Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50051012 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_65653 (CHEMBL678073) |
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Ki | 6.5±n/a nM |
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Citation | Winn, M; von Geldern, TW; Opgenorth, TJ; Jae, HS; Tasker, AS; Boyd, SA; Kester, JA; Mantei, RA; Bal, R; Sorensen, BK; Wu-Wong, JR; Chiou, WJ; Dixon, DB; Novosad, EI; Hernandez, L; Marsh, KC 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. J Med Chem39:1039-48 (1996) [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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BDBM50051012 |
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n/a |
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Name | BDBM50051012 |
Synonyms: | 4-tert-Butyl-N-[6-(3-hydroxy-propyl)-5-(2-methoxy-benzyl)-[2,2']bipyrimidinyl-4-yl]-benzenesulfonamide | CHEMBL428661 |
Type | Small organic molecule |
Emp. Form. | C29H33N5O4S |
Mol. Mass. | 547.668 |
SMILES | COc1ccccc1Cc1c(CCCO)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)-c1ncccn1 |
Structure |
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