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Target
Endothelin-1 receptor
Ligand
BDBM50143790
Substrate
n/a
Meas. Tech.
ChEMBL_63358 (CHEMBL679122)
IC50
0.14±n/a nM
Citation
 Wu, C; Decker, ER; Blok, N; Bui, H; You, TJ; Wang, J; Bourgoyne, AR; Knowles, V; Berens, KL; Holland, GW; Brock, TA; Dixon, RA Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem 47:1969-86 (2004) [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:
BDBM50143790
Synonyms:
3-(4-Chloro-3-methyl-isoxazol-5-ylsulfamoyl)-thiophene-2-carboxylic acid (2-carbamoyl-4,6-dimethyl-phenyl)-amide | CHEMBL60276
Type:
Small organic molecule
Emp. Form.:
C18H17ClN4O5S2
Mol. Mass.:
468.934
SMILES:
Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2c(C)cc(C)cc2C(N)=O)c1Cl
Structure:
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