DG-041 [Ligand Id: 5822] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL565591 (DG-041)
  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Displacement of [3H]PGE2 from human EP1 receptor after 1 hr by liquid scintillation counting B 4.7 pIC50 >20000 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting B 5.38 pIC50 4169 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
GtoPdb - - 8.41 pKi 3.9 nM Ki Br J Pharmacol (2009) 158: 372-81 [PMID:19486006]
GtoPdb - - 9.52 pKi 0.3 nM Ki Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
GtoPdb - - 9.92 pKi 0.12 nM Ki Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
GtoPdb - - 10.1 pKi 0.08 nM Ki Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum B 8.22 pIC50 6 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting B 8.34 pIC50 4.6 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting B 8.34 pIC50 4.6 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor B 8.34 pIC50 4.6 nM IC50 Bioorg Med Chem Lett (2009) 19: 6797-6800 [PMID:19836233]
EP3 receptor/Prostanoid EP3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
ChEMBL Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting B 7.96 pIC50 11 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation counting B 5.09 pIC50 8039 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting B 4.84 pIC50 14414 nM IC50 J Med Chem (2010) 53: 18-36 [PMID:19957930]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]