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] |
| ChEMBL | Inhibition of human group IB phospholipase A2 incubated for 1 hrs by scintillation counter analysis | B | 6.64 | pIC50 | 228 | nM | IC50 | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
| 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] |
| ChEMBL | Inhibition of pig group IB phospholipase A2 incubated for 1 hrs by scintillation counter analysis | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
| 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 group2A phospholipase A2 fluorimetric assay | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2008) 51: 4708-4714 [PMID:18605714] |
| 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 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 group IIA phospholipase A2 incubated for 1 hrs by scintillation counter analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
| 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 | 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] |
| 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] |
| 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 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]
