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Target
Endothelin-1 receptor
Ligand
BDBM50146648
Substrate
n/a
Meas. Tech.
ChEMBL_65482 (CHEMBL682357)
IC50
6.6±n/a nM
Citation
 Bolli, MH; Marfurt, J; Grisostomi, C; Boss, C; Binkert, C; Hess, P; Treiber, A; Thorin, E; Morrison, K; Buchmann, S; Bur, D; Ramuz, H; Clozel, M; Fischli, W; Weller, T Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists. J Med Chem 47:2776-95 (2004) [PubMed]  Article 
Target
Name:
Endothelin-1 receptor
Synonyms:
EDNRA | EDNRA_HUMAN | ET-A | ETA | ETA-R | ETRA | Endothelin receptor type A | Endothelin receptor, ET-A/ET-B | hET-AR
Type:
Enzyme Catalytic Domain
Mol. Mass.:
48736.88
Organism:
Homo sapiens (Human)
Description:
P25101
Residue:
427
Sequence:
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN
  
Inhibitor
Name:
BDBM50146648
Synonyms:
(S)-(4,6-Dimethyl-pyrimidin-2-yloxy)-[(S)-2-oxo-5-phenyl-1-(2H-tetrazol-5-ylmethyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-5-yl]-acetic acid | CHEMBL94964
Type:
Small organic molecule
Emp. Form.:
C25H24N8O4
Mol. Mass.:
500.5093
SMILES:
Cc1cc(C)nc(O[C@H](C(O)=O)[C@]2(NCC(=O)N(Cc3nnn[nH]3)c3ccccc23)c2ccccc2)n1
Structure:
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