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TargetEndothelin-1 receptor
LigandBDBM50066370
Substrate/Competitorn/a
Meas. Tech.ChEMBL_65654 (CHEMBL678074)
Ki 0.13±n/a nM
Citation Liu, GHenry, KJSzczepankiewicz, BGWinn, MKozmina, NSBoyd, SAWasicak, Jvon Geldern, TWWu-Wong, JRChiou, WJDixon, DBNguyen, BMarsh, KCOpgenorth, 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
More Info.:Get all data from this article,  Assay Method
 
Endothelin-1 receptor
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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  Blast E-value cutoff:
BDBM50066370
n/a
NameBDBM50066370
Synonyms:5-Methyl-pyridine-2-sulfonic acid {6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-[2-(2H-tetrazol-5-yl)-pyridin-4-yl]-pyrimidin-4-yl}-amide | CHEMBL109648 | clazosentan
TypeSmall organic molecule
Emp. Form.C25H23N9O6S
Mol. Mass.577.572
SMILESCOc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(nc1OCCO)-c1ccnc(c1)-c1nnn[nH]1
Structure
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