darapladib [Ligand Id: 6696] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL204021 (Darapladib, SB-480848)
  • PLA2-G7/LDL-associated phospholipase A2 in Human [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
  • This target only has 1 pki data point
  • 9.96
1 CHEMBL204021_lig_chart_1 LDL-associated phospholipase A2 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
PLA2-G7/LDL-associated phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
ChEMBL Binding affinity to human Lp-PLA2 by ITC assay B 7.3 pKd 49.7 nM Kd J. Med. Chem. (2016) 59: 5115-5120 [PMID:27078579]
ChEMBL Inhibitory activity against recombinant human Lp-PLA2 by mechanistic studies B 9.96 pKi 0.11 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 1067-1070 [PMID:12643913]
ChEMBL Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mins by CPM-based fluorescence assay B 7.46 pIC50 35 nM IC50 J. Med. Chem. (2016) 59: 5356-5367 [PMID:27167608]
GtoPdb In an assay using whole human plasma and recombinant hPLA2-G7, that approximates the physiological environment of the enzyme. - 7.46 pIC50 35 nM IC50 J Med Chem (2016) 59: 10738-10749 [PMID:27933945]
ChEMBL Inhibitory activity against Lp-PLA2 in whole human plasma B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1067-1070 [PMID:12643913]
ChEMBL Inhibition of recombinant human Lp-PLA2 using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis B 9.15 pIC50 0.7 nM IC50 J. Med. Chem. (2016) 59: 2674-2687 [PMID:26927682]
ChEMBL Inhibition of recombinant human Lp-PLA2 using 2-thio-PAF substrate after 10 mins B 9.15 pIC50 0.7 nM IC50 J. Med. Chem. (2015) 58: 8529-8541 [PMID:26479945]
ChEMBL Inhibition of human recombinant GST-tagged Lp-PLA2 (47 to 429 residues) expressed in Escherichia coli Rosetta(DE3) pLysS using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay B 9.22 pIC50 0.6 nM IC50 J Med Chem (2017) 60: 10231-10244 [PMID:29193967]
ChEMBL Inhibition of human Lp-PLA2 B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem Lett (2018) 28: 787-792 [PMID:29336874]
ChEMBL Inhibition of Lp-PLA2 (unknown origin) B 9.6 pIC50 0.25 nM IC50 J. Med. Chem. (2015) 58: 8529-8541 [PMID:26479945]
ChEMBL Inhibitory activity against recombinant human Lp-PLA2 B 9.6 pIC50 0.25 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1067-1070 [PMID:12643913]
GtoPdb - - 9.96 pIC50 0.11 nM IC50 Bioorg Med Chem Lett (2003) 13: 1067-70 [PMID:12643913]
ChEMBL Inhibition of recombinant human Lp-PLA2 using [3H]PAF as substrate at 10 nM incubated for 5 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis B 10 pIC50 0.1 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 2897-2901 [PMID:23575276]
ChEMBL Inhibition of Lp-PLA2 in human plasma LDL fractions using 2-thio platelet-activating factor as substrate by TMB dye based spectrophotometry B 10 pIC50 <0.1 nM IC50 Bioorg Med Chem Lett (2018) 28: 787-792 [PMID:29336874]
ChEMBL Inhibition of human recombinant LpPLA2 B 10.2 pIC50 0.06 nM IC50 ACS Med Chem Lett (2017) 8: 43-48 [PMID:28105273]
ChEMBL Inhibition of recombinant human Lp-PLA2 incubated for 20 mins by Thio-PAF assay B 10.31 pIC50 0.05 nM IC50 J Med Chem (2016) 59: 10738-10749 [PMID:27933945]
ChEMBL Inhibition of recombinant human Lp-PLA2 pre-incubated for 30 mins before PED6 fluorogenic substrate B 10.31 pIC50 0.05 nM IC50 J Med Chem (2016) 59: 10738-10749 [PMID:27933945]
ChEMBL Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assay B 10.31 pIC50 0.05 nM IC50 J. Med. Chem. (2016) 59: 5356-5367 [PMID:27167608]
GtoPdb In a biochemical assay, measuring fluorescence intensity and using Thio-Paf. - 10.31 pIC50 0.05 nM IC50 J Med Chem (2016) 59: 10738-10749 [PMID:27933945]
ChEMBL Inhibition of Lp-PLA2 in whole human plasma pre-incubated for 15 mins before 2-thio-PAF substrate addition B 10.46 pIC50 0.04 nM IC50 J Med Chem (2016) 59: 10738-10749 [PMID:27933945]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]