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TargetProstaglandin E2 receptor
LigandBDBM50303696
Substrate/Competitorn/a
Meas. Tech.ChEMBL_596837
IC50 14.2±n/a nM
Citation Singh JZeller WZhou NHategan GMishra RKPolozov AYu POnua EZhang JRamírez JLSigthorsson GThorsteinnsdottir MKiselyov ASZembower DEAndrésson TGurney ME Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that J Med Chem 53:18-36 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Prostaglandin E2 receptor
Name:Prostaglandin E2 receptor
Synonyms:PGE receptor, EP3 subtype | PGE2-R | Prostaglandin E2 receptor EP3 subtype | Prostaglandin E2 receptor EP3 subtype (EP3) | Prostaglandin E2 receptor EP3A subtype (EP3A) | Prostaglandin E2 receptor EP3D subtype (EP3D) | Prostanoid EP3 receptor
Type:Enzyme
Mol. Mass.:43335.03
Organism:Homo sapiens (Human)
Description:P43115
Residue:390
Sequence:
MKETRGYGGDAPFCTRLNHSYTGMWAPERSAEARGNLTRPPGSGEDCGSVSVAFPITMLL
TGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTTPVVIVVYLSKQRW
EHIDPSGRLCTFFGLTMTVFGLSSLFIASAMAVERALAIRAPHWYASHMKTRATRAVLLG
VWLAVLAFALLPVLGVGQYTVQWPGTWCFISTGRGGNGTSSSHNWGNLFFASAFAFLGLL
ALTVTFSCNLATIKALVSRCRAKATASQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLI
MMLKMIFNQTSVEHCKTHTEKQKECNFFLIAVRLASLNQILDPWVYLLLRKILLRKFCQI
RYHTNNYASSSTSLPCQCSSTLMWSDHLER
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  Blast E-value cutoff:
BDBM50303696
n/a
NameBDBM50303696
Synonyms:CHEMBL565597 | Thiophene-2-sulfonic Acid{(E)-3-[1-(3,4-Dichlorobenzyl)-3-methyl-1H-indol-7-yl]acryloyl}amide
TypeSmall organic molecule
Emp. Form.C23H18Cl2N2O3S2
Mol. Mass.505.437
SMILESCc1cn(Cc2ccc(Cl)c(Cl)c2)c2c(\C=C\C(=O)NS(=O)(=O)c3cccs3)cccc12
Structure
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