LY3023703 [Ligand Id: 12211] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3342693
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.38 pKi 41300 nM Ki J Med Chem (2016) 59: 194-205 [PMID:26653180]
ChEMBL Inhibition of human ERG B 4.08 pIC50 82600 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of mPGES-1 in human A549 cells assessed as PEG2 formation preincubated for 30 mins followed by recombinant human interleukin 1beta addition measured after 18 hrs by LC/MS analysis B 7.92 pIC50 12 nM IC50 J Med Chem (2016) 59: 5970-5986 [PMID:26791385]
ChEMBL Inhibition of mPGES-1 in human A549 cells assessed as inhibition of IL-1beta-induced PGE2 production incubated for 30 mins prior to IL-1beta challenge measured after 18 hrs by plate reader analysis B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492]
ChEMBL Inhibition of mPGES-1 in human whole blood assessed as inhibition of LPS-induced PGE2 production incubated for 30 mins prior to LPS challenge measured after 20 to 24 hrs by LC/MS/MS analysis B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492]
ChEMBL Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis B 7.92 pIC50 12 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
ChEMBL Inhibition of mPGES-1 in human whole blood cells assessed as PEG2 formation by LC/MS analysis B 7.92 pIC50 12 nM IC50 J Med Chem (2016) 59: 5970-5986 [PMID:26791385]
ChEMBL Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method B 7.92 pIC50 12 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
ChEMBL Inhibition of human mPGES-1 expressed in 293E cell microsomes using PGH2 substrate by LC/MS analysis1 B 9.03 pIC50 0.94 nM IC50 Bioorg Med Chem Lett (2014) 24: 4838-4844 [PMID:25260492]
GtoPdb Potency for inhibition of human mPGES-1 expressed in 293E cell microsomes - 9.03 pIC50 0.94 nM IC50 Bioorg Med Chem Lett (2014) 24: 4838-44 [PMID:25260492]
ChEMBL Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis B 9.05 pIC50 0.9 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
Prostaglandin E synthase in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3341581] [UniProtKB: A0SYQ0]
ChEMBL Inhibition of mPGES1 in LPS-induced dog whole blood assessed as suppression of PGE2 response pre-incubated for 30 mins followed by LPS addition and measured after 5 hrs by LC-MS/MS analysis B 6.86 pIC50 139 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]

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]