ChEMBL ligand: CHEMBL204021 (Darapladib, SB-480848)
PLA2-G7/LDL-associated phospholipase A2 in Human [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093] There should be some charts here, you may need to enable JavaScript!

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 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]