Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL204021 (Darapladib, SB-480848) |
---|
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]