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PLA2G1B

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Summary

PLA2G1B (phospholipase A2 group IB, HGNC:9030) is a protein-coding gene on chromosome 12q24.31, encoding Phospholipase A2 (P04054). Secretory calcium-dependent phospholipase A2 that primarily targets dietary phospholipids in the intestinal tract.

This gene encodes a secreted member of the phospholipase A2 (PLA2) class of enzymes, which is produced by the pancreatic acinar cells. The encoded calcium-dependent enzyme catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to release arachidonic acid (AA) and lysophospholipids. AA is subsequently converted by downstream metabolic enzymes to several bioactive lipophilic compounds (eicosanoids), including prostaglandins (PGs) and leukotrienes (LTs). The enzyme may be involved in several physiological processes including cell contraction, cell proliferation and pathological response.

Source: NCBI Gene 5319 — RefSeq curated summary.

At a glance

  • GWAS associations: 1
  • Clinical variants (ClinVar): 22 total
  • Druggable target: yes — 6 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_000928

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9030
Approved symbolPLA2G1B
Namephospholipase A2 group IB
Location12q24.31
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000170890
Ensembl biotypeprotein_coding
OMIM172410
Entrez5319

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000308366, ENST00000423423, ENST00000549767

RefSeq mRNA: 1 — MANE Select: NM_000928 NM_000928

CCDS: CCDS9195

Canonical transcript exons

ENST00000308366 — 4 exons

ExonStartEnd
ENSE00001129471120324934120325061
ENSE00001129475120325861120326020
ENSE00002273546120327720120327779
ENSE00002397040120322115120322317

Expression profiles

Bgee: expression breadth ubiquitous, 166 present calls, max score 99.97.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 69.5813 / max 116611.9637, expressed in 37 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
13363968.689237
1336360.44443
1336380.41183
1336370.03594

Top tissues by expression

291 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
body of pancreasUBERON:000115099.97gold quality
pancreasUBERON:000126499.38gold quality
islet of LangerhansUBERON:000000699.37gold quality
type B pancreatic cellCL:000016998.74gold quality
lower lobe of lungUBERON:000894993.35gold quality
epithelial cell of pancreasCL:000008392.81gold quality
spermCL:000001992.06gold quality
male germ cellCL:000001588.44gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047387.49gold quality
upper lobe of lungUBERON:000894885.14gold quality
right lungUBERON:000216784.70gold quality
upper lobe of left lungUBERON:000895284.44gold quality
lungUBERON:000204882.06gold quality
left ovaryUBERON:000211978.88gold quality
right adrenal glandUBERON:000123378.70gold quality
left adrenal glandUBERON:000123478.46gold quality
left adrenal gland cortexUBERON:003582577.82gold quality
right adrenal gland cortexUBERON:003582777.18gold quality
right lobe of liverUBERON:000111477.10gold quality
body of stomachUBERON:000116177.05gold quality
right ovaryUBERON:000211876.80gold quality
ectocervixUBERON:001224976.56gold quality
right coronary arteryUBERON:000162576.26gold quality
adrenal cortexUBERON:000123575.57gold quality
adrenal glandUBERON:000236974.65gold quality
adrenal tissueUBERON:001830374.59gold quality
ovaryUBERON:000099274.11gold quality
right uterine tubeUBERON:000130273.31gold quality
left uterine tubeUBERON:000130372.98gold quality
descending thoracic aortaUBERON:000234572.80gold quality

Single-cell (SCXA)

Detected in 7 experiment(s), a significant marker in 6.

ExperimentMarker?Max mean expression
E-GEOD-81547yes12366.11
E-HCAD-1yes75.07
E-MTAB-5061yes21.09
E-ENAD-27yes7.54
E-HCAD-31yes4.47
E-GEOD-83139no2.98
E-ANND-3no0.00

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 17)

  • stimulation of three isoforms of PLA2 by thapsigargin liberates free AA that, in turn, induces capacitative calcium influx in human T-cells (PMID:12423354)
  • results indicate a selective sorting of a cell-derived cPLA2 during human cytomegalovirus maturation, which is further required for infectivity (PMID:15220446)
  • Group IB phospholipase A2 (PLA2G1B) stimulates leukotriene B4 (LTB4) production in the absence of cytochalasin B in human neutrophils. (PMID:16005851)
  • Here, we report sPLA2-IB in rat and human brain as well as in neurons in primary culture. The distribution of sPLA2-IB seems to be mainly neuronal, with the highest abundance occurring in the cerebral cortex and hippocampus. (PMID:16392040)
  • a critical regulatory role of arachidonate reacylation that limits leukotriene biosynthesis in concert with 5-lipoxygenase and cytosolic phospholipase A(2)alpha activation (PMID:16495221)
  • Results describe the structural basis for bile salt inhibition of pancreatic phospholipase A2. (PMID:17434532)
  • MMP-2/9 production is regulated by sPLA2-IB acting as a receptor ligand to activate cPLA2 (PMID:17981679)
  • pro-hG1B forms a trimer and PROP occupies the catalytic cavity and can be self-cleaved at 37 degrees C; A new membrane-bound surface and activation mechanism are proposed based on the trimeric model of pro-hG1B (PMID:19297324)
  • Exogenously added sPLA(2)-IB decreases phagocytosis of photoreceptor outer segments regardless of enzymatic activity. (PMID:22680611)
  • TNF-alpha-induced cPLA2 expression and PGE2 release were mediated through a Jak2/PDGFR/PI3K/Akt/p42/p44 MAPK/Elk-1 pathway in human lung epithelial cells. (PMID:24441870)
  • The sPLA2 IB-PLA2R interaction stimulated podocyte apoptosis through activating ERK1/2 and cPLA2alpha and through increasing the podocyte AA content (PMID:25335547)
  • sPLA2-IB was correlated with the level of proteinuria in membranous nephropathy patients suggesting to be a potential biomarker for monitoring disease severity and therapeutic effects of both primary membranous nephropathy and secondary membranous nephropathy. (PMID:29649452)
  • PLA2G1B is involved in CD4 anergy and CD4 lymphopenia in HIV-infected patients. (PMID:32436864)
  • sPLA2-IB Level Correlates with Hyperlipidemia and the Prognosis of Idiopathic Membranous Nephropathy. (PMID:32862379)
  • sPLA2-IB and PLA2R mediate insufficient autophagy and contribute to podocyte injury in idiopathic membranous nephropathy by activation of the p38MAPK/mTOR/ULK1(ser757) signaling pathway. (PMID:33184968)
  • Genetic analysis of pancreatic phospholipase A2 (PLA2G1B) in patients with chronic pancreatitis. (PMID:35031208)
  • Microbial Protein Binding to gC1qR Drives PLA2G1B-Induced CD4 T-Cell Anergy. (PMID:35392090)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_reriopla2g1bENSDARG00000009153
mus_musculusPla2g1bENSMUSG00000029522
rattus_norvegicusPla2g1bENSRNOG00000001153
caenorhabditis_elegansWBGENE00007419
caenorhabditis_elegansWBGENE00015406

Paralogs (8): PLA2G10 (ENSG00000069764), PLA2G2D (ENSG00000117215), PLA2G5 (ENSG00000127472), PLA2G2F (ENSG00000158786), PLA2G2C (ENSG00000187980), PLA2G2A (ENSG00000188257), PLA2G2E (ENSG00000188784), OC90 (ENSG00000253117)

Protein

Protein identifiers

Phospholipase A2 — P04054 (reviewed: P04054)

Alternative names: Group IB phospholipase A2, Phosphatidylcholine 2-acylhydrolase 1B

All UniProt accessions (3): P04054, F8W062, Q9BS22

UniProt curated annotations — full annotation on UniProt →

Function. Secretory calcium-dependent phospholipase A2 that primarily targets dietary phospholipids in the intestinal tract. Hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) with preference for phosphatidylethanolamines and phosphatidylglycerols over phosphatidylcholines. May play a role in the biosynthesis of N-acyl ethanolamines that regulate energy metabolism and inflammation in the intestinal tract. Hydrolyzes N-acyl phosphatidylethanolamines to N-acyl lysophosphatidylethanolamines, which are further cleaved by a lysophospholipase D to release N-acyl ethanolamines. May act in an autocrine and paracrine manner. Upon binding to the PLA2R1 receptor can regulate podocyte survival and glomerular homeostasis. Has anti-helminth activity in a process regulated by gut microbiota. Upon helminth infection of intestinal epithelia, directly affects phosphatidylethanolamine contents in the membrane of helminth larvae, likely controlling an array of phospholipid-mediated cellular processes such as membrane fusion and cell division while providing for better immune recognition, ultimately reducing larvae integrity and infectivity.

Subunit / interactions. The inactive pro-form is a homotrimer. When anchored into the cell membrane, the inactive homotrimer is likely cleaved either by trypsin or by itself, producing an active trimer. The resulting conformational changes are thought to open up a center hole forming a channel for substrate entry. Interacts with PLA2R1; this interaction mediates intracellular signaling as well as clearance of extracellular PLA2G1B via endocytotic pathway.

Subcellular location. Secreted.

Tissue specificity. Selectively expressed in pancreas, lung, liver and kidney. Also detected at lower levels in ovary and testis.

Post-translational modifications. Activated by trypsin cleavage in the duodenum. Can also be activated by thrombin or autocatalytically.

Activity regulation. Regulated by bile acid salts. Up-regulated by cholate and down-regulated by taurochenodeoxycholate. Cholate-activated rate of hydrolysis is lowered by hypolipidemic drug ezetimibe.

Cofactor. Binds 1 Ca(2+) ion per subunit.

Similarity. Belongs to the phospholipase A2 family.

RefSeq proteins (1): NP_000919* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001211PLA2Family
IPR016090PLA2-like_domDomain
IPR033112PLA2_Asp_ASActive_site
IPR033113PLA2_histidineActive_site
IPR036444PLipase_A2_dom_sfHomologous_superfamily

Pfam: PF00068

Catalyzed reactions (Rhea), 9 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-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40427)
  • 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)
  • 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:41223)
  • N-hexadecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + H2O = N-hexadecanoyl-1-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + (9Z)-octadecenoate + H(+) (RHEA:45424)
  • 1,2-ditetradecanoyl-sn-glycero-3-phosphocholine + H2O = 1-tetradecanoyl-sn-glycero-3-phosphocholine + tetradecanoate + H(+) (RHEA:54456)
  • N,1-dihexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = N,1-dihexadecanoyl-sn-glycero-3-phosphoethanolamine + (9Z,12Z)-octadecadienoate + H(+) (RHEA:56424)

UniProt features (36 total): helix 9, disulfide bond 7, strand 4, binding site 4, sequence variant 3, turn 3, active site 2, signal peptide 1, propeptide 1, sequence conflict 1, chain 1

Structure

Experimental structures (PDB)

2 structures.

PDBMethodResolution (Å)
3ELOX-RAY DIFFRACTION1.55
6Q42X-RAY DIFFRACTION1.9

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P04054-F188.970.74

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): 70; 121

Ligand- & substrate-binding residues (4): 50; 52; 54; 71

Disulfide bonds (7): 49–146, 51–67, 66–127, 73–120, 83–113, 106–118, 33–99

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

IDPathway
R-HSA-1482788Acyl chain remodelling of PC
R-HSA-1482801Acyl chain remodelling of PS
R-HSA-1482839Acyl chain remodelling of PE
R-HSA-1482922Acyl chain remodelling of PI
R-HSA-1482925Acyl chain remodelling of PG
R-HSA-1483166Synthesis of PA
R-HSA-9925561Developmental Lineage of Pancreatic Acinar Cells

MSigDB gene sets: 259 (showing top): GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_CARBOHYDRATE_TRANSPORT, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_REGULATION_OF_EPITHELIAL_CELL_APOPTOTIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_ANTIMICROBIAL_HUMORAL_RESPONSE, HNF3ALPHA_Q6, GOBP_MYELOID_LEUKOCYTE_MIGRATION, GOBP_CELL_CHEMOTAXIS, GOBP_POSITIVE_REGULATION_OF_INTERLEUKIN_8_PRODUCTION, KEGG_MAPK_SIGNALING_PATHWAY, GOBP_POSITIVE_REGULATION_OF_FIBROBLAST_PROLIFERATION, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE

GO Biological Process (28): innate immune response in mucosa (GO:0002227), neutrophil mediated immunity (GO:0002446), fatty acid biosynthetic process (GO:0006633), actin filament organization (GO:0007015), signal transduction (GO:0007165), positive regulation of cell population proliferation (GO:0008284), positive regulation of calcium ion transport into cytosol (GO:0010524), lipid catabolic process (GO:0016042), leukotriene biosynthetic process (GO:0019370), antibacterial humoral response (GO:0019731), neutrophil chemotaxis (GO:0030593), positive regulation of interleukin-8 production (GO:0032757), cellular response to insulin stimulus (GO:0032869), intracellular signal transduction (GO:0035556), positive regulation of MAPK cascade (GO:0043410), positive regulation of transcription by RNA polymerase II (GO:0045944), regulation of D-glucose import across plasma membrane (GO:0046324), phosphatidylcholine metabolic process (GO:0046470), phosphatidylglycerol metabolic process (GO:0046471), positive regulation of fibroblast proliferation (GO:0048146), arachidonate secretion (GO:0050482), positive regulation of protein secretion (GO:0050714), positive regulation of immune response (GO:0050778), defense response to Gram-positive bacterium (GO:0050830), antimicrobial humoral immune response mediated by antimicrobial peptide (GO:0061844), positive regulation of podocyte apoptotic process (GO:1904635), lipid metabolic process (GO:0006629), phospholipid metabolic process (GO:0006644)

GO Molecular Function (9): A2-type glycerophospholipase activity (GO:0004623), signaling receptor binding (GO:0005102), calcium ion binding (GO:0005509), phospholipid binding (GO:0005543), bile acid binding (GO:0032052), obsolete calcium-dependent phospholipase A2 activity (GO:0047498), protein binding (GO:0005515), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (3): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), cell surface (GO:0009986)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Glycerophospholipid biosynthesis6
Developmental Cell Lineages of the Exocrine Pancreas1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
glycerophospholipid metabolic process2
cellular anatomical structure2
mucosal immune response1
innate immune response1
myeloid leukocyte mediated immunity1
fatty acid metabolic process1
lipid biosynthetic process1
monocarboxylic acid biosynthetic process1
actin cytoskeleton organization1
supramolecular fiber organization1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
cell population proliferation1
regulation of cell population proliferation1
positive regulation of cellular process1
positive regulation of cytosolic calcium ion concentration1
regulation of calcium ion transport into cytosol1
calcium ion transport into cytosol1
positive regulation of calcium ion transmembrane transport1
lipid metabolic process1
catabolic process1
leukotriene metabolic process1
icosanoid biosynthetic process1
antimicrobial humoral response1
defense response to bacterium1
granulocyte chemotaxis1
neutrophil migration1
positive regulation of cytokine production1
interleukin-8 production1
regulation of interleukin-8 production1
response to insulin1
cellular response to peptide hormone stimulus1
intracellular anatomical structure1
signal transduction1
MAPK cascade1
regulation of MAPK cascade1
positive regulation of intracellular signal transduction1

Protein interactions and networks

STRING

852 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PLA2G1BPLA2R1Q13018884
PLA2G1BPLA2G4AP47712814
PLA2G1BP2RX4Q99571782
PLA2G1BLYNX1P0DP58637
PLA2G1BPNLIPP16233621
PLA2G1BPNLIPRP1P54315606
PLA2G1BPTGISQ16647593
PLA2G1BPLA2G7Q13093579
PLA2G1BPLA2G12BQ9BX93557
PLA2G1BCELP19835553
PLA2G1BENPP2Q13822552
PLA2G1BPLA2G6O60733550
PLA2G1BPLA2G12AQ9BZM1542
PLA2G1BCYP4A11Q02928518
PLA2G1BPLA2G10O15496506
PLA2G1BSERPINI2O75830506

IntAct

3 interactions, top by confidence:

ABTypeScore
SOCS2PLA2G1Bpsi-mi:“MI:0915”(physical association)0.370
PLA2G1BKLHL22psi-mi:“MI:0914”(association)0.350

BioGRID (7): PLA2G2A (Reconstituted Complex), PLA2G1B (Affinity Capture-MS), HSP90AB4P (Affinity Capture-MS), UBR3 (Affinity Capture-MS), KLHL22 (Affinity Capture-MS), PLA2G1B (Positive Genetic), SOCS2 (Two-hybrid)

ESM2 similar proteins: A8CG90, F8QN51, F8QN53, O42187, P00592, P00593, P00594, P04054, P04055, P04056, P04416, P04417, P06596, P0DJN7, P11407, P14419, P14421, P14423, P14424, P14555, P20255, P20256, P20258, P20259, P24293, P34180, P43434, P59170, P59172, P81236, P81237, Q1ZY03, Q2YHJ2, Q2YHJ7, Q6EER3, Q6EER4, Q6EER5, Q6EER6, Q71QE8, Q7M334

Diamond homologs: A4FS04, A6MEY4, C0HKB8, C0HKB9, C1IC45, C1IC46, F5CPF1, F8J2D0, P00592, P00593, P00595, P00596, P00597, P00598, P00599, P00600, P00601, P00602, P00603, P00604, P00605, P00606, P00608, P00616, P00627, P00628, P00629, P04054, P04055, P04416, P06596, P07037, P08873, P0C551, P14411, P14419, P14556, P14615, P15445, P17934

SIGNOR signaling

2 interactions.

AEffectBMechanism
GRPRup-regulatesPLA2G1Bbinding
Varespladibdown-regulatesPLA2G1B“chemical inhibition”

Disease & clinical

Clinical variants and AI predictions

ClinVar

22 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance20
Likely benign1
Benign1

Top pathogenic / likely-pathogenic (0)

SpliceAI

346 predictions. Top by Δscore:

VariantEffectΔscore
12:120324930:CTA:Cdonor_loss1.0000
12:120324931:TACTG:Tdonor_loss1.0000
12:120324932:A:ACdonor_gain1.0000
12:120324933:C:CAdonor_gain1.0000
12:120324933:CT:Cdonor_gain1.0000
12:120324933:CTG:Cdonor_gain1.0000
12:120324933:CTGCT:Cdonor_gain1.0000
12:120324934:TGC:Tdonor_gain1.0000
12:120325856:CTTA:Cdonor_gain1.0000
12:120325857:TTA:Tdonor_loss1.0000
12:120325858:TA:Tdonor_loss1.0000
12:120325859:A:ACdonor_gain1.0000
12:120325860:C:CTdonor_gain1.0000
12:120325860:CT:Cdonor_gain1.0000
12:120325860:CTT:Cdonor_gain1.0000
12:120325860:CTTG:Cdonor_gain1.0000
12:120325860:CTTGT:Cdonor_gain1.0000
12:120326016:GGCCA:Gacceptor_gain1.0000
12:120326017:GCCA:Gacceptor_gain1.0000
12:120326018:CCA:Cacceptor_gain1.0000
12:120326018:CCAC:Cacceptor_gain1.0000
12:120326019:CA:Cacceptor_gain1.0000
12:120326019:CAC:Cacceptor_gain1.0000
12:120326020:ACTG:Aacceptor_loss1.0000
12:120326021:C:CCacceptor_gain1.0000
12:120326021:C:Tacceptor_loss1.0000
12:120326024:C:CTacceptor_gain1.0000
12:120322314:TTGC:Tacceptor_gain0.9900
12:120322318:C:CCacceptor_gain0.9900
12:120324928:ACCT:Adonor_loss0.9900

AlphaMissense

980 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
12:120325865:C:GD64H0.996
12:120322275:C:GR122P0.995
12:120322287:C:GC118S0.995
12:120322288:A:TC118S0.995
12:120322278:T:AD121V0.994
12:120322278:T:GD121A0.994
12:120325056:C:GC67S0.994
12:120325057:A:TC67S0.994
12:120325038:C:GC73S0.993
12:120325039:A:TC73S0.993
12:120325056:C:TC67Y0.993
12:120325903:C:GC51S0.993
12:120325904:A:TC51S0.993
12:120325913:C:AG48C0.993
12:120322287:C:TC118Y0.992
12:120325864:T:AD64V0.992
12:120322287:C:AC118F0.991
12:120325055:G:CC67W0.991
12:120325903:C:TC51Y0.991
12:120322267:C:GA125P0.990
12:120322279:C:GD121H0.990
12:120322281:C:AC120F0.990
12:120322281:C:GC120S0.990
12:120322281:C:TC120Y0.990
12:120322282:A:TC120S0.990
12:120322286:G:CC118W0.990
12:120325864:T:GD64A0.990
12:120325874:C:GD61H0.990
12:120325912:C:AG48V0.990
12:120325912:C:TG48D0.990

dbSNP variants (sampled 300 via entrez): RS1000190054 (12:120329238 C>G), RS1000675828 (12:120321759 C>G,T), RS1000808358 (12:120328988 T>TA), RS1000831627 (12:120327928 T>A), RS1000963775 (12:120327411 G>A), RS1001496198 (12:120324870 T>C), RS1002677238 (12:120325789 G>A,C), RS1003188449 (12:120323446 A>C,G), RS1004225717 (12:120325157 G>A,T), RS1004323596 (12:120325359 C>T), RS1004491360 (12:120327003 G>A), RS1004860438 (12:120321970 G>A,C), RS1004956763 (12:120321800 G>A), RS1005284758 (12:120326617 A>C,G), RS1005426749 (12:120328205 C>G,T)

Disease associations

OMIM: gene MIM:172410 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

1 associations (top):

StudyTraitp-value
GCST008103_87Bipolar disorder1.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4426 (SINGLE PROTEIN), CHEMBL4524005 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 144,718 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL272427TAURURSODIOL44,753
CHEMBL277535BIFONAZOLE412,513
CHEMBL50QUERCETIN374,559
CHEMBL121626TOLFENAMIC ACID220,424
CHEMBL148674VARESPLADIB2272
CHEMBL473535FENTICLOR232,197

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 (2 total), top 2:

LigandActionAffinityParameter
compound 28xvii [PMID: 8809154]Inhibition8.89pIC50
compound 12e [PMID: 18605714]Inhibition7.08pIC50

Binding affinities (BindingDB)

310 measured of 339 human assays (372 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
dexamethasone (tetramethyl-rhodamine conjugated )EC500.2 nM
hnpsPLA2-IIa Inhibitor, 2lIC5019 nM
6-bromanyl-2-(furan-2-yl)quinoline-4-carboxylic acidIC5023 nM
hnpsPLA2-IIa Inhibitor, 2bIC5029 nM
hnpsPLA2-IIa Inhibitor, 2mIC5039 nM
hnpsPLA2-IIa Inhibitor, 2kIC5057 nM
MLS000530403IC5058.8 nM
[3-(1-Benzyl-3-carbamoylmethyl-2-methyl-1H-indol-5-yloxy)-propyl]-phosphonic acidIC5060 nM
hnpsPLA2-IIa Inhibitor, 2jIC5067 nM
hnpsPLA2-IIa Inhibitor, 2pIC5086 nM
2-(benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acidEC5092 nM
hnpsPLA2-IIa Inhibitor, 2nIC50116 nM
4-chloranyl-N-(3,4-dihydro-2H-thiochromen-4-yl)-3-sulfamoyl-benzamideIC50121 nM
hnpsPLA2-IIa Inhibitor, 2oIC50170 nM
hnpsPLA2-IIa Inhibitor, 2hIC50214 nM
hnpsPLA2-IIa Inhibitor, 2iIC50247 nM
4-[2-(2-cyclohexyl-5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)sulfanylacetyl]-1,3-dihydroquinoxalin-2-oneIC50316 nM
7-Ethyl-5-(4-nitro-phenyl)-2-phenyl-3H-benzo[e][1,2,4]triazepineIC50399 nM
SMR000255593IC50502 nM
4-[(E)-[3-(2-methylanilino)-4-oxo-1-naphthalenylidene]amino]sulfonylbenzoic acidIC50522 nM
4-[(2,5-dichlorophenoxy)methyl]-N-[3,5-dimethyl-1-[(2,3,4,5,6-pentafluorophenyl)methyl]-4-pyrazolyl]benzamideIC50532 nM
hnpsPLA2-IIa Inhibitor, 2gIC50536 nM
hnpsPLA2-IIa Inhibitor, 2aIC50662 nM
hnpsPLA2-IIa Inhibitor, 2fIC50761 nM
SMR000200958IC50870 nM
4-({(4Z)-1-oxo-4-[(phenylsulfonyl)imino]-1,4-dihydronaphthalen-2-yl}amino)benzoic acidIC50967 nM
2-[(2-fluorobenzyl)thio]-5-(4-methylphenyl)-1,3,4-oxadiazoleEC501140 nM
SMR000516584IC501270 nM
1-ethyl-6-methyl-3-[(E)-2-phenylethenyl]pyrimido[5,4-e][1,2,4]triazine-5,7-dioneEC501440 nM
(4E)-4-(1,3-benzodioxol-5-ylhydrazinylidene)-5-imino-1-phenyl-3-pyrazolamineEC501600 nM
1,3,6-Trimethyl-1H-pyrimido[5,4-e][1,2,4]triazine-5,7-dioneEC501610 nM
SMR000236924IC501620 nM
3-[[(E)-(3-methyl-5-nitro-6-oxidanylidene-cyclohexa-2,4-dien-1-ylidene)methyl]amino]-2-(phenoxymethyl)quinazolin-4-oneIC501640 nM
1,6-dimethyl-3-propyl-pyrimido[5,4-e][1,2,4]triazine-5,7-dioneEC501770 nM
(1Z)-1-[[2-[4-(1H-imidazol-2-yl)phthalazin-1-yl]hydrazinyl]methylidene]naphthalen-2-oneEC501960 nM
MLS002608219IC502020 nM
3-[[anilino(oxo)methyl]amino]-5-phenyl-2-thiophenecarboxylic acid ethyl esterEC502160 nM
(6E)-2-(2-furanyl)-5-imino-6-[[1-(4-methoxyphenyl)-2-pyrrolyl]methylidene]-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-oneIC502270 nM
(E)-4-(1,3-benzothiazol-2-yl)-5-[4-(N-methylanilino)-3-nitro-phenyl]pent-4-enoic acidIC502270 nM
4-[(3aR,4S,9bS)-8-[(4-methoxyphenyl)sulfamoyl]-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]benzoic acidEC502280 nM
MLS000537883IC502360 nM
2-[[5-[(4-chlorophenoxy)methyl]-4-(2-furanylmethyl)-1,2,4-triazol-3-yl]thio]-1-(2-fluorophenyl)ethanoneIC502360 nM
4-bromobenzoic acid [2-(3,5-dimethoxyphenyl)-4-oxo-3-quinazolinyl] esterIC502510 nM
2-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-(3-ethoxy-4-hydroxybenzylidene)-5-phenyl-2,4-dihydro-3H-pyrazol-3-oneIC502540 nM
2-chloranyl-4-[5-[(1-oxidanylidene-[1,3]thiazolo[3,2-a]benzimidazol-2-ylidene)methyl]furan-2-yl]benzoic acidIC502890 nM
3-(4-Biphenyl-4-yl-thiazol-2-ylamino)-6,7-dimethoxy-3H-isobenzofuran-1-oneEC502980 nM
4-({4-[5-(2-methyl-3-phenyl-2-propen-1-ylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]butanoyl}amino)benzoic acidEC502980 nM
4-[(5Z)-4-keto-5-[(E)-2-methyl-3-phenyl-prop-2-enylidene]-2-thioxo-thiazolidin-3-yl]benzoic acidIC503090 nM
MLS000778639IC503100 nM
1,8-bis(azanyl)-3,6-dipyrrolidin-1-yl-2,7-naphthyridine-4-carbonitrileIC503170 nM

ChEMBL bioactivities

341 potent at pChembl≥5 of 493 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.89IC501.3nMCHEMBL331755
8.85IC501.4nMCHEMBL121627
8.52IC503nMCHEMBL332993
8.52IC503nMCHEMBL332547
8.52IC503nMCHEMBL120112
8.52IC503nMCHEMBL121245
8.38IC504.2nMCHEMBL332957
8.30IC505nMCHEMBL121617
8.30IC505nMCHEMBL123774
8.30IC505nMCHEMBL121609
8.22IC506nMCHEMBL331755
8.22IC506nMCHEMBL332993
8.22IC506nMCHEMBL121645
8.22IC506nMCHEMBL121245
8.14IC507.3nMCHEMBL121422
8.10IC508nMCHEMBL121627
8.10IC508nMCHEMBL121617
8.10IC508nMCHEMBL332547
8.05IC509nMCHEMBL332957
8.05IC509nMCHEMBL121645
8.05IC509nMCHEMBL120112
8.00IC5010nMCHEMBL123182
8.00IC5010nMCHEMBL414424
7.96IC5011nMCHEMBL123182
7.96IC5011nMCHEMBL123774
7.96IC5011nMCHEMBL122736
7.89IC5013nMCHEMBL420169
7.89IC5013nMCHEMBL332393
7.89IC5013nMCHEMBL122736
7.89IC5013nMCHEMBL123384
7.89IC5013nMCHEMBL121030
7.85IC5014nMCHEMBL330987
7.85IC5014nMCHEMBL121481
7.82IC5015nMCHEMBL420169
7.82IC5015nMCHEMBL414424
7.82IC5015nMCHEMBL121199
7.80IC5016nMCHEMBL121605
7.77IC5017nMCHEMBL121422
7.77IC5017nMCHEMBL120111
7.77IC5017nMCHEMBL123394
7.75IC5018nMCHEMBL332393
7.72IC5019nMCHEMBL334242
7.70IC5020nMCHEMBL331184
7.68IC5021nMCHEMBL120553
7.68IC5021nMCHEMBL120909
7.66IC5022nMCHEMBL330987
7.64IC5023nMCHEMBL330844
7.64IC5023nMCHEMBL332532
7.62IC5024nMCHEMBL121609
7.60IC5025nMCHEMBL331184

PubChem BioAssay actives

171 with measured affinity, of 441 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
2-[3-[(2-benzylphenyl)methyl]-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0013uM
methyl 2-[2-methyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetate158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0014uM
2-(3-benzyl-2-methyl-1-oxamoylindolizin-8-yl)oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0030uM
2-[3-[(3-chlorophenyl)methyl]-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0030uM
2-[2-ethyl-1-oxamoyl-3-[[3-(trifluoromethyl)phenyl]methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0030uM
2-[2-ethyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0030uM
methyl 2-[2-ethyl-1-oxamoyl-3-[(3-phenylphenyl)methyl]indolizin-8-yl]oxyacetate158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0042uM
2-[3-[(4-butylphenyl)methyl]-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0050uM
2-[2-ethyl-3-(naphthalen-1-ylmethyl)-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0050uM
2-(3-benzyl-2-ethyl-1-oxamoylindolizin-8-yl)oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0050uM
2-[2-cyclopropyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0060uM
2-[2-ethyl-3-(naphthalen-2-ylmethyl)-1-oxamoylindolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0073uM
2-[3-(cyclohexylmethyl)-2-methyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0100uM
2-[2-ethyl-1-oxamoyl-3-[(5-thiophen-2-ylthiophen-3-yl)methyl]indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0100uM
2-[2-ethyl-1-oxamoyl-3-(thiophen-2-ylmethyl)indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0110uM
2-[2-methoxy-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0130uM
2-[1-(2-amino-2-oxoethyl)-2-cyclopropyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0130uM
2-[2-ethyl-1-oxamoyl-3-[(4-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0130uM
2-[1-(2-amino-2-oxoethyl)-3-benzyl-2-ethylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0130uM
2-[1-(2-amino-2-oxoethyl)-2-ethyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0140uM
2-[3-(cyclopentylmethyl)-2-methyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0140uM
(2R)-3-[3-(5-benzyl-2-carbamoylphenyl)phenyl]-2-methylpropanoic acid1631141: Inhibition of sPLA2 in human HepG2 cellsic500.0140uM
2-[1-(2-amino-2-oxoethyl)-3-[(3-chlorophenyl)methyl]-2-ethylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0150uM
2-[2-methylsulfanyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0160uM
2-[2-ethyl-3-(2-methylpentyl)-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0170uM
methyl 2-[2-ethyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0170uM
2-[3-(cyclopentylmethyl)-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0190uM
(4S)-5-[4-(naphthalen-1-ylmethoxy)phenyl]-4-(7-phenylheptanoylamino)pentanoic acid1799608: In Vitro Colorimetric Enzyme Assay from Article 10.1002/cbic.200390029: “D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.”ic500.0190uM
2-[2-ethyl-1-oxamoyl-3-[[(3S)-3-pentylcyclohexyl]methyl]indolizin-8-yl]oxyacetic acid158926: Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).ic500.0200uM
2-[3-(cyclohexylmethyl)-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0210uM
2-[2-ethyl-3-[(3-methoxyphenyl)methyl]-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0210uM
2-[3-(cycloheptylmethyl)-2-ethyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0230uM
methyl 2-[2-cyclopropyl-3-(naphthalen-1-ylmethyl)-1-oxamoylindolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0230uM
2-[3-(cyclopentylmethyl)-2-cyclopropyl-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0290uM
(4S)-4-(7-phenylheptanoylamino)-5-(4-phenylmethoxyphenyl)pentanoic acid1799608: In Vitro Colorimetric Enzyme Assay from Article 10.1002/cbic.200390029: “D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.”ic500.0290uM
2-[1-carbamoyl-2-ethyl-3-(naphthalen-1-ylmethyl)indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0300uM
methyl 2-[1-oxamoyl-3-[(2-phenylphenyl)methyl]-2-propan-2-ylindolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0350uM
2-[2-ethyl-3-[(2-nitrophenyl)methyl]-1-oxamoylindolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0360uM
methyl 2-[2-ethyl-1-oxamoyl-3-[(E)-3-phenylprop-2-enyl]indolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0380uM
(4S)-5-[4-(naphthalen-2-ylmethoxy)phenyl]-4-(7-phenylheptanoylamino)pentanoic acid1799608: In Vitro Colorimetric Enzyme Assay from Article 10.1002/cbic.200390029: “D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.”ic500.0390uM
methyl 2-[3-(cyclohexylmethyl)-2-cyclopropyl-1-oxamoylindolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0430uM
3-[2-ethyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxypropanoic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0440uM
2-(3-benzyl-2-cyclopropyl-1-oxamoylindolizin-8-yl)oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0460uM
2-[2-ethyl-3-[(2-phenylphenyl)methyl]-8-(pyridin-2-ylmethoxy)indolizin-1-yl]-2-oxoacetamide158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0460uM
(E)-4-(4-octadecylphenyl)-4-oxobut-2-enoic acid1904112: Inhibition of PLA2 (unknown origin)ic500.0490uM
2-[2-ethyl-1-oxamoyl-3-(2-phenylethyl)indolizin-8-yl]oxyacetic acid158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0510uM
methyl 2-[2-ethyl-1-oxamoyl-3-(2-phenylethyl)indolizin-8-yl]oxyacetate158925: Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay.ic500.0510uM
(4S)-5-[4-(cyclopentylmethoxy)phenyl]-4-(7-phenylheptanoylamino)pentanoic acid1799608: In Vitro Colorimetric Enzyme Assay from Article 10.1002/cbic.200390029: “D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.”ic500.0570uM
3-[3-(2-amino-2-oxoethyl)-1-benzyl-2-methylindol-5-yl]oxypropylphosphonic acid1799608: In Vitro Colorimetric Enzyme Assay from Article 10.1002/cbic.200390029: “D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.”ic500.0600uM
2-[1-[(2-benzylphenyl)methyl]-2-ethyl-3-oxamoylindol-4-yl]oxyacetic acid158796: Compound was tested for inhibition of human secretory pancreatic Phospholipase A2ic500.0620uM

CTD chemical–gene interactions

26 total (human), top 26 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects methylation, decreases expression2
methyleugenoldecreases expression1
propionaldehydedecreases expression1
bisphenol Adecreases methylation1
sodium arsenitedecreases expression1
pyrrolidine dithiocarbamic aciddecreases reaction, increases expression1
vanadyl sulfateincreases expression1
1,2-bis(2-aminophenoxy)ethane N,N,N’,N’-tetraacetic acid acetoxymethyl esterincreases expression, decreases reaction, increases abundance1
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-onedecreases reaction, increases expression1
perfluoro-n-nonanoic aciddecreases expression1
U 0126affects expression, affects reaction1
quinocetoneincreases expression1
Arsenic Trioxideincreases expression1
Acetaminophendecreases expression1
Biological Factorsdecreases expression1
Calciumincreases expression, decreases reaction, increases abundance1
Cycloheximidedecreases reaction, increases expression1
Dexamethasonedecreases reaction, increases expression1
Egtazic Aciddecreases activity1
Flavonoidsdecreases expression1
Sulfasalazineincreases expression, decreases reaction1
Tetrachlorodibenzodioxindecreases reaction, increases expression1
1-Methyl-4-phenylpyridiniumaffects expression, affects reaction1
Aflatoxin B1decreases expression1
Antirheumatic Agentsdecreases expression1
Okadaic Aciddecreases expression1

ChEMBL screening assays

77 unique, capped per target: 75 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1005072BindingInhibition of PLA2 in fMLP and A23187 ionophore-stimulated human HL60 cells assessed as effect on [3H]arachidonic acid releasePhospholipase A 2 Inhibitors from an Erythrina Species from Samoa — J Nat Prod
CHEMBL1794348FunctionalPUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors in a Phospholipase A2 assay Set 2. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504462, AID504475]PubChem BioAssay data set

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 80

This page pulls from 80 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot