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 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]