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Target
Endothelin-1 receptor
Ligand
BDBM50034435
Substrate
n/a
Meas. Tech.
ChEMBL_65824 (CHEMBL682958)
Ki
55±n/a nM
Citation
Stein, PD; Hunt, JT; Floyd, DM; Moreland, S; Dickinson, KE; Mitchell, C; Liu, EC; Webb, ML; Murugesan, N; Dickey, 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
More Info.:
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