An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of phospholipase A2 (EC 3.1.1.4).
ChEBI ID: 50469
| Member | Definition | Class |
|---|---|---|
| 4-amylcinnamoylanthranilic acid | An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 4-pentylcinnamoyl group. It is a transient receptor potential (TRP) channel blocker and phospholipase A2 (PLA2) inhibitor. | N-(p-amylcinnamoyl)anthranilic acid |
| alminoprofen | A substituted aniline that is ibuprofen in which the isobutyl group is replaced by a (2-methylprop-2-en-1-yl)amino group. A non-steroidal anti-inflammatory drug, it is used for treatment of inflammatory and rheumatic disorders. | alminoprofen |
| arachidonyltrifluoromethane | A fatty acid derivative that is arachidonic acid in which the OH part of the carboxy group has been replaced by a trifluoromethyl group | AACOCF3 |
| benzylideneacetone | The trans-isomer of benzylideneacetone. It acts as an inhibitor of the enzyme phospholipase A2 (EC 3.1.1.4) of insects like diamond back moth. | trans-benzylideneacetone |
| berberine | berberine | |
| manoalide | A sesterterpenoid isolated from the marine sponge Luffariella variabilis and which has been shown to exhibit inhibitory activity towards phospholipase A2. | manoalide |
| ochnaflavone | A biflavonoid with an ether linkage between the B-rings of the apigenin and luteolin subunits. It has been isolated from several members of the Ochnaceae plant family. | ochnaflavone |
| papyriflavonol a | A pentahydroxyflavone that is flavone substituted with hydroxy groups at positions 3, 5, 7, 3' and 4' and prenyl groups at positions 6 and 5'. Isolated from Broussonetia papyrifera, it exhibits inhibitory activity against phospholipase A2 and tyrosinase. | papyriflavonol A |
| scalaradial | A scalarane sesterterpenoid with formula C27H40O4. It is a natural product found in the marine sponges Spongia officinalis and Cacospongia mollior, and exhibits anti-inflammatory activity. | scalaradial |
| varespladib | A member of the class of indoles that is 1H-indole substituted by benzyl, ethyl, oxamoyl, and carboxymethoxy groups at positions 1, 2, 3, and 4, respectively. It is an oral secretory phospholipase A2 inhibitor and exhibits anti-inflammatory effects. | varespladib |
| varespladib methyl | A methyl ester resulting from the formal condensation of the carboxy group of varespladib with methanol. It is a potential therapy for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s. | varespladib methyl |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 253 (5.50) | 18.7374 |
| 1990's | 417 (9.07) | 18.2507 |
| 2000's | 835 (18.16) | 29.6817 |
| 2010's | 2,007 (43.66) | 24.3611 |
| 2020's | 1,085 (23.60) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 119 (2.51%) | 5.53% |
| Reviews | 328 (6.92%) | 6.00% |
| Case Studies | 7 (0.15%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4,289 (90.43%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 32.3105 | 1 | 2 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 75.5522 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 11.5774 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 15.8489 | 1 | 1 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 6.5656 | 1 | 2 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 13.4504 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 23.9185 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 15.4034 | 2 | 4 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 95.1146 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 14.0398 | 4 | 8 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 33.1734 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 13.4504 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.2239 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 55.3055 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 19.9526 | 1 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 13.4504 | 1 | 1 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 2.5119 | 2 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 13.4504 | 1 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 10.4304 | 2 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 11.1891 | 2 | 4 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 24.1175 | 2 | 3 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 55.9334 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 6.2426 | 2 | 2 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 28.1838 | 1 | 1 |
| polyprotein | Zika virus | Potency | 33.1734 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 10.4353 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 76.9588 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 68.5896 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 75.5522 | 1 | 1 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 42.8712 | 2 | 2 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.9626 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 85/88 kDa calcium-independent phospholipase A2 | Homo sapiens (human) | IC50 | 3.0076 | 8 | 8 |
| Acetylcholinesterase | Electrophorus electricus (electric eel) | IC50 | 0.7827 | 3 | 3 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 0.4000 | 2 | 2 |
| Acidic phospholipase A2 2 | Naja naja (Indian cobra) | IC50 | 17.0000 | 1 | 1 |
| Acidic phospholipase A2 beta | Crotalus adamanteus (eastern diamondback rattlesnake) | IC50 | 0.4000 | 1 | 1 |
| Aldo-keto reductase family 1 member C2 | Homo sapiens (human) | IC50 | 6.7100 | 1 | 1 |
| Aldo-keto reductase family 1 member C3 | Homo sapiens (human) | IC50 | 4.9900 | 2 | 2 |
| Cannabinoid receptor 2 | Mus musculus (house mouse) | IC50 | 100.0000 | 1 | 1 |
| Cholinesterase | Equus caballus (horse) | IC50 | 15.2667 | 3 | 3 |
| Cholinesterase | Homo sapiens (human) | IC50 | 15.8950 | 2 | 2 |
| Cytochrome P450 1B1 | Homo sapiens (human) | IC50 | 0.9747 | 3 | 3 |
| Cytochrome P450 1B1 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| Cytosolic phospholipase A2 | Homo sapiens (human) | IC50 | 26.7250 | 4 | 4 |
| Cytosolic phospholipase A2 | Bos taurus (cattle) | IC50 | 11.0000 | 2 | 2 |
| Cytosolic phospholipase A2 beta | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| Cytosolic phospholipase A2 gamma | Homo sapiens (human) | IC50 | 0.4200 | 1 | 1 |
| DNA polymerase kappa | Homo sapiens (human) | IC50 | 4.5000 | 2 | 2 |
| Fatty-acid amide hydrolase 1 | Homo sapiens (human) | IC50 | 1.0082 | 3 | 3 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 | 3.7000 | 1 | 1 |
| Group 10 secretory phospholipase A2 | Homo sapiens (human) | IC50 | 11.1927 | 9 | 9 |
| Group 10 secretory phospholipase A2 | Mus musculus (house mouse) | IC50 | 0.0750 | 2 | 2 |
| Group 3 secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.1225 | 2 | 2 |
| Group IID secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.1017 | 3 | 3 |
| Group IID secretory phospholipase A2 | Mus musculus (house mouse) | IC50 | 0.4300 | 1 | 1 |
| Group IIE secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.0863 | 4 | 4 |
| Group IIE secretory phospholipase A2 | Mus musculus (house mouse) | IC50 | 0.0750 | 2 | 2 |
| Group IIF secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.1250 | 3 | 3 |
| Group IIF secretory phospholipase A2 | Mus musculus (house mouse) | IC50 | 1.6000 | 1 | 1 |
| Group XIIA secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.1225 | 2 | 2 |
| Group XIIB secretory phospholipase A2-like protein | Homo sapiens (human) | IC50 | 0.1225 | 2 | 2 |
| Lysine-specific histone demethylase 1A | Homo sapiens (human) | IC50 | 6.9700 | 1 | 1 |
| Maltase-glucoamylase, intestinal | Homo sapiens (human) | Ki | 2.3000 | 1 | 1 |
| Monoglyceride lipase | Homo sapiens (human) | IC50 | 6.3833 | 2 | 2 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.5000 | 1 | 1 |
| Neuraminidase | Influenza A virus (A/USSR/90/1977(H1N1)) | IC50 | 35.3500 | 2 | 2 |
| Neuraminidase | Influenza A virus (A/Puerto Rico/8/1934(H1N1)) | Ki | 14.3000 | 1 | 1 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | IC50 | 2.3000 | 1 | 1 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | IC50 | 2.3000 | 1 | 1 |
| Phenol oxidase | Plutella xylostella (diamondback moth) | IC50 | 38.3100 | 1 | 1 |
| Phosphatidylcholine 2-acylhydrolase | Apis mellifera (honey bee) | IC50 | 0.0550 | 1 | 2 |
| Phospholipase A2 | Apis mellifera (honey bee) | IC50 | 11.6962 | 8 | 8 |
| Phospholipase A2 | Homo sapiens (human) | IC50 | 3.5126 | 8 | 8 |
| Phospholipase A2 | Mus musculus (house mouse) | IC50 | 0.1400 | 2 | 2 |
| Phospholipase A2 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Phospholipase A2 group V | Homo sapiens (human) | IC50 | 0.2738 | 5 | 5 |
| Phospholipase A2 group V | Mus musculus (house mouse) | IC50 | 0.7500 | 2 | 2 |
| Phospholipase A2, major isoenzyme | Sus scrofa (pig) | IC50 | 0.0480 | 2 | 2 |
| Phospholipase A2, membrane associated | Homo sapiens (human) | IC50 | 94.6459 | 17 | 17 |
| Phospholipase A2, membrane associated | Mus musculus (house mouse) | IC50 | 0.0700 | 2 | 2 |
| Phospholipase A2, membrane associated | Rattus norvegicus (Norway rat) | IC50 | 1,019.2000 | 2 | 2 |
| Platelet-activating factor acetylhydrolase | Homo sapiens (human) | IC50 | 2.3500 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 66.0693 | 1 | 1 |
| Prolyl endopeptidase | Homo sapiens (human) | IC50 | 143.5000 | 2 | 2 |
| Putative inactive group IIC secretory phospholipase A2 | Homo sapiens (human) | IC50 | 0.1225 | 2 | 2 |
| Telomerase reverse transcriptase | Homo sapiens (human) | IC50 | 37.0000 | 1 | 1 |
| Tissue alpha-L-fucosidase | Bos taurus (cattle) | IC50 | 89.0000 | 1 | 1 |
| Transient receptor potential cation channel subfamily M member 2 | Homo sapiens (human) | IC50 | 1.5050 | 7 | 8 |
| Transient receptor potential cation channel subfamily M member 2 | Rattus norvegicus (Norway rat) | IC50 | 0.3300 | 1 | 1 |
| Transient receptor potential cation channel subfamily M member 7 | Mus musculus (house mouse) | IC50 | 0.7600 | 1 | 1 |
| Transient receptor potential cation channel subfamily M member 8 | Homo sapiens (human) | IC50 | 3.9000 | 2 | 2 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 67.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Transient receptor potential cation channel subfamily A member 1 | Homo sapiens (human) | EC50 | 28.0919 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 85/88 kDa calcium-independent phospholipase A2 | Homo sapiens (human) | XI50 | 0.0047 | 8 | 8 |
| Group 10 secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group 3 secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group IID secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group IIE secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group IIF secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group XIIA secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Group XIIB secretory phospholipase A2-like protein | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Phospholipase A2 group V | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Phospholipase A2, membrane associated | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Putative inactive group IIC secretory phospholipase A2 | Homo sapiens (human) | XI50 | 0.0010 | 7 | 7 |
| Quinone oxidoreductase | Mus musculus (house mouse) | CD | 15.0000 | 1 | 1 |
| Substance-P receptor | Cavia porcellus (domestic guinea pig) | CD | 15.0000 | 1 | 1 |