Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50255781
Substrate
n/a
Meas. Tech.
ChEMBL_515713 (CHEMBL993101)
IC50
9.5±n/a nM
Citation
 O'Connell, MZeller, WBurgeson, JMishra, RKRamirez, JKiselyov, ASAndrésson, TGurney, MESingh, J Peri-substituted hexahydro-indolones as novel, potent and selective human EP3 receptor antagonists. Bioorg Med Chem Lett 19:778-82 (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:
BDBM50255781
Synonyms:
CHEMBL517369 | N-(4,5-dichlorothiophen-2-ylsulfonyl)-3-(1-(3-fluorobenzyl)-3a-methyl-2-oxo-2,3,3a,4,5,6-hexahydro-1H-indol-7-yl)acrylamide
Type:
Small organic molecule
Emp. Form.:
C23H21Cl2FN2O4S2
Mol. Mass.:
543.458
SMILES:
CC12CC(=O)N(Cc3cccc(F)c3)C1=C(CCC2)\C=C\C(=O)NS(=O)(=O)c1cc(Cl)c(Cl)s1 |c:16|
Structure:
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