Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50315506
Substrate
n/a
Meas. Tech.
ChEMBL_626787 (CHEMBL1107234)
IC50
0.4±n/a nM
Citation
 Zhou, NPolozov, AMO'Connell, MBurgeson, JYu, PZeller, WZhang, JOnua, ERamirez, JPalsdottir, GAHalldorsdottir, GVAndresson, TKiselyov, ASGurney, MSingh, J 1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists. Bioorg Med Chem Lett 20:2658-64 (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:
BDBM50315506
Synonyms:
CHEMBL1091146 | N-(4,5-dichlorothiophen-2-ylsulfonyl)-3-(1-(3,4-difluorobenzyl)-2-oxoindolin-7-yl)acrylamide
Type:
Small organic molecule
Emp. Form.:
C22H14Cl2F2N2O4S2
Mol. Mass.:
543.39
SMILES:
Fc1ccc(CN2C(=O)Cc3cccc(\C=C\C(=O)NS(=O)(=O)c4cc(Cl)c(Cl)s4)c23)cc1F
Structure:
Search PDB for entries with ligand similarity: