varespladib [Ligand Id: 9657] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL148674 (LY-315920, LY315920, Varepladib, Varespladib, Varespladib sodium) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| iPLA2-G6/Calcium-independent phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3213] [GtoPdb: 1431] [UniProtKB: O60733] | ||||||||
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPG as substrate assessed as reduction in free [14C]-AA formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPE as substrate assessed as assessed as reduction in free AA formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPE as substrate assessed as reduction in 16:0 LPC formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPS as substrate assessed as reduction in 16:0 LPC formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPG as substrate assessed as reduction in 16:0 LPC formation after 30 mins in presence of equal molar mixture of PAPA/PAPC/PAPE/PAPG/PAPS/PLPC by HPLC-MS analysis | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPC as substrate assessed as reduction in free AA formation after 30 mins by HPLC-MS analysis | B | 6.88 | pIC50 | 131 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPC as substrate assessed as reduction in 16:0 LPC formation after 30 mins by HPLC-MS analysis | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| ChEMBL | Inhibition of human recombinant calcium-independent PLA2 using PAPC as substrate assessed as reduction in free [14C]-AA formation after 30 mins by scintillation counting | B | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2019) 62: 1999-2007 [PMID:30615445] |
| sPLA2-2D/Group IID secretory phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4281] [GtoPdb: 1418] [UniProtKB: Q9UNK4] | ||||||||
| ChEMBL | Inhibition of human group2D phospholipase A2 by [3H]oleic acid-labeled Escherichia coli membrane assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2D/Group IID secretory phospholipase A2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5537] [GtoPdb: 1418] [UniProtKB: Q9WVF6] | ||||||||
| ChEMBL | Inhibition of mouse group2D phospholipase A2 fluorimetric assay | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2E/Group IIE secretory phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2154] [GtoPdb: 1419] [UniProtKB: Q9NZK7] | ||||||||
| ChEMBL | Inhibition of human recombinant sPLA2 G2E | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of human group2E phospholipase A2 fluorimetric assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2E/Group IIE secretory phospholipase A2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4201] [GtoPdb: 1419] [UniProtKB: Q9QUL3] | ||||||||
| ChEMBL | Inhibition of mouse recombinant sPLA2 G2E | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of mouse group2E phospholipase A2 fluorimetric assay | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2F/Group IIF secretory phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4278] [GtoPdb: 1420] [UniProtKB: Q9BZM2] | ||||||||
| ChEMBL | Inhibition of human group2F phospholipase A2 fluorimetric assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2F/Group IIF secretory phospholipase A2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5361] [GtoPdb: 1420] [UniProtKB: Q9QZT4] | ||||||||
| ChEMBL | Inhibition of mouse group2F phospholipase A2 fluorimetric assay | B | 5.8 | pIC50 | >1600 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-10/Group X secretory phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4342] [GtoPdb: 1422] [UniProtKB: O15496] | ||||||||
| ChEMBL | Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using HDL as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins | B | 6.82 | pIC50 | 150 | nM | IC50 | ACS Med Chem Lett (2018) 9: 594-599 [PMID:30034585] |
| ChEMBL | Inhibition of human sPLA2X using 1,2-bis(heptanoylthio) glycerophosphocholine substrate incubated for 30 mins | B | 6.97 | pIC50 | 107.15 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5251-5255 [PMID:25316315] |
| ChEMBL | Inhibition of human recombinant sPLA2 G10 | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of human group2X phospholipase A2 fluorimetric assay | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| ChEMBL | Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2018) 9: 594-599 [PMID:30034585] |
| ChEMBL | Inhibition of recombinant sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by colorimetric method | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2016) 7: 884-889 [PMID:27774123] |
| sPLA2-10/Group X secretory phospholipase A2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4200] [GtoPdb: 1422] [UniProtKB: Q9QXX3] | ||||||||
| ChEMBL | Inhibition of mouse recombinant sPLA2 G10 | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of mouse group2X phospholipase A2 fluorimetric assay | B | 7.12 | pIC50 | 75 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-1B/Phospholipase A2 group 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4426] [GtoPdb: 1416] [UniProtKB: P04054] | ||||||||
| ChEMBL | Inhibition of human recombinant sPLA2 G1B | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of human group1B phospholipase A2 fluorimetric assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| ChEMBL | Compound was tested for inhibition of human secretory pancreatic Phospholipase A2 | B | 6.64 | pIC50 | 228 | nM | IC50 | J Med Chem (1996) 39: 5159-5175 [PMID:8978844] |
| Phospholipase A2 group 1B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4715] [UniProtKB: P00592] | ||||||||
| ChEMBL | Compound was tested for inhibition of porcine secretory pancreatic PLA2 | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (1996) 39: 5159-5175 [PMID:8978844] |
| sPLA2-1B/Phospholipase A2 group 1B in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4378] [GtoPdb: 1416] [UniProtKB: Q9Z0Y2] | ||||||||
| ChEMBL | Inhibition of mouse recombinant sPLA2 G1B | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of mouse group1B phospholipase A2 fluorimetric assay | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2A/Phospholipase A2 group IIA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3474] [GtoPdb: 1417] [UniProtKB: P14555] | ||||||||
| ChEMBL | Inhibition of human recombinant sPLA2 G2A | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of human group2A phospholipase A2 fluorimetric assay | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| ChEMBL | Inhibition of recombinant sPLA2-2A (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by colorimetric method | B | 7.55 | pIC50 | 28 | nM | IC50 | ACS Med Chem Lett (2016) 7: 884-889 [PMID:27774123] |
| ChEMBL | Inhibitory concentration against human nonpancreatic secretory phospholipase A2 | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2005) 48: 893-896 [PMID:15689175] |
| ChEMBL | Inhibition of recombinant human sPLA2-2A expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins | B | 7.92 | pIC50 | 12 | nM | IC50 | ACS Med Chem Lett (2018) 9: 594-599 [PMID:30034585] |
| ChEMBL | Inhibition of human nonpancreatic secretory Phospholipase A2 through chromogenic assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (1996) 39: 5159-5175 [PMID:8978844] |
| GtoPdb | IC50 from a chromogenic in vitro assay. | - | 8.05 | pIC50 | 9 | nM | IC50 |
J Med Chem (1996) 39: 5159-75 [PMID:8978844]; J Pharmacol Exp Ther (1999) 288: 1117-24 [PMID:10027849] |
| GtoPdb | IC50 from a radiometric deoxycholate/phosphatidylcholine assay. | - | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1996) 39: 5159-75 [PMID:8978844] |
| ChEMBL | Inhibitory concentration against human nonpancreatic secretory phospholipase A2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2005) 48: 893-896 [PMID:15689175] |
| ChEMBL | Inhibition of human nonpancreatic secretory Phospholipase A2 through DOC/PC assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1996) 39: 5159-5175 [PMID:8978844] |
| PLA2-G5/Phospholipase A2 group V in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4323] [GtoPdb: 1430] [UniProtKB: P39877] | ||||||||
| ChEMBL | Inhibition of human recombinant sPLA2 G5 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of human group2V phospholipase A2 fluorimetric assay | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| ChEMBL | Inhibition of recombinant human sPLA2-5 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins | B | 6.91 | pIC50 | 124 | nM | IC50 | ACS Med Chem Lett (2018) 9: 594-599 [PMID:30034585] |
| PLA2-G5/Phospholipase A2 group V in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4167] [GtoPdb: 1430] [UniProtKB: P97391] | ||||||||
| ChEMBL | Inhibition of mouse recombinant sPLA2 G5 | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of mouse group2V phospholipase A2 fluorimetric assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| sPLA2-2A in Human [GtoPdb: 1417] [UniProtKB: P14555] | ||||||||
| GtoPdb | IC50 from a chromogenic in vitro assay. | - | 8.05 | pIC50 | 9 | nM | IC50 |
J Med Chem (1996) 39: 5159-75 [PMID:8978844]; J Pharmacol Exp Ther (1999) 288: 1117-24 [PMID:10027849] |
| GtoPdb | IC50 from a radiometric deoxycholate/phosphatidylcholine assay. | - | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1996) 39: 5159-75 [PMID:8978844] |
| sPLA2-2A/Phospholipase A2, membrane associated in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5761] [GtoPdb: 1417] [UniProtKB: P31482] | ||||||||
| ChEMBL | Inhibition of mouse recombinant sPLA2 G2A | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2006) 49: 2858-2860 [PMID:16686528] |
| ChEMBL | Inhibition of mouse group2A phospholipase A2 fluorimetric assay | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
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]
