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TargetEndothelin-1 receptor
LigandBDBM50395624
Substrate/Competitorn/a
Meas. Tech.ChEMBL_859881 (CHEMBL2166382)
IC50 4.4±n/a nM
Citation Bolli, MHBoss, CBinkert, CBuchmann, SBur, DHess, PIglarz, MMeyer, SRein, JRey, MTreiber, AClozel, MFischli, WWeller, T The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem55:7849-61 (2012) [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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BDBM50395624
n/a
NameBDBM50395624
Synonyms:CHEMBL2165340
TypeSmall organic molecule
Emp. Form.C19H18Br2N6O4S
Mol. Mass.586.257
SMILESBrc1ccc(cc1)-c1c(NS(=O)(=O)NC2CC2)ncnc1OCCOc1ncc(Br)cn1
Structure
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