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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]