Target
Endothelin-1 receptor
Ligand
BDBM50034440
Substrate
n/a
Meas. Tech.
ChEMBL_65826 (CHEMBL877809)
IC50
27000±n/a nM
Citation
 Stein, PDHunt, JTFloyd, DMMoreland, SDickinson, KEMitchell, CLiu, ECWebb, MLMurugesan, NDickey, J The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide. J Med Chem 37:329-31 (1994) [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:
BDBM50034440
Synonyms:
CHEMBL286682 | N-(3,4-Dimethyl-isoxazol-5-yl)-4-propylamino-benzenesulfonamide
Type:
Small organic molecule
Emp. Form.:
C14H19N3O3S
Mol. Mass.:
309.384
SMILES:
CCCNc1ccc(cc1)S(=O)(=O)Nc1onc(C)c1C
Structure:
Search PDB for entries with ligand similarity: