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TargetEndothelin-1 receptor
LigandBDBM50122680
Substrate/Competitorn/a
Meas. Tech.ChEMBL_65652
Ki 0.3±n/a nM
Citation Murugesan NGu ZSpergel SYoung MChen PMathur ALeith LHermsmeier MLiu ECZhang RBird EWaldron TMarino AKoplowitz BHumphreys WGChong SMorrison RAWebb MLMoreland STrippodo NBarrish JC Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. J Med Chem 46:125-37 (2002) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Endothelin-1 receptor
Name:Endothelin-1 receptor
Synonyms:EDNRA | ET-A | ETA | ETA-R | ETRA | Endothelin receptor type A | 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:
BDBM50122680
n/a
NameBDBM50122680
Synonyms:4'-Oxazol-2-yl-2'-pyrazol-1-ylmethyl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | CHEMBL30092
TypeSmall organic molecule
Emp. Form.C24H21N5O4S
Mol. Mass.475.52
SMILESCc1noc(NS(=O)(=O)c2ccccc2-c2ccc(cc2Cn2cccn2)-c2ncco2)c1C
Structure
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