Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50068737 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_63207 (CHEMBL676575) |
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Ki | 8800±n/a nM |
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Citation | Murugesan, N; Gu, Z; Stein, PD; Bisaha, S; Spergel, S; Girotra, R; Lee, VG; Lloyd, J; Misra, RN; Schmidt, J; Mathur, A; Stratton, L; Kelly, YF; Bird, E; Waldron, T; Liu, EC; Zhang, R; Lee, H; Serafino, R; Abboa-Offei, B; Mathers, P; Giancarli, M; Seymour, AA; Webb, ML; Hunt, JT Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308). J Med Chem41:5198-218 (1999) [PubMed] Article |
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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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BDBM50068737 |
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n/a |
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Name | BDBM50068737 |
Synonyms: | CHEMBL357678 | N-(3,4-Dimethyl-isoxazol-5-yl)-2-pyrimidin-2-yl-benzenesulfonamide |
Type | Small organic molecule |
Emp. Form. | C15H14N4O3S |
Mol. Mass. | 330.362 |
SMILES | Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C |
Structure |
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