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Target
Endothelin-1 receptor
Ligand
BDBM50143784
Substrate
n/a
Ki
0.03±n/a nM
Comments
PDSP_999
Citation
 Nishikibe, M; Ohta, H; Okada, M; Ishikawa, K; Hayama, T; Fukuroda, T; Noguchi, K; Saito, M; Kanoh, T; Ozaki, S; Kamei, T; Hara, K; William, D; Kivlighn, S; Krause, S; Gabel, R; Zingaro, G; Nolan, N; O'Brien, J; Clayton, F; Lynch, J; Pettibone, D; Siegl, P Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther 289:1262-70 (1999) [PubMed] 
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:
BDBM50143784
Synonyms:
(5S,6R,7R)-5-Benzo[1,3]dioxol-5-yl-2-butyl-7-[2-((S)-2-carboxy-propyl)-4-methoxy-phenyl]-6,7-dihydro-5H-[1]pyrindine-6-carboxylic acid | CHEMBL305576 | J-104132
Type:
Small organic molecule
Emp. Form.:
C31H33NO7
Mol. Mass.:
531.5962
SMILES:
CCCCc1ccc2[C@@H]([C@H]([C@@H](c2n1)c1ccc(OC)cc1C[C@H](C)C(O)=O)C(O)=O)c1ccc2OCOc2c1
Structure:
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