Reaction Details |
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Target | Prostaglandin E2 receptor EP3 subtype |
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Ligand | BDBM50303668 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_596837 (CHEMBL1042648) |
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IC50 | 14±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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BDBM50303668 |
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n/a |
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Name | BDBM50303668 |
Synonyms: | CHEMBL566631 | Thiophene-2-sulfonic Acid[(E)-3-(5-Fluoro-3-methyl-1-naphthalen-2-ylmethyl-1H-indol-7-yl)acryloyl]amide |
Type | Small organic molecule |
Emp. Form. | C27H21FN2O3S2 |
Mol. Mass. | 504.596 |
SMILES | Cc1cn(Cc2ccc3ccccc3c2)c2c(\C=C\C(=O)NS(=O)(=O)c3cccs3)cc(F)cc12 |
Structure |
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