An antogonist that interferes with the action of activator protein 1 (AP-1).
ChEBI ID: 67199
| Member | Definition | Class |
|---|---|---|
| sr 11302 | A retinoid that is all-trans-retinoic acid in which the methyl group at position 9 is replaced by a 4-methylphenyl group. It is an inhibitor of activator protein-1 which exhibits antitumour effects in vivo. | SR11302 |
| tretinoin | A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | all-trans-retinoic acid |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 3,534 (15.48) | 18.7374 |
| 1990's | 6,538 (28.63) | 18.2507 |
| 2000's | 6,054 (26.51) | 29.6817 |
| 2010's | 5,295 (23.19) | 24.3611 |
| 2020's | 1,414 (6.19) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,083 (4.58%) | 5.53% |
| Reviews | 1,986 (8.39%) | 6.00% |
| Case Studies | 1,372 (5.80%) | 4.05% |
| Observational | 15 (0.06%) | 0.25% |
| Other | 19,214 (81.17%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| activating transcription factor 6 | Homo sapiens (human) | Potency | 58.2993 | 1 | 2 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 33.2214 | 1 | 4 |
| AR protein | Homo sapiens (human) | Potency | 12.4064 | 7 | 15 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 39.1150 | 2 | 3 |
| Ataxin-2 | Homo sapiens (human) | Potency | 27.4122 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 33.8078 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 31.1448 | 2 | 3 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0224 | 2 | 2 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 68.5199 | 1 | 1 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 68.5199 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 55.9470 | 2 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 8.9125 | 1 | 1 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 37.0814 | 1 | 3 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.1838 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 19.4971 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 7.4771 | 11 | 29 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 31.1877 | 2 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 11.9970 | 10 | 22 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 34.0237 | 1 | 4 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 28.3860 | 4 | 9 |
| G | Vesicular stomatitis virus | Potency | 27.5404 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 30.7051 | 2 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 9.0323 | 3 | 7 |
| GLS protein | Homo sapiens (human) | Potency | 0.2512 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 58.3079 | 1 | 2 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 0.2188 | 1 | 3 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 49.6428 | 2 | 6 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 28.1838 | 1 | 2 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 56.0456 | 2 | 4 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 0.2512 | 2 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 27.5404 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 47.2810 | 2 | 4 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 30.2021 | 2 | 8 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 7.0795 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 41.3145 | 4 | 8 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 3.2643 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 6.3903 | 1 | 3 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 24.0778 | 3 | 9 |
| Parkin | Homo sapiens (human) | Potency | 3.6626 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 0.1994 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 13.8468 | 4 | 10 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 22.1439 | 3 | 5 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 79.4328 | 1 | 2 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 42.8055 | 2 | 5 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 37.6188 | 1 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 3.9743 | 2 | 6 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 26.6795 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 11.0429 | 3 | 10 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 0.4110 | 3 | 8 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 15.3236 | 2 | 6 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 35.4813 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 23.9625 | 2 | 3 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 30.6776 | 3 | 8 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0028 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 21.3156 | 3 | 3 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 37.9117 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 67.8334 | 1 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 39.0581 | 1 | 3 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 0.2188 | 1 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 10 kDa chaperonin | Escherichia coli | IC50 | 13.8500 | 2 | 2 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 0.3580 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.2280 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli K-12 | IC50 | 250.0000 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli | IC50 | 13.8500 | 2 | 2 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 5.2750 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 2.9820 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 5.2750 | 1 | 1 |
| Alpha-1A adrenergic receptor | Bos taurus (cattle) | Ki | 0.0004 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.7458 | 2 | 4 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 5.2750 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.7458 | 2 | 4 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 3 |
| Alpha-synuclein | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| Amyloid-beta precursor protein | Homo sapiens (human) | IC50 | 0.1800 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 71.5000 | 2 | 2 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cellular retinoic acid-binding protein 1 | Gallus gallus (chicken) | IC50 | 0.5233 | 3 | 3 |
| Chain A, Nuclear Receptor ROR-beta | Rattus norvegicus (Norway rat) | Ki | 0.2800 | 1 | 1 |
| Indoleamine 2,3-dioxygenase 1 | Mus musculus (house mouse) | IC50 | 301.3000 | 1 | 1 |
| Indoleamine 2,3-dioxygenase 2 | Mus musculus (house mouse) | IC50 | 28.7000 | 1 | 1 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 | 0.5760 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Nuclear receptor ROR-alpha | Homo sapiens (human) | IC50 | 0.1995 | 1 | 1 |
| Nuclear receptor ROR-beta | Homo sapiens (human) | IC50 | 12.6224 | 2 | 2 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | IC50 | 0.1995 | 1 | 1 |
| Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | IC50 | 0.8200 | 1 | 1 |
| Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Ki | 0.8200 | 1 | 1 |
| Retinoic acid receptor alpha | Homo sapiens (human) | IC50 | 2.2542 | 4 | 4 |
| Retinoic acid receptor alpha | Mus musculus (house mouse) | IC50 | 0.0057 | 3 | 3 |
| Retinoic acid receptor alpha | Homo sapiens (human) | Ki | 0.0688 | 3 | 3 |
| Retinoic acid receptor beta | Homo sapiens (human) | IC50 | 0.7537 | 4 | 4 |
| Retinoic acid receptor beta | Mus musculus (house mouse) | IC50 | 0.0050 | 2 | 2 |
| Retinoic acid receptor beta | Homo sapiens (human) | Ki | 0.0095 | 3 | 3 |
| Retinoic acid receptor gamma | Mus musculus (house mouse) | IC50 | 0.0040 | 2 | 2 |
| Retinoic acid receptor gamma | Homo sapiens (human) | IC50 | 0.0064 | 3 | 3 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Ki | 0.0056 | 4 | 4 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Retinoic acid receptor RXR-alpha | Mus musculus (house mouse) | IC50 | 18.0000 | 3 | 3 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | Ki | 0.2268 | 3 | 3 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Retinoic acid receptor RXR-beta | Mus musculus (house mouse) | IC50 | 50.0000 | 1 | 1 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | Ki | 0.3118 | 3 | 3 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | IC50 | 0.3500 | 1 | 1 |
| Retinoic acid receptor RXR-gamma | Mus musculus (house mouse) | IC50 | 50.0000 | 1 | 1 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | Ki | 0.1365 | 3 | 3 |
| Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 | 91.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cellular retinoic acid-binding protein 1 | Mus musculus (house mouse) | Kd | 0.0004 | 2 | 2 |
| Cellular retinoic acid-binding protein 2 | Mus musculus (house mouse) | Kd | 0.0020 | 2 | 2 |
| Cytochrome P450 1A2 | Homo sapiens (human) | EC50 | 0.0005 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | EC50 | 0.0006 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | EC50 | 0.0012 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | EC50 | 0.0002 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | EC50 | 0.0015 | 1 | 1 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | EC50 | 18.0000 | 1 | 1 |
| Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Kd | 0.8000 | 1 | 1 |
| Retinoic acid receptor alpha | Homo sapiens (human) | EC50 | 0.2112 | 19 | 19 |
| Retinoic acid receptor alpha | Mus musculus (house mouse) | EC50 | 0.0082 | 3 | 3 |
| Retinoic acid receptor alpha | Homo sapiens (human) | Kd | 0.0102 | 10 | 12 |
| Retinoic acid receptor alpha | Mus musculus (house mouse) | Kd | 0.0150 | 1 | 1 |
| Retinoic acid receptor beta | Homo sapiens (human) | EC50 | 0.0827 | 20 | 20 |
| Retinoic acid receptor beta | Mus musculus (house mouse) | EC50 | 0.0012 | 3 | 3 |
| Retinoic acid receptor beta | Homo sapiens (human) | Kd | 0.0086 | 11 | 13 |
| Retinoic acid receptor beta | Mus musculus (house mouse) | Kd | 0.0130 | 1 | 1 |
| Retinoic acid receptor gamma | Mus musculus (house mouse) | EC50 | 0.0004 | 2 | 2 |
| Retinoic acid receptor gamma | Mus musculus (house mouse) | Kd | 0.0180 | 1 | 1 |
| Retinoic acid receptor gamma | Homo sapiens (human) | EC50 | 0.0697 | 17 | 17 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Kd | 0.0103 | 12 | 14 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | EC50 | 0.6570 | 8 | 9 |
| Retinoic acid receptor RXR-alpha | Mus musculus (house mouse) | EC50 | 2.0000 | 1 | 1 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | Kd | 0.0681 | 6 | 8 |
| Retinoic acid receptor RXR-alpha | Mus musculus (house mouse) | Kd | 1.0000 | 1 | 1 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | EC50 | 1.0496 | 4 | 4 |
| Retinoic acid receptor RXR-beta | Mus musculus (house mouse) | EC50 | 1.2110 | 1 | 1 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | Kd | 0.0000 | 1 | 1 |
| Retinoic acid receptor RXR-beta | Mus musculus (house mouse) | Kd | 0.6530 | 2 | 2 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | EC50 | 0.8568 | 4 | 4 |
| Retinoic acid receptor RXR-gamma | Mus musculus (house mouse) | EC50 | 0.4835 | 2 | 2 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | Kd | 0.1530 | 2 | 2 |
| Retinoic acid receptor RXR-gamma | Mus musculus (house mouse) | Kd | 0.3500 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cellular retinoic acid-binding protein 1 | Gallus gallus (chicken) | ID50 | 1.0000 | 1 | 1 |
| Ornithine decarboxylase | Mus musculus (house mouse) | ID50 | 0.0001 | 1 | 1 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | ID50 | 0.0000 | 1 | 1 |
| Retinoic acid receptor alpha | Homo sapiens (human) | EC30 | 0.0010 | 2 | 2 |
| Retinoic acid receptor alpha | Homo sapiens (human) | Relative EC30 | 0.0022 | 2 | 2 |
| Retinoic acid receptor alpha | Homo sapiens (human) | Relative IC50 | 0.0009 | 2 | 2 |
| Retinoic acid receptor beta | Homo sapiens (human) | EC30 | 0.0008 | 2 | 2 |
| Retinoic acid receptor beta | Homo sapiens (human) | Relative EC30 | 0.0016 | 2 | 2 |
| Retinoic acid receptor beta | Homo sapiens (human) | Relative IC50 | 0.0007 | 2 | 2 |
| Retinoic acid receptor gamma | Homo sapiens (human) | EC30 | 0.0002 | 2 | 2 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Relative EC30 | 0.0006 | 2 | 2 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Relative IC50 | 0.0007 | 2 | 2 |