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TargetEndothelin-1 receptor
LigandBDBM50098777
Substrate/Competitorn/a
Meas. Tech.ChEMBL_63358 (CHEMBL679122)
IC50 0.04±n/a nM
Citation Wu, CDecker, ERBlok, NBui, HYou, TJWang, JBourgoyne, ARKnowles, VBerens, KLHolland, GWBrock, TADixon, 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 Chem47:1969-86 (2004) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Endothelin-1 receptor
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:
MGVLCFLASFWLALVGGAIADNAERYSANLSSHVEDFTPFPGTEFNFLGTTLQPPNLALP
SNGSMHGYCPQQTKITTAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLITAIEIVSIWILSFILAIPEAIGFVMVPFEYKGEQHRTCM
LNATTKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYDEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCHQSKSLMTSVPMNGTSIQWKNQEQNHNTERSS
HKDSMN
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  Blast E-value cutoff:
BDBM50098777
n/a
NameBDBM50098777
Synonyms:3-(4-Chloro-3-methyl-isoxazol-5-ylsulfamoyl)-thiophene-2-carboxylic acid (2-acetyl-4,6-dimethyl-phenyl)-amide | CHEMBL19950
TypeSmall organic molecule
Emp. Form.C19H18ClN3O5S2
Mol. Mass.467.946
SMILESCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
Structure
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