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TargetProstaglandin E2 receptor EP3 subtype
LigandBDBM50303662
Substrate/Competitorn/a
Meas. Tech.ChEMBL_596846 (CHEMBL1042657)
IC50 4.6±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 Chem53:18-36 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Prostaglandin E2 receptor EP3 subtype
Name:Prostaglandin E2 receptor EP3 subtype
Synonyms:PE2R3_HUMAN | PGE receptor, EP3 subtype | PGE2-R | PTGER3 | Prostaglandin E2 receptor | 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:
BDBM50303662
n/a
NameBDBM50303662
Synonyms:3-(1-(2,4-dichlorobenzyl)-5-fluoro-3-methyl-1H-indol-7-yl)-N-(4,5-dichlorothiophen-2-ylsulfonyl)acrylamide | CHEMBL565591
TypeSmall organic molecule
Emp. Form.C23H15Cl4FN2O3S2
Mol. Mass.592.317
SMILESCc1cn(Cc2ccc(Cl)cc2Cl)c2c(\C=C\C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12
Structure
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