Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50117909 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_65473 (CHEMBL876873) |
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IC50 | 24±n/a nM |
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Citation | Murugesan, N; Tellew, JE; Gu, Z; Kunst, BL; Fadnis, L; Cornelius, LA; Baska, RA; Yang, Y; Beyer, SM; Monshizadegan, H; Dickinson, KE; Panchal, B; Valentine, MT; Chong, S; Morrison, RA; Carlson, KE; Powell, JR; Moreland, S; Barrish, JC; Kowala, MC; Macor, JE Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. J Med Chem45:3829-35 (2002) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Endothelin-1 receptor |
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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: | METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM
LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS
SHKDSMN
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BDBM50117909 |
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n/a |
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Name | BDBM50117909 |
Synonyms: | CHEMBL278176 | N-{2-Benzo[1,3]dioxol-5-yl-2-[4-(2-ethyl-5,7-dimethyl-imidazo[4,5-b]pyridin-3-ylmethyl)-2-propyl-phenoxy]-acetyl}-4-isopropyl-benzenesulfonamide |
Type | Small organic molecule |
Emp. Form. | C38H42N4O6S |
Mol. Mass. | 682.828 |
SMILES | CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc23)ccc1OC(C(=O)NS(=O)(=O)c1ccc(cc1)C(C)C)c1ccc2OCOc2c1 |
Structure |
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