Target
Chymase
Ligand
BDBM50208235
Substrate
n/a
Meas. Tech.
ChEMBL_429291 (CHEMBL915852)
IC50
165±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:
BDBM50208235
Synonyms:
(E)-2-(3,4-difluorostyrylamino)-1-(5-chlorobenzo[b]thiophen-3-yl)-2-oxoethyl(ethyl)phosphinic acid | CHEMBL223183
Type:
Small organic molecule
Emp. Form.:
C20H17ClF2NO3PS
Mol. Mass.:
455.842
SMILES:
CCP(O)(=O)C(C(=O)NC=Cc1ccc(F)c(F)c1)c1csc2ccc(Cl)cc12 |w:10.10|
Structure:
Search PDB for entries with ligand similarity: