Reaction Details |
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Target | Prostaglandin E2 receptor EP3 subtype |
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Ligand | BDBM50303670 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_596837 (CHEMBL1042648) |
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IC50 | 4.9±n/a nM |
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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 Chem53:18-36 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Prostaglandin E2 receptor EP3 subtype |
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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: | MKETRGYGGDAPFCTRLNHSYTGMWAPERSAEARGNLTRPPGSGEDCGSVSVAFPITMLL
TGFVGNALAMLLVSRSYRRRESKRKKSFLLCIGWLALTDLVGQLLTTPVVIVVYLSKQRW
EHIDPSGRLCTFFGLTMTVFGLSSLFIASAMAVERALAIRAPHWYASHMKTRATRAVLLG
VWLAVLAFALLPVLGVGQYTVQWPGTWCFISTGRGGNGTSSSHNWGNLFFASAFAFLGLL
ALTVTFSCNLATIKALVSRCRAKATASQSSAQWGRITTETAIQLMGIMCVLSVCWSPLLI
MMLKMIFNQTSVEHCKTHTEKQKECNFFLIAVRLASLNQILDPWVYLLLRKILLRKFCQI
RYHTNNYASSSTSLPCQCSSTLMWSDHLER
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BDBM50303670 |
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n/a |
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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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