PLA2G12A
gene geneOn this page
Summary
PLA2G12A (phospholipase A2 group XIIA, HGNC:18554) is a protein-coding gene on chromosome 4q25, encoding Group XIIA secretory phospholipase A2 (Q9BZM1). PA2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides.
Secreted phospholipase A2 (sPLA2) enzymes liberate arachidonic acid from phospholipids for production of eicosanoids and exert a variety of physiologic and pathologic effects. Group XII sPLA2s, such as PLA2G12A, have relatively low specific activity and are structurally and functionally distinct from other sPLA2s (Gelb et al., 2000 [PubMed 11031251]).
Source: NCBI Gene 81579 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 46 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_030821
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:18554 |
| Approved symbol | PLA2G12A |
| Name | phospholipase A2 group XIIA |
| Location | 4q25 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000123739 |
| Ensembl biotype | protein_coding |
| OMIM | 611652 |
| Entrez | 81579 |
Gene structure
Transcript identifiers
Ensembl transcripts: 6 — 4 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay
ENST00000243501, ENST00000502283, ENST00000502772, ENST00000507961, ENST00000858473, ENST00000858474
RefSeq mRNA: 1 — MANE Select: NM_030821
NM_030821
CCDS: CCDS3686
Canonical transcript exons
ENST00000243501 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000841706 | 109709989 | 109714495 |
| ENSE00000841708 | 109718683 | 109718759 |
| ENSE00000841709 | 109729602 | 109730070 |
| ENSE00003588438 | 109717548 | 109717713 |
Expression profiles
Bgee: expression breadth ubiquitous, 263 present calls, max score 98.01.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 12.9696 / max 95.6140, expressed in 1750 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 53603 | 11.1427 | 1745 |
| 53602 | 1.1351 | 474 |
| 53601 | 0.6918 | 337 |
Top tissues by expression
263 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| oviduct epithelium | UBERON:0004804 | 98.01 | gold quality |
| upper arm skin | UBERON:0004263 | 96.79 | gold quality |
| kidney epithelium | UBERON:0004819 | 96.78 | gold quality |
| endothelial cell | CL:0000115 | 96.53 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 96.28 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 96.00 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 95.87 | gold quality |
| renal medulla | UBERON:0000362 | 95.78 | gold quality |
| pons | UBERON:0000988 | 95.56 | gold quality |
| medulla oblongata | UBERON:0001896 | 95.29 | gold quality |
| parietal pleura | UBERON:0002400 | 95.26 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 95.05 | gold quality |
| tibialis anterior | UBERON:0001385 | 95.01 | gold quality |
| pancreatic ductal cell | CL:0002079 | 94.98 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 94.74 | gold quality |
| ileal mucosa | UBERON:0000331 | 94.69 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 94.65 | gold quality |
| superior vestibular nucleus | UBERON:0007227 | 94.57 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 94.43 | gold quality |
| deltoid | UBERON:0001476 | 94.32 | gold quality |
| nipple | UBERON:0002030 | 94.31 | gold quality |
| substantia nigra pars compacta | UBERON:0001965 | 94.22 | gold quality |
| ventral tegmental area | UBERON:0002691 | 94.13 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 94.12 | gold quality |
| visceral pleura | UBERON:0002401 | 94.10 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 94.09 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 93.46 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 93.44 | gold quality |
| cardia of stomach | UBERON:0001162 | 93.22 | gold quality |
| corpus callosum | UBERON:0002336 | 93.07 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 10.82 |
| E-GEOD-125970 | yes | 4.84 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
140 targeting PLA2G12A, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-511-3P | 99.99 | 68.85 | 1467 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-196A-1-3P | 99.99 | 72.15 | 2772 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-568 | 99.98 | 69.86 | 2084 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
| HSA-MIR-302C-5P | 99.97 | 72.56 | 3642 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-551B-5P | 99.96 | 71.28 | 3493 |
| HSA-MIR-548AT-5P | 99.96 | 70.83 | 2666 |
| HSA-MIR-302E | 99.96 | 70.74 | 2669 |
| HSA-MIR-545-3P | 99.95 | 70.74 | 2783 |
| HSA-MIR-9983-3P | 99.94 | 71.48 | 3631 |
| HSA-MIR-548AH-3P | 99.93 | 72.54 | 4872 |
| HSA-MIR-548AM-3P | 99.93 | 72.54 | 4872 |
| HSA-MIR-515-5P | 99.92 | 69.82 | 2343 |
| HSA-MIR-519E-5P | 99.92 | 69.62 | 2358 |
Literature-anchored findings (GeneRIF, showing 4)
- cellular arachidonate (AA) release and prostaglandin (PG) production are regulated by novel classes of secretory phospholipase A(2)s (sPLA(2)s), groups III and XII (PMID:12522102)
- The study demonstrated that PLA2G12A SNPs or haplotypes might influence the susceptibility to schizophrenia in the Han Chinese population from Northeast China. (PMID:27434078)
- The results of this study revealed that PLA2G12A rs3087494 polymorphism did not influence age at onset in patients with schizophrenia. (PMID:29527719)
- PLA2G12A protects against diet-induced obesity and insulin resistance by enhancing energy expenditure and clearance of circulating triglycerides. (PMID:38703030)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | pla2g12a | ENSDARG00000070454 |
| mus_musculus | Pla2g12a | ENSMUSG00000027999 |
| rattus_norvegicus | Pla2g12a | ENSRNOG00000057470 |
| drosophila_melanogaster | GXIVsPLA2 | FBGN0036545 |
| caenorhabditis_elegans | WBGENE00016288 | |
| caenorhabditis_elegans | WBGENE00018411 |
Paralogs (1): PLA2G12B (ENSG00000138308)
Protein
Protein identifiers
Group XIIA secretory phospholipase A2 — Q9BZM1 (reviewed: Q9BZM1)
Alternative names: Phosphatidylcholine 2-acylhydrolase 12A
All UniProt accessions (4): A0A0C4DGC6, D6RBP5, Q9BZM1, Q542Y6
UniProt curated annotations — full annotation on UniProt →
Function. PA2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides. Does not exhibit detectable activity toward sn-2-arachidonoyl- or linoleoyl-phosphatidylcholine or -phosphatidylethanolamine.
Subcellular location. Secreted. Cytoplasm.
Tissue specificity. Abundantly expressed in heart, skeletal muscle, kidney, liver and pancreas.
Cofactor. Binds 1 Ca(2+) ion per subunit.
Similarity. Belongs to the phospholipase A2 family.
RefSeq proteins (1): NP_110448* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR010711 | PLA2G12 | Family |
| IPR033113 | PLA2_histidine | Active_site |
| IPR036444 | PLipase_A2_dom_sf | Homologous_superfamily |
Pfam: PF06951
Catalyzed reactions (Rhea), 1 shown:
- a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 1-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:15801)
UniProt features (9 total): binding site 4, active site 2, signal peptide 1, chain 1, sequence conflict 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BZM1-F1 | 81.38 | 0.31 |
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): 110; 125
Ligand- & substrate-binding residues (4): 88; 90; 92; 111
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: 187 (showing top):
WAMUNYOKOLI_OVARIAN_CANCER_LMP_DN, chr4q25, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, KEGG_MAPK_SIGNALING_PATHWAY, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, TGACCTY_ERR1_Q2, KEGG_FC_EPSILON_RI_SIGNALING_PATHWAY, GOBP_ORGANIC_ACID_TRANSPORT, UEDA_PERIFERAL_CLOCK, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_SECRETION, GOBP_LIPID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_TRANSPORT
GO Biological Process (4): phospholipid metabolic process (GO:0006644), lipid catabolic process (GO:0016042), arachidonate secretion (GO:0050482), lipid metabolic process (GO:0006629)
GO Molecular Function (6): A2-type glycerophospholipase activity (GO:0004623), calcium ion binding (GO:0005509), obsolete calcium-dependent phospholipase A2 activity (GO:0047498), protein binding (GO:0005515), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)
GO Cellular Component (2): extracellular region (GO:0005576), cytoplasm (GO:0005737)
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 |
|---|---|
| lipid metabolic process | 2 |
| cellular anatomical structure | 2 |
| organophosphate metabolic process | 1 |
| catabolic process | 1 |
| icosanoid secretion | 1 |
| arachidonate transport | 1 |
| primary metabolic process | 1 |
| glycerophospholipase activity | 1 |
| carboxylic ester hydrolase activity | 1 |
| metal ion binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| intracellular anatomical structure | 1 |
Protein interactions and networks
STRING
678 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PLA2G12A | PLA2G10 | O15496 | 955 |
| PLA2G12A | PLA2G3 | Q9NZ20 | 929 |
| PLA2G12A | PLA2G2D | Q9UNK4 | 898 |
| PLA2G12A | PLA2G2A | P14555 | 875 |
| PLA2G12A | PLA2G2E | Q9NZK7 | 623 |
| PLA2G12A | PLA2G2C | Q5R387 | 616 |
| PLA2G12A | PLA2G2F | Q9BZM2 | 612 |
| PLA2G12A | PLA2G5 | P39877 | 583 |
| PLA2G12A | PLA2G4C | Q9UP65 | 570 |
| PLA2G12A | PLA2G1B | P04054 | 542 |
| PLA2G12A | ENPP2 | Q13822 | 508 |
| PLA2G12A | PLA2G4A | P47712 | 481 |
| PLA2G12A | CYP2E1 | P05181 | 471 |
| PLA2G12A | PLA2G6 | O60733 | 451 |
| PLA2G12A | SMAD4 | Q13485 | 429 |
IntAct
20 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| GRN | PLA2G12A | psi-mi:“MI:0915”(physical association) | 0.560 |
| PLA2G12A | WFS1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| EPB41L3 | AP3B1 | psi-mi:“MI:0914”(association) | 0.530 |
| PLA2G12A | PXDN | psi-mi:“MI:0915”(physical association) | 0.400 |
| PLA2G12A | HSPA5 | psi-mi:“MI:0915”(physical association) | 0.400 |
| PLA2G12A | WDTC1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| PLA2G12A | DVL2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| MEF2C | PLA2G12A | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLA2G12A | RB1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLA2G12A | RPS6 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLA2G12A | RPS15 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLA2G12A | UMPS | psi-mi:“MI:0915”(physical association) | 0.370 |
| YWHAG | PLA2G12A | psi-mi:“MI:0915”(physical association) | 0.370 |
| PLA2G12A | UCK1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| TMEM37 | PLA2G12A | psi-mi:“MI:0915”(physical association) | 0.370 |
BioGRID (16): PLA2G12A (Affinity Capture-MS), PXDN (Affinity Capture-MS), PLA2G12A (Affinity Capture-RNA), PLA2G12A (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), WDTC1 (Affinity Capture-MS), PLA2G12A (Synthetic Rescue), RPS6 (Two-hybrid), UCK1 (Two-hybrid), RB1 (Two-hybrid), UMPS (Two-hybrid), RPS15 (Two-hybrid), YWHAG (Two-hybrid), TMEM37 (Two-hybrid), PLA2G12A (Two-hybrid)
ESM2 similar proteins: A0A1L4BJ46, A0A5C1ZXT8, A0A5C2A2T2, A8WP66, F4JP36, H2KZU7, I7GQA7, O45879, O55159, O62301, O76411, P00630, P02675, P0C8L9, P0DKU2, P0DMI6, P0DPT7, P0DPT9, P0DPZ3, P0DPZ9, P0DXZ6, P0DY42, P14480, P16422, P42579, P58239, P59888, Q09553, Q10128, Q1WER1, Q3T0L5, Q5F381, Q6P9Z6, Q6PXP0, Q6T178, Q75QW1, Q8BGV3, Q8BJ83, Q8K0E8, Q8VCM7
Diamond homologs: Q99P27, Q9BX93, Q9BZM1, Q9EPR2
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
46 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 38 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
695 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 4:109714341:T:TA | donor_gain | 1.0000 |
| 4:109717542:CCTTA:C | donor_loss | 1.0000 |
| 4:109717543:CTTA:C | donor_loss | 1.0000 |
| 4:109717544:TTACC:T | donor_loss | 1.0000 |
| 4:109717545:TA:T | donor_loss | 1.0000 |
| 4:109717546:A:AT | donor_loss | 1.0000 |
| 4:109717546:AC:A | donor_gain | 1.0000 |
| 4:109717547:CC:C | donor_gain | 1.0000 |
| 4:109717709:TTAAG:T | acceptor_gain | 1.0000 |
| 4:109717710:TAAG:T | acceptor_gain | 1.0000 |
| 4:109717714:C:CC | acceptor_gain | 1.0000 |
| 4:109718681:A:AC | donor_gain | 1.0000 |
| 4:109718682:C:CC | donor_gain | 1.0000 |
| 4:109729617:A:AC | donor_gain | 1.0000 |
| 4:109729618:C:CC | donor_gain | 1.0000 |
| 4:109729631:T:TA | donor_gain | 1.0000 |
| 4:109714492:CATG:C | acceptor_gain | 0.9900 |
| 4:109717682:CACTT:C | acceptor_gain | 0.9900 |
| 4:109717686:T:C | acceptor_gain | 0.9900 |
| 4:109717690:C:CT | acceptor_gain | 0.9900 |
| 4:109718661:T:C | donor_gain | 0.9900 |
| 4:109718684:TGAAC:T | donor_gain | 0.9900 |
| 4:109729597:CTCAC:C | donor_loss | 0.9900 |
| 4:109729598:TCACC:T | donor_loss | 0.9900 |
| 4:109729600:ACCG:A | donor_loss | 0.9900 |
| 4:109729601:CCG:C | donor_gain | 0.9900 |
| 4:109729636:G:A | donor_gain | 0.9900 |
| 4:109714494:TG:T | acceptor_gain | 0.9800 |
| 4:109714496:C:CC | acceptor_gain | 0.9800 |
| 4:109717546:A:AC | donor_gain | 0.9800 |
AlphaMissense
1230 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 4:109717636:C:A | K121N | 0.998 |
| 4:109717636:C:G | K121N | 0.998 |
| 4:109714436:A:C | Y171D | 0.997 |
| 4:109717616:A:C | F128C | 0.997 |
| 4:109717627:A:C | C124W | 0.997 |
| 4:109717628:C:A | C124F | 0.997 |
| 4:109717628:C:T | C124Y | 0.997 |
| 4:109717679:C:G | C107S | 0.997 |
| 4:109717679:C:T | C107Y | 0.997 |
| 4:109717680:A:T | C107S | 0.997 |
| 4:109718708:C:G | C87S | 0.997 |
| 4:109718709:A:T | C87S | 0.997 |
| 4:109729622:C:G | C63S | 0.997 |
| 4:109729623:A:T | C63S | 0.997 |
| 4:109714422:T:A | Q175H | 0.996 |
| 4:109714422:T:G | Q175H | 0.996 |
| 4:109714444:C:G | C168S | 0.996 |
| 4:109714445:A:T | C168S | 0.996 |
| 4:109717628:C:G | C124S | 0.996 |
| 4:109717629:A:T | C124S | 0.996 |
| 4:109717661:C:G | C113S | 0.996 |
| 4:109717662:A:T | C113S | 0.996 |
| 4:109717682:C:G | C106S | 0.996 |
| 4:109717683:A:G | C106R | 0.996 |
| 4:109717683:A:T | C106S | 0.996 |
| 4:109718709:A:G | C87R | 0.996 |
| 4:109714492:C:G | C152S | 0.995 |
| 4:109714492:C:T | C152Y | 0.995 |
| 4:109714493:A:T | C152S | 0.995 |
| 4:109717592:C:G | C136S | 0.995 |
dbSNP variants (sampled 300 via entrez): RS1000067548 (4:109711432 T>A,C), RS1000161169 (4:109718584 T>G), RS1000179770 (4:109712775 T>C), RS10004377 (4:109726968 G>A,C,T), RS1000548245 (4:109731721 AC>A), RS1000842685 (4:109725250 T>C,G), RS1001224666 (4:109729050 A>T), RS1001245827 (4:109709952 A>G), RS1001511511 (4:109724431 T>A,C), RS1001614234 (4:109716594 T>C), RS1001730303 (4:109716954 C>A,T), RS1001894260 (4:109722215 T>C), RS1001946508 (4:109716539 G>A,C), RS1001954142 (4:109714832 T>A,C), RS1002009933 (4:109724165 G>T)
Disease associations
OMIM: gene MIM:611652 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006611_118 | HDL cholesterol | 2.000000e-08 |
| GCST006613_27 | Triglycerides | 1.000000e-12 |
| GCST012232_11 | Lipoprotein (a) levels | 1.000000e-11 |
| GCST90002397_19 | Mean spheric corpuscular volume | 4.000000e-11 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004612 | high density lipoprotein cholesterol measurement |
| EFO:0004530 | triglyceride measurement |
| EFO:0006925 | lipoprotein A measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4524005 (PROTEIN FAMILY), CHEMBL6122 (SINGLE PROTEIN)
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
ChEMBL bioactivities
8 potent at pChembl≥5 of 9 total, top 8 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.25 | IC50 | 56 | nM | CHEMBL4593409 |
| 6.94 | IC50 | 114 | nM | VARESPLADIB |
| 6.88 | IC50 | 131 | nM | VARESPLADIB |
| 6.08 | IC50 | 840 | nM | CHEMBL5194852 |
| 6.04 | IC50 | 910 | nM | CHEMBL5200953 |
| 5.85 | IC50 | 1410 | nM | CHEMBL5179709 |
| 5.59 | IC50 | 2580 | nM | CHEMBL5207115 |
| 5.42 | IC50 | 3810 | nM | CHEMBL5203236 |
PubChem BioAssay actives
9 with measured affinity, of 43 total; 7 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-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 |
| 3-[(2E)-2-[(3-methoxyphenyl)methylidene]hydrazinyl]-1H-quinoxalin-2-one | 1859296: Inhibition of human PLA2G12A | ic50 | 0.8400 | uM |
| 1-(2,4-dihydroxyphenyl)-5H-pyrrolo[1,2-a]quinoxalin-4-one | 1859296: Inhibition of human PLA2G12A | ic50 | 0.9100 | uM |
| 1-(3,4-dichlorophenyl)-5H-pyrrolo[1,2-a]quinoxalin-4-one | 1859296: Inhibition of human PLA2G12A | ic50 | 1.4100 | uM |
| 1-(2,4-dinitrophenyl)-5H-pyrrolo[1,2-a]quinoxalin-4-one | 1859296: Inhibition of human PLA2G12A | ic50 | 2.5800 | uM |
| 3-[(2E)-2-(thiophen-2-ylmethylidene)hydrazinyl]-1H-quinoxalin-2-one | 1859296: Inhibition of human PLA2G12A | ic50 | 3.8100 | uM |
CTD chemical–gene interactions
30 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects expression, affects cotreatment, increases expression | 9 |
| mono-(2-ethylhexyl)phthalate | increases methylation, decreases expression, increases abundance | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| methylmercuric chloride | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | affects cotreatment, decreases methylation | 1 |
| trichostatin A | increases expression | 1 |
| cobaltous chloride | decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| abrine | decreases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| Sunitinib | increases expression | 1 |
| Fulvestrant | affects cotreatment, decreases methylation | 1 |
| Acetaminophen | increases expression | 1 |
| Carbamazepine | affects expression | 1 |
| Dichlorodiphenyl Dichloroethylene | increases expression | 1 |
| Diclofenac | affects expression | 1 |
| Diethylhexyl Phthalate | increases abundance, increases methylation | 1 |
| Estradiol | increases expression | 1 |
| Hydrogen Peroxide | increases expression | 1 |
| Lead | affects expression | 1 |
| Methotrexate | increases expression | 1 |
| Selenium | affects cotreatment, decreases expression | 1 |
| Thiram | decreases expression | 1 |
| Tretinoin | increases expression | 1 |
| Vitamin E | affects cotreatment, decreases expression | 1 |
| Cyclosporine | increases expression | 1 |
| Antirheumatic Agents | increases expression | 1 |
| Copper Sulfate | decreases expression | 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 |
|---|---|---|---|
| CHEMBL4383327 | Binding | Inhibition of human sPLA2 | 1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio. — Eur J Med Chem |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2B0 | Abcam HeLa PLA2G12A KO | Cancer cell line | Female |
| CVCL_TE05 | HAP1 PLA2G12A (-) 1 | Cancer cell line | Male |
| CVCL_TE06 | HAP1 PLA2G12A (-) 2 | Cancer cell line | Male |
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.