Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50303674
Substrate
n/a
Meas. Tech.
ChEMBL_596837 (CHEMBL1042648)
IC50
8.9±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 
Target
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:
MKETRGYGGDAPFCTRLNHSYTGMWAPERSAEARGNLTRPPGSGEDCGSVSVAFPITMLLTGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTTPVVIVVYLSKQRWEHIDPSGRLCTFFGLTMTVFGLSSLFIASAMAVERALAIRAPHWYASHMKTRATRAVLLGVWLAVLAFALLPVLGVGQYTVQWPGTWCFISTGRGGNGTSSSHNWGNLFFASAFAFLGLLALTVTFSCNLATIKALVSRCRAKATASQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLIMMLKMIFNQTSVEHCKTHTEKQKECNFFLIAVRLASLNQILDPWVYLLLRKILLRKFCQIRYHTNNYASSSTSLPCQCSSTLMWSDHLER
  
Inhibitor
Name:
BDBM50303674
Synonyms:
4,5-Dichloro-thiophene-2-sulfonic acid{2-[3-(naphthalene-2-sulfonyl)-benzofuran-4-yloxy]-acetyl}-amide | CHEMBL567051
Type:
Small organic molecule
Emp. Form.:
C24H15Cl2NO7S3
Mol. Mass.:
596.479
SMILES:
Clc1cc(sc1Cl)S(=O)(=O)NC(=O)COc1cccc2occ(c12)S(=O)(=O)c1ccc2ccccc2c1
Structure:
Search PDB for entries with ligand similarity: