An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of IkappaB kinase (EC 2.7.11.10).
ChEBI ID: 77113
| Member | Definition | Class |
|---|---|---|
| bay 11-7082 | A nitrile that is acrylonitrile in which the hydrogen located beta,trans to the cyano group is replaced by a tosyl group. It is an inhibitor of cytokine-induced IkappaB-alpha phosphorylation in cells. | (E)-3-tosylacrylonitrile |
| bay 11-7085 | A sulfone that is benzene substituted by [(E)-2-cyanoethenyl]sulfonyl and tert-butyl groups at position 1 and 4, respectively. It is an irreversible inhibitor of IkappaB-alpha phosphorylation in cells (IC50 = 10 muM) and prevents the activation of NF-kappaB. | BAY11-7085 |
| berberine | berberine |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 219 (4.68) | 18.7374 |
| 1990's | 262 (5.60) | 18.2507 |
| 2000's | 825 (17.63) | 29.6817 |
| 2010's | 2,265 (48.41) | 24.3611 |
| 2020's | 1,108 (23.68) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 103 (2.15%) | 5.53% |
| Reviews | 307 (6.39%) | 6.00% |
| Case Studies | 8 (0.17%) | 4.05% |
| Observational | 1 (0.02%) | 0.25% |
| Other | 4,382 (91.27%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 11.2250 | 2 | 4 |
| Alpha-synuclein | Homo sapiens (human) | Potency | 7.6701 | 1 | 3 |
| Amyloid-beta precursor protein | Homo sapiens (human) | Potency | 1.7346 | 1 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 7.5686 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 26.9577 | 2 | 4 |
| Ataxin-2 | Homo sapiens (human) | Potency | 22.7406 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 20.4730 | 1 | 2 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 11.9955 | 1 | 1 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 8.3152 | 1 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0056 | 2 | 2 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 9.6475 | 1 | 3 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 17.3931 | 1 | 4 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 42.2395 | 1 | 2 |
| 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 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 8.7790 | 2 | 3 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 17.8739 | 4 | 7 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 1.1939 | 1 | 4 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 8.3572 | 4 | 4 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 34.7120 | 1 | 3 |
| 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 |
| geminin | Homo sapiens (human) | Potency | 1.1220 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 9.8344 | 1 | 2 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 2.9309 | 2 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 21.4796 | 1 | 4 |
| hypothetical protein, conserved | Trypanosoma brucei | Potency | 12.7181 | 1 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 2.5119 | 2 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 10.4304 | 2 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 10.4353 | 1 | 3 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 7.1912 | 2 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 7.7390 | 1 | 3 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 3.5481 | 1 | 1 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 94.4495 | 1 | 2 |
| Nrf2 | Homo sapiens (human) | Potency | 11.5821 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.8422 | 2 | 2 |
| Parkin | Homo sapiens (human) | Potency | 29.0929 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 6.2426 | 2 | 2 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 8.4921 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 2.5286 | 1 | 2 |
| polyprotein | Zika virus | Potency | 34.7120 | 1 | 3 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 10.4353 | 1 | 2 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 58.0479 | 1 | 3 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 2.7001 | 1 | 3 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 0.5212 | 1 | 1 |
| Smad3 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 21.2804 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.8268 | 2 | 4 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.9684 | 3 | 6 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 6.5789 | 1 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Acetylcholinesterase | Electrophorus electricus (electric eel) | IC50 | 0.7827 | 3 | 3 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 0.4000 | 2 | 2 |
| 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 |
| C-C chemokine receptor type 2 | Homo sapiens (human) | IC50 | 4.1770 | 1 | 1 |
| C-C chemokine receptor type 2 | Homo sapiens (human) | Ki | 1.6140 | 1 | 1 |
| Cholinesterase | Equus caballus (horse) | IC50 | 15.2667 | 3 | 3 |
| Cholinesterase | Homo sapiens (human) | IC50 | 15.8950 | 2 | 2 |
| Class A sortase SrtA | Staphylococcus aureus | IC50 | 129.0000 | 1 | 1 |
| Cytochrome P450 1B1 | Homo sapiens (human) | IC50 | 0.9747 | 3 | 3 |
| Cytochrome P450 1B1 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 4.4120 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 2.2060 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 3.4600 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 1.1750 | 1 | 1 |
| Lysine-specific histone demethylase 1A | Homo sapiens (human) | IC50 | 6.9700 | 1 | 1 |
| NACHT, LRR and PYD domains-containing protein 3 | Mus musculus (house mouse) | IC50 | 12.0000 | 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 |
| Nuclear factor NF-kappa-B p100 subunit | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Nuclear factor NF-kappa-B p105 subunit | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 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 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | IC50 | 10.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 0.8300 | 1 | 2 |
| Telomerase reverse transcriptase | Homo sapiens (human) | IC50 | 37.0000 | 1 | 1 |
| Transcription factor p65 | Homo sapiens (human) | IC50 | 2.5000 | 2 | 2 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 67.0000 | 1 | 1 |