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Target
Prostaglandin E2 receptor EP3 subtype
Ligand
BDBM50303670
Substrate
n/a
Meas. Tech.
ChEMBL_596837 (CHEMBL1042648)
IC50
4.9±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_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:
BDBM50303670
Synonyms:
(2E)-3-[1-(2,4-dichlorobenzyl)-2-oxo-1,2-dihydrospiro[indole-3,2'-[1,3]thiazolidin]-7-yl]-N-[(4,5-dichlorothiophen-2-yl)sulfonyl]prop-2-enamide | 3-(1-(2,4-dichlorobenzyl)-2-oxospiro[indoline-3,2'-thiazolidine]-7-yl)-N-(4,5-dichlorothiophen-2-ylsulfonyl)acrylamide | CHEMBL585507
Type:
Small organic molecule
Emp. Form.:
C24H17Cl4N3O4S3
Mol. Mass.:
649.416
SMILES:
Clc1cc(sc1Cl)S(=O)(=O)NC(=O)\C=C\c1cccc2c1N(Cc1ccc(Cl)cc1Cl)C(=O)C21NCCS1
Structure:
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