Target
Chymase
Ligand
BDBM50208243
Substrate
n/a
Meas. Tech.
ChEMBL_429291 (CHEMBL915852)
IC50
11±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:
BDBM50208243
Synonyms:
(E)-2-(3,4-difluorostyrylamino)-1-(5-chlorobenzo[b]thiophen-3-yl)-2-oxoethylphosphonic acid | CHEMBL373898
Type:
Small organic molecule
Emp. Form.:
C18H13ClF2NO4PS
Mol. Mass.:
443.789
SMILES:
OP(O)(=O)C(C(=O)NC=Cc1ccc(F)c(F)c1)c1csc2ccc(Cl)cc12 |w:9.9|
Structure:
Search PDB for entries with ligand similarity: