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 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]