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Target
Endothelin-1 receptor
Ligand
BDBM50125341
Substrate
n/a
Meas. Tech.
ChEBML_65644
Ki
105±n/a nM
Citation
 Tellew, JE; Baska, RA; Beyer, SM; Carlson, KE; Cornelius, LA; Fadnis, L; Gu, Z; Kunst, BL; Kowala, MC; Monshizadegan, H; Murugesan, N; Ryan, CS; Valentine, MT; Yang, Y; Macor, JE Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists. Bioorg Med Chem Lett 13:1093-6 (2003) [PubMed]
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:
BDBM50125341
Synonyms:
4'-(8-Oxo-2-propyl-5,6,7,8-tetrahydro-4H-cycloheptaimidazol-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | CHEMBL12779
Type:
Small organic molecule
Emp. Form.:
C29H32N4O4S
Mol. Mass.:
532.654
SMILES:
CCCc1nc2CCCCC(=O)c2n1Cc1ccc(cc1)-c1ccccc1S(=O)(=O)Nc1onc(C)c1C
Structure:
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