Reaction Details |
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Target | Endothelin-1 receptor |
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Ligand | BDBM50029352 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_65498 (CHEMBL682971) |
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IC50 | 8.3±n/a nM |
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Citation | Fukami, T; Nagase, T; Fujita, K; Hayama, T; Niiyama, K; Mase, T; Nakajima, S; Fukuroda, T; Saeki, T; Nishikibe, M Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. J Med Chem38:4309-24 (1995) [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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BDBM50029352 |
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n/a |
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Name | BDBM50029352 |
Synonyms: | CHEMBL336033 | [(5S,8S,11R,14S,16aR)-8-(1H-Indol-3-ylmethyl)-11-isobutyl-14-isopropyl-4,7,10,13,16-pentaoxo-hexadecahydro-3a,6,9,12,15-pentaaza-cyclopentacyclopentadecen-5-yl]-acetic acid |
Type | Small organic molecule |
Emp. Form. | C31H42N6O7 |
Mol. Mass. | 610.7012 |
SMILES | CC(C)C[C@H]1NC(=O)[C@@H](NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O)C(C)C |
Structure |
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