Target id: 1417

Nomenclature: sPLA2-2A

Family: Hydrolases, Phospholipase A2

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for sPLA2-2A in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 144 1p35 PLA2G2A phospholipase A2 group IIA
Mouse - 146 4 D3 Pla2g2a phospholipase A2, group IIA (platelets, synovial fluid)
Rat - 146 5q36 Pla2g2a phospholipase A2 group IIA
Previous and Unofficial Names
GIIC sPLA2 | NPS-PLA2 | PLA2B | PLA2L | phospholipase A2, membrane associated | secreted enzyme type IIA phospholipase A2 | EF | Enhancing factor | phospholipase A2, group IIA (platelets, synovial fluid) | phospholipase A2
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
varespladib Hs Inhibition 8.1 – 8.1 pIC50 1,4
pIC50 8.1 (IC50 7x10-9 M) [1]
Description: IC50 from a radiometric deoxycholate/phosphatidylcholine assay.
pIC50 8.1 (IC50 9x10-9 M) [1,4]
Description: IC50 from a chromogenic in vitro assay.
KH064 Hs Inhibition 7.5 pIC50 2
pIC50 7.5 (IC50 2.9x10-8 M) [2]
compound 12e [PMID: 18605714] Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
Inhibitor Comments
A more valid measurement of varespladib's inhibitory activity is represented by the mole fraction (Xi50, which is the IC50 divided by the lipid concentration used in the assay) calculated from the deoxycholate/phosphatidylcholine (DOC/PC) assay, which addresses the fact that the very high potency of varespladib approaches the stoichiometric limit of the assay (limited by the enzyme concentration used in the assay). The Xi50 for varespladib in the DOC/PC assay was 1.5-1.8 x 10-6 [1,4].
Clinically-Relevant Mutations and Pathophysiology
Disease:  Colorectal cancer
Disease Ontology: DOID:9256
OMIM: 114500


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1. Draheim SE, Bach NJ, Dillard RD, Berry DR, Carlson DG, Chirgadze NY, Clawson DK, Hartley LW, Johnson LM, Jones ND et al.. (1996) Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. J. Med. Chem.39 (26): 5159-75. [PMID:8978844]

2. Hansford KA, Reid RC, Clark CI, Tyndall JD, Whitehouse MW, Guthrie T, McGeary RP, Schafer K, Martin JL, Fairlie DP. (2003) D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem4 (2-3): 181-5. [PMID:12616631]

3. Oslund RC, Cermak N, Gelb MH. (2008) Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. J. Med. Chem.51 (15): 4708-14. [PMID:18605714]

4. Snyder DW, Bach NJ, Dillard RD, Draheim SE, Carlson DG, Fox N, Roehm NW, Armstrong CT, Chang CH, Hartley LW et al.. (1999) Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. J. Pharmacol. Exp. Ther.288 (3): 1117-24. [PMID:10027849]

How to cite this page

Phospholipase A2: sPLA2-2A. Last modified on 28/08/2017. Accessed on 20/03/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1417.