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Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50303662
Substrate
n/a
Meas. Tech.
ChEMBL_618650 (CHEMBL1101699)
IC50
4.6±n/a nM
Citation
 Hategan, G; Polozov, AM; Zeller, W; Cao, H; Mishra, RK; Kiselyov, AS; Ramirez, J; Halldorsdottir, G; Andrésson, T; Gurney, ME; Singh, J Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists. Bioorg Med Chem Lett 19:6797-800 (2009) [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:
BDBM50303662
Synonyms:
3-(1-(2,4-dichlorobenzyl)-5-fluoro-3-methyl-1H-indol-7-yl)-N-(4,5-dichlorothiophen-2-ylsulfonyl)acrylamide | CHEMBL565591
Type:
Small organic molecule
Emp. Form.:
C23H15Cl4FN2O3S2
Mol. Mass.:
592.317
SMILES:
Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(\C=C\C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12
Structure:
Search PDB for entries with ligand similarity: