Reaction Details Report a problem with these data
Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50254473
Substrate
n/a
Meas. Tech.
ChEMBL_596851 (CHEMBL1045310)
IC50
4±n/a nM
Citation
 Singh, J; Zeller, W; Zhou, N; Hategan, G; Mishra, RK; Polozov, A; Yu, P; Onua, E; Zhang, J; Ramírez, JL; Sigthorsson, G; Thorsteinnsdottir, M; Kiselyov, AS; Zembower, DE; Andrésson, T; Gurney, 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 
Target
Name:
Prostaglandin E2 receptor EP3 subtype
Synonyms:
PE2R3_MOUSE | PGE receptor, EP3 isoform alpha | Prostaglandin E2 receptor EP3 isoform alpha | Prostaglandin E3 | Prostanoid EP3 receptor | Ptger3 | Ptgerep3
Type:
G-protein coupled receptor
Mol. Mass.:
40092.50
Organism:
Mus musculus (Mouse)
Description:
n/a
Residue:
365
Sequence:
MASMWAPEHSAEAHSNLSSTTDDCGSVSVAFPITMMVTGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTSPVVILVYLSQRRWEQLDPSGRLCTFFGLTMTVFGLSSLLVASAMAVERALAIRAPHWYASHMKTRATPVLLGVWLSVLAFALLPVLGVGRYSVQWPGTWCFISTGPAGNETDPAREPGSVAFASAFACLGLLALVVTFACNLATIKALVSRCRAKAAVSQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLIMMLKMIFNQMSVEQCKTQMGKEKECNSFLIAVRLASLNQILDPWVYLLLRKILLRKFCQIRDHTNYASSSTSLPCPGSSALMWSDQLER
  
Inhibitor
Name:
BDBM50254473
Synonyms:
4,5-Dichlorothiophene-2-sulfonic Acid[2-(3-Naphthalen-2-ylmethyl-1H-indol-4-yloxy)acetyl]amide | CHEMBL467632 | N-(4,5-dichlorothiophen-2-ylsulfonyl)-2-(3-(naphthalen-2-ylmethyl)-1H-indol-4-yloxy)acetamide
Type:
Small organic molecule
Emp. Form.:
C25H18Cl2N2O4S2
Mol. Mass.:
545.457
SMILES:
Clc1cc(sc1Cl)S(=O)(=O)NC(=O)COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12
Structure:
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