M, Yuda A, Sasaki S, Miyazaki M. (2004) A specific chymase inhibitor, 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), suppresses development of abdominal aortic aneurysm in hamsters. J Pharmacol Exp Ther, 309 (3): 879-83. [PMID:14960660]

9. Welle M. (1997) Development, significance, and heterogeneity of mast cells with particular regard to the mast cell-specific proteases chymase and tryptase. J Leukoc Biol, 61 (3): 233-45. [PMID:9060446]

10. Yahiro E, Miura S, Imaizumi S, Uehara Y, Saku K. (2013) Chymase inhibitors. Curr Pharm Des, 19 (17): 3065-71. [PMID:23176221]

How to cite this page

S1: Chymotrypsin: chymase 1. Last modified on 15/02/2018. Accessed on 15/07/2024. IUPHAR/BPS Guide to PHARMACOLOGY,