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TargetEndothelin-1 receptor
LigandBDBM50051012
Substrate/Competitorn/a
Meas. Tech.ChEMBL_65653 (CHEMBL678073)
Ki 6.5±n/a nM
Citation Winn, Mvon Geldern, TWOpgenorth, TJJae, HSTasker, ASBoyd, SAKester, JAMantei, RABal, RSorensen, BKWu-Wong, JRChiou, WJDixon, DBNovosad, EIHernandez, LMarsh, 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
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50051012
n/a
NameBDBM50051012
Synonyms:4-tert-Butyl-N-[6-(3-hydroxy-propyl)-5-(2-methoxy-benzyl)-[2,2']bipyrimidinyl-4-yl]-benzenesulfonamide | CHEMBL428661
TypeSmall organic molecule
Emp. Form.C29H33N5O4S
Mol. Mass.547.668
SMILESCOc1ccccc1Cc1c(CCCO)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)-c1ncccn1
Structure
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