varespladib [Ligand Id: 9657] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL148674 (Varespladib, Varespladib sodium, Varepladib, LY315920, LY-315920)
  • iPLA2-G6/Calcium-independent phospholipase A2 in Human [ChEMBL: CHEMBL3213] [GtoPdb: 1431] [UniProtKB: O60733]
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  • sPLA2-2D/Group IID secretory phospholipase A2 in Human [ChEMBL: CHEMBL4281] [GtoPdb: 1418] [UniProtKB: Q9UNK4]
  • sPLA2-2D/Group IID secretory phospholipase A2 in Mouse [ChEMBL: CHEMBL5537] [GtoPdb: 1418] [UniProtKB: Q9WVF6]
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  • sPLA2-2E/Group IIE secretory phospholipase A2 in Human [ChEMBL: CHEMBL2154] [GtoPdb: 1419] [UniProtKB: Q9NZK7]
  • sPLA2-2E/Group IIE secretory phospholipase A2 in Mouse [ChEMBL: CHEMBL4201] [GtoPdb: 1419] [UniProtKB: Q9QUL3]
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  • sPLA2-2F/Group IIF secretory phospholipase A2 in Human [ChEMBL: CHEMBL4278] [GtoPdb: 1420] [UniProtKB: Q9BZM2]
  • sPLA2-2F/Group IIF secretory phospholipase A2 in Mouse [ChEMBL: CHEMBL5361] [GtoPdb: 1420] [UniProtKB: Q9QZT4]
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  • sPLA2-10/Group X secretory phospholipase A2 in Human [ChEMBL: CHEMBL4342] [GtoPdb: 1422] [UniProtKB: O15496]
  • sPLA2-10/Group X secretory phospholipase A2 in Mouse [ChEMBL: CHEMBL4200] [GtoPdb: 1422] [UniProtKB: Q9QXX3]
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  • sPLA2-2A/Phospholipase A2 group IIA in Human [ChEMBL: CHEMBL3474] [GtoPdb: 1417] [UniProtKB: P14555]
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  • sPLA2-2A in Human [GtoPdb: 1417] [UniProtKB: P14555]
  • sPLA2-2A/Phospholipase A2, membrane associated in Mouse [ChEMBL: CHEMBL5761] [GtoPdb: 1417] [UniProtKB: P31482]
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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 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 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 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 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 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 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 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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]