Target
Endothelin-1 receptor
Ligand
BDBM50068692
Substrate
n/a
Meas. Tech.
ChEMBL_63369 (CHEMBL676105)
Ki
100±n/a nM
Citation
 Murugesan, NGu, ZStein, PDBisaha, SSpergel, SGirotra, RLee, VGLloyd, JMisra, RNSchmidt, JMathur, AStratton, LKelly, YFBird, EWaldron, TLiu, ECZhang, RLee, HSerafino, RAbboa-Offei, BMathers, PGiancarli, MSeymour, AAWebb, MLHunt, 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_RAT | ENDOTHELIN A | Ednra | Endothelin receptor | Endothelin-1 receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
48256.91
Organism:
RAT
Description:
ENDOTHELIN A EDNRA RAT::P26684
Residue:
426
Sequence:
MGVLCFLASFWLALVGGAIADNAERYSANLSSHVEDFTPFPGTEFNFLGTTLQPPNLALPSNGSMHGYCPQQTKITTAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLITAIEIVSIWILSFILAIPEAIGFVMVPFEYKGEQHRTCMLNATTKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYDEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCHQSKSLMTSVPMNGTSIQWKNQEQNHNTERSSHKDSMN
  
Inhibitor
Name:
BDBM50068692
Synonyms:
2'-(3,4-Dimethyl-isoxazol-5-ylsulfamoyl)-4-isobutyl-biphenyl-2-carboxylic acid amide | CHEMBL146904
Type:
Small organic molecule
Emp. Form.:
C22H25N3O4S
Mol. Mass.:
427.517
SMILES:
CC(C)Cc1ccc(c(c1)C(N)=O)-c1ccccc1S(=O)(=O)Nc1onc(C)c1C
Structure:
Search PDB for entries with ligand similarity: