Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50117911 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_65647 (CHEMBL678559) |
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Ki | 39±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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BDBM50117911 |
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n/a |
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Name | BDBM50117911 |
Synonyms: | 4'-(2-Butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | CHEMBL126755 |
Type | Small organic molecule |
Emp. Form. | C29H34N4O4S |
Mol. Mass. | 534.67 |
SMILES | CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(cc1)-c1ccccc1S(=O)(=O)Nc1onc(C)c1C |t:4| |
Structure |
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