PLA2G2F
gene geneOn this page
Summary
PLA2G2F (phospholipase A2 group IIF, HGNC:30040) is a protein-coding gene on chromosome 1p36.12, encoding Group IIF secretory phospholipase A2 (Q9BZM2). Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids.
Enables calcium-dependent phospholipase A2 activity. Involved in glycerophospholipid metabolic process. Predicted to be located in cytosol and extracellular region.
Source: NCBI Gene 64600 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 55 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_022819
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:30040 |
| Approved symbol | PLA2G2F |
| Name | phospholipase A2 group IIF |
| Location | 1p36.12 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000158786 |
| Ensembl biotype | protein_coding |
| OMIM | 616793 |
| Entrez | 64600 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 1 protein_coding, 1 retained_intron
ENST00000375102, ENST00000465062
RefSeq mRNA: 2 — MANE Select: NM_022819
NM_001360869, NM_022819
CCDS: CCDS204
Canonical transcript exons
ENST00000375102 — 5 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000908635 | 20143446 | 20143590 |
| ENSE00000908636 | 20144580 | 20144689 |
| ENSE00001465759 | 20148190 | 20150381 |
| ENSE00001664731 | 20140166 | 20140218 |
| ENSE00001958398 | 20139323 | 20139543 |
Expression profiles
Bgee: expression breadth broad, 42 present calls, max score 82.03.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1000 / max 28.1037, expressed in 33 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 1102 | 0.0926 | 33 |
| 1103 | 0.0074 | 3 |
Top tissues by expression
265 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| skin of leg | UBERON:0001511 | 82.03 | gold quality |
| skin of abdomen | UBERON:0001416 | 80.98 | gold quality |
| zone of skin | UBERON:0000014 | 77.49 | gold quality |
| urinary bladder | UBERON:0001255 | 64.11 | gold quality |
| jejunal mucosa | UBERON:0000399 | 56.76 | gold quality |
| pancreatic ductal cell | CL:0002079 | 56.69 | silver quality |
| decidua | UBERON:0002450 | 56.55 | gold quality |
| heart right ventricle | UBERON:0002080 | 55.77 | gold quality |
| tibialis anterior | UBERON:0001385 | 54.79 | silver quality |
| myocardium | UBERON:0002349 | 54.38 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 54.15 | gold quality |
| cerebellar vermis | UBERON:0004720 | 53.34 | gold quality |
| deltoid | UBERON:0001476 | 53.11 | gold quality |
| gingival epithelium | UBERON:0001949 | 53.00 | gold quality |
| hair follicle | UBERON:0002073 | 52.43 | gold quality |
| gall bladder | UBERON:0002110 | 51.90 | gold quality |
| jejunum | UBERON:0002115 | 51.87 | gold quality |
| gingiva | UBERON:0001828 | 51.76 | gold quality |
| upper leg skin | UBERON:0004262 | 51.05 | gold quality |
| tibia | UBERON:0000979 | 50.87 | gold quality |
| upper arm skin | UBERON:0004263 | 50.67 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 50.62 | gold quality |
| ileal mucosa | UBERON:0000331 | 50.32 | silver quality |
| tonsil | UBERON:0002372 | 50.13 | gold quality |
| mammalian vulva | UBERON:0000997 | 49.37 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 49.30 | gold quality |
| blood vessel layer | UBERON:0004797 | 49.29 | gold quality |
| mucosa of stomach | UBERON:0001199 | 49.22 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 49.20 | gold quality |
| quadriceps femoris | UBERON:0001377 | 49.17 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.02 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
80 targeting PLA2G2F, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4283 | 100.00 | 66.42 | 2097 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-12118 | 100.00 | 65.88 | 1270 |
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-4455 | 100.00 | 65.48 | 1587 |
| HSA-MIR-6870-5P | 99.99 | 68.55 | 2115 |
| HSA-MIR-4500 | 99.99 | 72.72 | 2367 |
| HSA-MIR-4531 | 99.99 | 69.70 | 3181 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-3173-3P | 99.98 | 66.49 | 1217 |
| HSA-MIR-7111-5P | 99.97 | 68.48 | 2062 |
| HSA-MIR-4723-5P | 99.97 | 68.70 | 2034 |
| HSA-MIR-5698 | 99.97 | 68.49 | 2029 |
| HSA-MIR-4267 | 99.96 | 66.53 | 2368 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-6721-5P | 99.93 | 68.92 | 2981 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-4493 | 99.90 | 66.48 | 977 |
| HSA-MIR-4731-5P | 99.89 | 67.23 | 2537 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-579-3P | 99.86 | 71.66 | 3628 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-4447 | 99.85 | 67.81 | 2900 |
| HSA-MIR-664B-3P | 99.84 | 71.65 | 3590 |
| HSA-MIR-4319 | 99.76 | 69.83 | 2586 |
| HSA-MIR-4306 | 99.72 | 70.50 | 3630 |
| HSA-MIR-6887-3P | 99.66 | 67.83 | 1778 |
| HSA-MIR-7112-5P | 99.59 | 65.76 | 104 |
| HSA-MIR-762 | 99.58 | 66.61 | 1994 |
| HSA-MIR-12123 | 99.52 | 71.79 | 2990 |
Literature-anchored findings (GeneRIF, showing 1)
- two of these isoforms, sPLA2 IIA and sPLA2 IIF, localize to the upper stratum granulosum and increase in response to experimental barrier perturbation. (PMID:24269828)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Pla2g2f | ENSMUSG00000028749 |
| rattus_norvegicus | Pla2g2f | ENSRNOG00000016798 |
| caenorhabditis_elegans | WBGENE00007419 | |
| caenorhabditis_elegans | WBGENE00015406 |
Paralogs (8): PLA2G10 (ENSG00000069764), PLA2G2D (ENSG00000117215), PLA2G5 (ENSG00000127472), PLA2G1B (ENSG00000170890), PLA2G2C (ENSG00000187980), PLA2G2A (ENSG00000188257), PLA2G2E (ENSG00000188784), OC90 (ENSG00000253117)
Protein
Protein identifiers
Group IIF secretory phospholipase A2 — Q9BZM2 (reviewed: Q9BZM2)
Alternative names: Phosphatidylcholine 2-acylhydrolase 2F
All UniProt accessions (1): Q9BZM2
UniProt curated annotations — full annotation on UniProt →
Function. Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids. Hydrolyzes the ester bond of the fatty acyl group attached at the sn-2 position of phospholipids (phospholipase A2 activity), the catalytic efficiency decreasing in the following order: phosphatidylglycerols > phosphatidylethanolamines > phosphatidylcholines > phosphatidylserines. May play a role in lipid mediator production in inflammatory conditions, by providing arachidonic acid to downstream cyclooxygenases and lipoxygenases.
Subcellular location. Secreted. Cell membrane.
Tissue specificity. Expressed at high levels in placenta, testis, thymus and at lower levels in heart, kidney, liver and prostate. Highly expressed in rheumatoid arthritic tissues, including synovial lining cells in the intima, capillary endothelial cells and plasma cells.
Cofactor. Binds 1 Ca(2+) ion per subunit.
Miscellaneous. No signal peptide could be predicted in this isoform, challenging its subcellular location within the secretory pathway and hence the formation of disulfide bonds, which are required for its activity.
Similarity. Belongs to the phospholipase A2 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9BZM2-1 | 1 | yes |
| Q9BZM2-2 | 2 |
RefSeq proteins (2): NP_001347798, NP_073730* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001211 | PLA2 | Family |
| IPR016090 | PLA2-like_dom | Domain |
| IPR033113 | PLA2_histidine | Active_site |
| IPR036444 | PLipase_A2_dom_sf | Homologous_superfamily |
Pfam: PF00068
Catalyzed reactions (Rhea), 6 shown:
- a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 1-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:15801)
- 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:38779)
- 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40431)
- 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (9Z,12Z)-octadecadienoate + H(+) (RHEA:40815)
- 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phospho-(1’-sn-glycerol) + H2O = 1-hexadecanoyl-sn-glycero-3-phospho-(1’-sn-glycerol) + (9Z)-octadecenoate + H(+) (RHEA:40919)
- 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phospho-L-serine + H2O = 1-hexadecanoyl-sn-glycero-3-phospho-L-serine + (9Z)-octadecenoate + H(+) (RHEA:41752)
UniProt features (22 total): disulfide bond 7, glycosylation site 4, binding site 4, active site 2, signal peptide 1, chain 1, region of interest 1, splice variant 1, sequence conflict 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BZM2-F1 | 89.46 | 0.76 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (2): 67; 114
Ligand- & substrate-binding residues (4): 47; 49; 51; 68
Disulfide bonds (7): 46–138, 48–64, 63–120, 69–145, 70–113, 79–106, 98–111
Glycosylation sites (4): 102, 123, 144, 92
Function
Pathways and Gene Ontology
Reactome pathways
6 pathways
| ID | Pathway |
|---|---|
| R-HSA-1482788 | Acyl chain remodelling of PC |
| R-HSA-1482801 | Acyl chain remodelling of PS |
| R-HSA-1482839 | Acyl chain remodelling of PE |
| R-HSA-1482922 | Acyl chain remodelling of PI |
| R-HSA-1482925 | Acyl chain remodelling of PG |
| R-HSA-1483166 | Synthesis of PA |
MSigDB gene sets: 144 (showing top):
GOBP_PHOSPHATIDYLSERINE_ACYL_CHAIN_REMODELING, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_LEUKOCYTE_PROLIFERATION, KEGG_MAPK_SIGNALING_PATHWAY, IVANOVA_HEMATOPOIESIS_MATURE_CELL, GOBP_NEGATIVE_REGULATION_OF_CELL_CELL_ADHESION, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_LONG_CHAIN_FATTY_ACID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLGLYCEROL_METABOLIC_PROCESS, KEGG_FC_EPSILON_RI_SIGNALING_PATHWAY, GOBP_ORGANIC_ACID_TRANSPORT
GO Biological Process (14): lipid catabolic process (GO:0016042), arachidonate metabolic process (GO:0019369), phosphatidylglycerol acyl-chain remodeling (GO:0036148), phosphatidylserine acyl-chain remodeling (GO:0036150), phosphatidylcholine acyl-chain remodeling (GO:0036151), phosphatidylethanolamine acyl-chain remodeling (GO:0036152), negative regulation of T cell proliferation (GO:0042130), innate immune response (GO:0045087), phosphatidylcholine metabolic process (GO:0046470), phosphatidylglycerol metabolic process (GO:0046471), arachidonate secretion (GO:0050482), immune system process (GO:0002376), lipid metabolic process (GO:0006629), phospholipid metabolic process (GO:0006644)
GO Molecular Function (7): A2-type glycerophospholipase activity (GO:0004623), calcium ion binding (GO:0005509), phospholipid binding (GO:0005543), obsolete calcium-dependent phospholipase A2 activity (GO:0047498), protein binding (GO:0005515), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)
GO Cellular Component (4): extracellular region (GO:0005576), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Glycerophospholipid biosynthesis | 6 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| lipid metabolic process | 2 |
| phosphatidylcholine metabolic process | 2 |
| glycerophospholipid metabolic process | 2 |
| catabolic process | 1 |
| long-chain fatty acid metabolic process | 1 |
| icosanoid metabolic process | 1 |
| unsaturated fatty acid metabolic process | 1 |
| olefinic compound metabolic process | 1 |
| phosphatidylglycerol metabolic process | 1 |
| phosphatidylserine metabolic process | 1 |
| T cell proliferation | 1 |
| regulation of T cell proliferation | 1 |
| negative regulation of lymphocyte proliferation | 1 |
| negative regulation of T cell activation | 1 |
| immune response | 1 |
| defense response to symbiont | 1 |
| icosanoid secretion | 1 |
| arachidonate transport | 1 |
| biological_process | 1 |
| primary metabolic process | 1 |
| organophosphate metabolic process | 1 |
| glycerophospholipase activity | 1 |
| carboxylic ester hydrolase activity | 1 |
| metal ion binding | 1 |
| lipid binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| cytoplasm | 1 |
| membrane | 1 |
| cell periphery | 1 |
Protein interactions and networks
STRING
392 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PLA2G2F | PLA2G3 | Q9NZ20 | 700 |
| PLA2G2F | PLA2G12B | Q9BX93 | 631 |
| PLA2G2F | PLA2G12A | Q9BZM1 | 612 |
| PLA2G2F | PLA2G4D | Q86XP0 | 500 |
| PLA2G2F | PLA2G6 | O60733 | 491 |
| PLA2G2F | PLA2G4C | Q9UP65 | 451 |
| PLA2G2F | PLA2G4A | P47712 | 445 |
| PLA2G2F | PLA2G4F | Q68DD2 | 434 |
| PLA2G2F | ENPP2 | Q13822 | 432 |
| PLA2G2F | PLA2G4B | P0C869 | 424 |
| PLA2G2F | CYP2E1 | P05181 | 419 |
| PLA2G2F | PLA2G4E | Q3MJ16 | 407 |
| PLA2G2F | PNPLA1 | Q8N8W4 | 388 |
| PLA2G2F | APOB | P04114 | 353 |
| PLA2G2F | Q6ZTK2 | Q6ZTK2 | 330 |
IntAct
2 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| KLHL22 | TRAV18 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (4): PLA2G2F (Two-hybrid), PLA2G2F (Two-hybrid), MINOS1-NBL1 (Two-hybrid), PLA2G2F (Affinity Capture-MS)
ESM2 similar proteins: A0A411EZW9, A8E2V9, C1IC45, C1IC46, D0UGJ0, P00616, P00617, P00619, P00625, P06859, P0CAR9, P0CAS0, P0DUN0, P0DUN2, P17934, P20476, P23028, P58464, P59018, P70089, P70090, P84397, Q2HZ28, Q2PG81, Q2PG83, Q2PWA3, Q6H3D0, Q6H3D2, Q6H3D3, Q6H3D4, Q6H3D5, Q6H3D6, Q6H3D7, Q6YIJ3, Q6YNQ0, Q75S51, Q7T1R0, Q7ZTA7, Q800C2, Q800C3
Diamond homologs: A8CG78, A8CG82, A8CG84, A8CG87, A8CG89, B5U6Y4, B5U6Z2, B6CQR5, C0HJL8, C0HLF0, C0HMB2, C3W4R6, C9DPL5, F8QN52, F8QN54, G3DT18, O15496, O42187, O42188, P00606, P00622, P00626, P04057, P04417, P08872, P0CAR9, P0DJN7, P0DJP4, P0DMT1, P0DMT2, P0DMT3, P0DP54, P0DUP2, P11407, P14423, P14424, P14555, P17935, P20250, P20251
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
55 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 46 |
| Likely benign | 6 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
909 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:20139542:AGG:A | donor_loss | 1.0000 |
| 1:20139544:G:GA | donor_loss | 1.0000 |
| 1:20143444:A:AG | acceptor_gain | 1.0000 |
| 1:20143445:G:GG | acceptor_gain | 1.0000 |
| 1:20144687:GCA:G | donor_gain | 1.0000 |
| 1:20144690:G:GG | donor_gain | 1.0000 |
| 1:20148187:TAGGT:T | acceptor_loss | 1.0000 |
| 1:20148189:G:A | acceptor_loss | 1.0000 |
| 1:20148354:G:GT | donor_gain | 1.0000 |
| 1:20142855:G:GT | donor_gain | 0.9900 |
| 1:20143442:GCAGT:G | acceptor_loss | 0.9900 |
| 1:20143445:G:A | acceptor_loss | 0.9900 |
| 1:20143445:GT:G | acceptor_gain | 0.9900 |
| 1:20143445:GTT:G | acceptor_gain | 0.9900 |
| 1:20143445:GTTC:G | acceptor_gain | 0.9900 |
| 1:20143445:GTTCT:G | acceptor_gain | 0.9900 |
| 1:20143540:T:TA | donor_gain | 0.9900 |
| 1:20143587:ACTGG:A | donor_loss | 0.9900 |
| 1:20143588:CTGG:C | donor_loss | 0.9900 |
| 1:20143589:TGGT:T | donor_loss | 0.9900 |
| 1:20143591:G:GC | donor_loss | 0.9900 |
| 1:20143591:G:GG | donor_gain | 0.9900 |
| 1:20143592:T:G | donor_loss | 0.9900 |
| 1:20143594:GGT:G | donor_loss | 0.9900 |
| 1:20144686:TGCA:T | donor_gain | 0.9900 |
| 1:20144687:GCAG:G | donor_gain | 0.9900 |
| 1:20144688:CAG:C | donor_loss | 0.9900 |
| 1:20144689:AG:A | donor_loss | 0.9900 |
| 1:20144690:G:A | donor_loss | 0.9900 |
| 1:20144691:TGAG:T | donor_loss | 0.9900 |
AlphaMissense
1404 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000157925 (1:20141742 C>T), RS1000166259 (1:20144892 T>C), RS1000270590 (1:20146852 C>T), RS1000431844 (1:20150575 C>T), RS1000509031 (1:20141603 G>A,T), RS1000565457 (1:20145284 A>T), RS1000788812 (1:20140643 A>T), RS1000814520 (1:20150557 C>G,T), RS1001102926 (1:20150419 G>A), RS1001449622 (1:20142015 T>C), RS1001557203 (1:20145732 C>A,T), RS1001560884 (1:20141173 A>G), RS1001765336 (1:20145462 A>C), RS1001899347 (1:20140898 C>G), RS1002005029 (1:20145862 C>T)
Disease associations
OMIM: gene MIM:616793 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST008260_11 | Group IIA secretory phospholipase A2 levels in individuals with elevated hsCRP | 1.000000e-11 |
| GCST008260_8 | Group IIA secretory phospholipase A2 levels in individuals with elevated hsCRP | 2.000000e-26 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4278 (SINGLE PROTEIN), CHEMBL4524005 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 272 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL148674 | VARESPLADIB | 2 | 272 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Phospholipase A2
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| compound 12e [PMID: 18605714] | Inhibition | 7.3 | pIC50 |
ChEMBL bioactivities
12 potent at pChembl≥5 of 13 total, top 12 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.30 | IC50 | 50 | nM | CHEMBL515637 |
| 7.25 | IC50 | 56 | nM | CHEMBL4593409 |
| 7.05 | IC50 | 90 | nM | CHEMBL148649 |
| 7.05 | IC50 | 90 | nM | CHEMBL514705 |
| 6.94 | IC50 | 114 | nM | VARESPLADIB |
| 6.89 | IC50 | 130 | nM | VARESPLADIB |
| 6.88 | IC50 | 131 | nM | VARESPLADIB |
| 6.54 | IC50 | 290 | nM | CHEMBL506485 |
| 6.26 | IC50 | 550 | nM | CHEMBL504813 |
| 6.26 | IC50 | 550 | nM | CHEMBL446349 |
| 6.01 | IC50 | 970 | nM | CHEMBL478820 |
| 5.96 | IC50 | 1100 | nM | CHEMBL514692 |
PubChem BioAssay actives
13 with measured affinity, of 42 total; 10 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (2R)-3-[3-(5-benzyl-2-carbamoylphenyl)phenyl]-2-methylpropanoic acid | 1631141: Inhibition of sPLA2 in human HepG2 cells | ic50 | 0.0140 | uM |
| 2-(1-benzyl-2-ethyl-3-oxamoylbenzo[g]indol-4-yl)oxyacetic acid | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.0500 | uM |
| 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxypropanoic acid | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.0900 | uM |
| 2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylbenzo[g]indol-4-yl]oxyacetic acid | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.0900 | uM |
| 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid | 1614038: Inhibition of human recombinant sPLA2 assessed as reduction in 16:0 LPC formation after 30 mins by HPLC-MS analysis | ic50 | 0.1140 | uM |
| 2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-(2-methylpropyl)benzo[g]indol-3-yl]-2-oxoacetamide | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.2900 | uM |
| 2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylindol-4-yl]oxyacetic acid | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.5500 | uM |
| 2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-ethylbenzo[g]indol-3-yl]-2-oxoacetamide | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.5500 | uM |
| 2-[2-(2-methylpropyl)-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 0.9700 | uM |
| 2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-ethylindol-3-yl]-2-oxoacetamide | 341247: Inhibition of human group2F phospholipase A2 fluorimetric assay | ic50 | 1.1000 | uM |
CTD chemical–gene interactions
10 total (human), top 10 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Resveratrol | affects cotreatment, decreases expression | 2 |
| benzo(e)pyrene | increases methylation | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| theaflavin-3,3’-digallate | affects expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Copper | affects cotreatment, decreases expression | 1 |
| Methapyrilene | increases methylation | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
17 unique, capped per target: 17 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3773530 | Binding | Inhibition of human group 2F secreted phospholipase A2 assessed as remaining activity at 1000 nM by fluorescence assay | Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations. — Bioorg Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.