Target
Chymase
Ligand
BDBM50208229
Substrate
n/a
Meas. Tech.
ChEMBL_429291 (CHEMBL915852)
IC50
21±n/a nM
Citation
 Greco, MNHawkins, MJPowell, ETAlmond, HRde Garavilla, LHall, JMinor, LKWang, YCorcoran, TWDi Cera, ECantwell, AMSavvides, SNDamiano, BPMaryanoff, BE Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem 50:1727-30 (2007) [PubMed]  Article 
Target
Name:
Chymase
Synonyms:
Alpha-chymase | CMA1 | CMA1_HUMAN | CYH | CYM | Chymase precursor | Mast cell protease I
Type:
Enzyme
Mol. Mass.:
27340.12
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
247
Sequence:
MLLLPLPLLLFLLCSRAEAGEIIGGTECKPHSRPYMAYLEIVTSNGPSKFCGGFLIRRNFVLTAAHCAGRSITVTLGAHNITEEEDTWQKLEVIKQFRHPKYNTSTLHHDIMLLKLKEKASLTLAVGTLPFPSQFNFVPPGRMCRVAGWGRTGVLKPGSDTLQEVKLRLMDPQACSHFRDFDHNLQLCVGNPRKTKSAFKGDSGGPLLCAGVAQGIVSYGRSDAKPPAVFTRISHYRPWINQILQAN
  
Inhibitor
Name:
BDBM50208229
Synonyms:
(E)-2-(3,4-difluorostyrylamino)-1-(5-chloro-1-methyl-1H-indol-3-yl)-2-oxoethyl(methyl)phosphinic acid | CHEMBL376054
Type:
Small organic molecule
Emp. Form.:
C20H18ClF2N2O3P
Mol. Mass.:
438.792
SMILES:
Cn1cc(C(C(=O)NC=Cc2ccc(F)c(F)c2)P(C)(O)=O)c2cc(Cl)ccc12 |w:9.9|
Structure:
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