Target
Endothelin-1 receptor
Ligand
BDBM50034435
Substrate
n/a
Meas. Tech.
ChEMBL_65654 (CHEMBL678074)
Ki
48±n/a nM
Citation
 Liu, GHenry, KJSzczepankiewicz, BGWinn, MKozmina, NSBoyd, SAWasicak, Jvon Geldern, TWWu-Wong, JRChiou, WJDixon, DBNguyen, BMarsh, KCOpgenorth, TJ Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546). J Med Chem 41:3261-75 (1998) [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:
BDBM50034435
Synonyms:
5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-2,3-dihydro-oxazol-5-yl)-amide | 5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | 5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide (BMS 182874) | BMS-182874 | CHEMBL267458
Type:
Small organic molecule
Emp. Form.:
C17H19N3O3S
Mol. Mass.:
345.416
SMILES:
CN(C)c1cccc2c(cccc12)S(=O)(=O)Nc1onc(C)c1C
Structure:
Search PDB for entries with ligand similarity: