Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50066398 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_65654 (CHEMBL678074) |
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Ki | 0.43±n/a nM |
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Citation | Liu, G; Henry, KJ; Szczepankiewicz, BG; Winn, M; Kozmina, NS; Boyd, SA; Wasicak, J; von Geldern, TW; Wu-Wong, JR; Chiou, WJ; Dixon, DB; Nguyen, B; Marsh, KC; Opgenorth, TJ Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546). J Med Chem41:3261-75 (1998) [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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BDBM50066398 |
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n/a |
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Name | BDBM50066398 |
Synonyms: | 3-[2-(6-Methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-2-sulfonic acid (4-chloro-3-methyl-isoxazol-5-yl)-amide | CHEMBL326059 |
Type | Small organic molecule |
Emp. Form. | C18H15ClN2O6S2 |
Mol. Mass. | 454.905 |
SMILES | Cc1noc(NS(=O)(=O)c2sccc2C(=O)Cc2cc3OCOc3cc2C)c1Cl |
Structure |
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