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Target
Endothelin-1 receptor
Ligand
BDBM50068737
Substrate
n/a
Meas. Tech.
ChEMBL_63207 (CHEMBL676575)
Ki
8800±n/a nM
Citation
 Murugesan, N; Gu, Z; Stein, PD; Bisaha, S; Spergel, S; Girotra, R; Lee, VG; Lloyd, J; Misra, RN; Schmidt, J; Mathur, A; Stratton, L; Kelly, YF; Bird, E; Waldron, T; Liu, EC; Zhang, R; Lee, H; Serafino, R; Abboa-Offei, B; Mathers, P; Giancarli, M; Seymour, AA; Webb, ML; Hunt, JT Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308). J Med Chem 41:5198-218 (1999) [PubMed]  Article 
Target
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:
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN
  
Inhibitor
Name:
BDBM50068737
Synonyms:
CHEMBL357678 | N-(3,4-Dimethyl-isoxazol-5-yl)-2-pyrimidin-2-yl-benzenesulfonamide
Type:
Small organic molecule
Emp. Form.:
C15H14N4O3S
Mol. Mass.:
330.362
SMILES:
Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C
Structure:
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