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NF-kappaB inhibitor

An inhibitor of NF-kappaB (nuclear factor kappa-light-chain-enhancer of activated B cells), a protein complex involved in the transcription of DNA.

ChEBI ID: 73240

Members (17)

MemberDefinitionClass
1'-acetoxychavicol acetateAn acetate ester that is chavicol acetate substituted by an acetoxy group at position 1'.1'-acetoxychavicol acetate
bay 11-7085A 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
brazilinA organic heterotetracyclic compound that is a red pigment obtained from the wood of Caesalpinia echinata (Brazil-wood) or Caesalpinia sappan (sappan-wood).brazilin
cblc137A member of the class of carbazoles that is 9H-carbazole which is substituted by acetyl groups at positions 3 and 6, and by a 2-isopropylethyl group on the nitrogen atom (position 9). It is a modulator of histone chaperone FACT (FAcilitates Chromatin Transcription) - interaction of CBL0137 with the FACT complex results in simultaneous NF-kappa beta suppression, Heat Shock Transcription Factor 1 (HSF1) suppression and p53 activation - and shows antitumour effects in animal models of various cancers.CBL0137
disulfiramAn organic disulfide that results from the formal oxidative dimerisation of N,N-diethyldithiocarbamic acid. A multi-enzyme inhibitor that is used in alcohol aversion therapy and also exhibits anticancer properties.disulfiram
ergolideA sesquiterpene lactone that is decahydroazuleno[6,5-b]furan-2,5-dione substituted by methyl groups at positions 4a and 8, a methylidene group at position 3 and an acetyloxy group at position 4. It has been isolated from the aerial parts of Inula hupehensis.ergolide
eupomatenoid 6A member of the class of benzofurans that is 1-benzofuran substituted by a 4-hydroxyphenyl group at position 2, a methyl group at position 3 and a prop-1-en-1-yl group at position 5. It is a lignan derivative isolated from the roots of Krameria lappacea.rataniaphenol II
fr 148083A macrolide that is the 7-oxo derivative of zeaenol (the 5Z stereoisomer). Isolated from Fungi, it exhibits cytotoxic, antibacterial and inhibitory activity against NF-kappaB.5Z-7-oxozeaenol
glaucineAn aporphine alkaloid that is (S)-1,2,9,10-tetrahydroxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline in which the four phenolic hydrogens have been replaced by methyl groups.(S)-glaucine
jsh 23A diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1.JSH-23
kojic acidA pyranone that is 4H-pyran substituted by a hydroxy group at position 5, a hydroxymethyl group at position 2 and an oxo group at position 4. It has been isolated from the fungus Aspergillus oryzae.kojic acid
oleuropeinA secoiridoid glycoside that is the methyl ester of 3,4-dihydro-2H-pyran-5-carboxylic acid which is substituted at positions 2, 3, and 4 by hydroxy, ethylidene, and carboxymethyl groups, respectively and in which the anomeric hydroxy group at position 2 has been converted into its beta-D-glucoside and the carboxylic acid moiety of the carboxymethyl substituent has been converted to the corresponding 3,4-dihydroxyphenethyl ester (the 2S,3E,4S stereoisomer). The most important phenolic compound present in olive cultivars.oleuropein
piperineA N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum.piperine
pyrrolidine dithiocarbamateA member of the class of dithiocarbamic acids that is the N-dithiocarboxy derivative of pyrrolidine.pyrrolidine dithiocarbamate
rubimaillinA benzochromene that is 2H-benzo[h]chromene which is substituted by two methyl groups at position 2, a methoxycarbonyl group at position 5, and a hydroxy group at position 6. Found in the Chinese medical plant Rubia cordifola, It has an anti-cancer effect by inhibition of TNF-alpha-induced NF-kappaB activation. It is also a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1 and ACAT2), but is more selective for the ACAT2 isozyme.rubimaillin
tocotrienol, deltaA tocotrienol that is chroman-6-ol substituted by methyl groups at positions 2 and 8 and a farnesyl chain at position 2.delta-tocotrienol
tubocapsanolide aA withanolide that is 5beta,6beta:16alpha,17alpha-diepoxywitha-2,24-dienolide substituted by a hydroxy group at position 4 and an oxo group at position 1. Isolated from Tubocapsicum anomalum, it exhibits cytotoxic activity.tubocapsanolide A

Research

Studies (7,182)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,102 (29.27)18.7374
1990's770 (10.72)18.2507
2000's1,283 (17.86)29.6817
2010's2,139 (29.78)24.3611
2020's888 (12.36)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials259 (3.38%)5.53%
Reviews455 (5.94%)6.00%
Case Studies341 (4.46%)4.05%
Observational5 (0.07%)0.25%
Other6,594 (86.15%)84.16%

Protein Targets (280)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency9.138518
15-lipoxygenase, partialHomo sapiens (human)Potency0.320813
acetylcholinesteraseHomo sapiens (human)Potency61.453446
acid sphingomyelinaseHomo sapiens (human)Potency31.622811
activating transcription factor 6Homo sapiens (human)Potency0.627013
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency9.531618
Alpha-synucleinHomo sapiens (human)Potency5.533913
Amyloid-beta precursor proteinHomo sapiens (human)Potency3.165812
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency14.125411
AR proteinHomo sapiens (human)Potency5.96761034
aryl hydrocarbon receptorHomo sapiens (human)Potency21.744338
arylsulfatase AHomo sapiens (human)Potency7.568611
ATAD5 protein, partialHomo sapiens (human)Potency18.737247
Ataxin-2Homo sapiens (human)Potency26.034327
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency20.847223
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency26.165129
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency7.194412
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency6.287012
beta-2 adrenergic receptorHomo sapiens (human)Potency0.651311
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.005622
BRCA1Homo sapiens (human)Potency8.912511
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency11.426413
caspase-3Cricetulus griseus (Chinese hamster)Potency10.559012
caspase-3Homo sapiens (human)Potency11.426413
Caspase-7Cricetulus griseus (Chinese hamster)Potency10.559012
Cellular tumor antigen p53Homo sapiens (human)Potency28.850225
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency22.535822
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.308513
Chain A, Beta-lactamaseEscherichia coli K-12Potency58.763723
Chain A, CruzipainTrypanosoma cruziPotency11.669827
Chain A, Ferritin light chainEquus caballus (horse)Potency30.300122
Chain A, HADH2 proteinHomo sapiens (human)Potency19.373925
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.794311
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency18.823112
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency12.589312
Chain B, HADH2 proteinHomo sapiens (human)Potency19.373925
chromobox protein homolog 1Homo sapiens (human)Potency30.211723
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency0.538022
cytochrome P450 2C19 precursorHomo sapiens (human)Potency2.903112
cytochrome P450 2C9 precursorHomo sapiens (human)Potency1.455012
cytochrome P450 2C9, partialHomo sapiens (human)Potency7.864713
cytochrome P450 2D6Homo sapiens (human)Potency27.094212
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.248829
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency18.138013
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.595215
D(1A) dopamine receptorHomo sapiens (human)Potency5.670623
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.125112
estrogen nuclear receptor alphaHomo sapiens (human)Potency9.8894935
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency10.367826
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency6.50441040
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.517316
EWS/FLI fusion proteinHomo sapiens (human)Potency0.038944
farnesoid X nuclear receptorHomo sapiens (human)Potency14.311137
flap endonuclease 1Homo sapiens (human)Potency89.125113
Fumarate hydrataseHomo sapiens (human)Potency22.686015
GVesicular stomatitis virusPotency7.864713
GABA theta subunitRattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.382815
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.382815
gemininHomo sapiens (human)Potency10.917249
GLI family zinc finger 3Homo sapiens (human)Potency1.1666312
GLS proteinHomo sapiens (human)Potency18.294425
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency35.792133
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.674415
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency2.930922
heat shock protein beta-1Homo sapiens (human)Potency0.181426
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency5.7014214
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.386013
histone deacetylase 9 isoform 3Homo sapiens (human)Potency9.733225
Histone H2A.xCricetulus griseus (Chinese hamster)Potency26.214628
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency39.810711
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency7.864713
huntingtin isoform 2Homo sapiens (human)Potency0.794311
hypothetical protein, conservedTrypanosoma bruceiPotency9.652725
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency0.406224
IDH1Homo sapiens (human)Potency0.013011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency7.864716
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency15.848911
Integrin alpha-IIbHomo sapiens (human)Potency25.118911
Integrin beta-3Homo sapiens (human)Potency25.118911
Interferon betaHomo sapiens (human)Potency8.026329
lamin isoform A-delta10Homo sapiens (human)Potency2.941326
lethal factor (plasmid)Bacillus anthracis str. A2012Potency3.981111
LuciferasePhotinus pyralis (common eastern firefly)Potency8.983439
M-phase phosphoprotein 8Homo sapiens (human)Potency14.976312
Microtubule-associated protein tauHomo sapiens (human)Potency10.0495211
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.810722
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency12.589311
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency39.810711
neuropeptide S receptor isoform AHomo sapiens (human)Potency19.839613
NFKB1 protein, partialHomo sapiens (human)Potency7.079522
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency3.390513
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency37.795012
Nrf2Homo sapiens (human)Potency11.582111
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency17.6978310
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency20.596211
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency0.472913
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency2.6451213
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency2.8554315
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency25.118911
ParkinHomo sapiens (human)Potency29.092911
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.261523
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency10.243812
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.2818511
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency1.417026
phosphopantetheinyl transferaseBacillus subtilisPotency3.130514
plasminogen precursorMus musculus (house mouse)Potency11.294712
polyproteinZika virusPotency22.686015
polypyrimidine tract-binding protein 1 isoform aHomo sapiens (human)Potency14.550022
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency2.901913
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency8.886114
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency19.149812
PPM1D proteinHomo sapiens (human)Potency8.107114
pregnane X nuclear receptorHomo sapiens (human)Potency22.106327
pregnane X receptorRattus norvegicus (Norway rat)Potency7.079511
progesterone receptorHomo sapiens (human)Potency20.425526
pyruvate kinaseLeishmania mexicana mexicanaPotency15.848922
pyruvate kinase PKM isoform bHomo sapiens (human)Potency25.118922
RAR-related orphan receptor gammaMus musculus (house mouse)Potency2.1064212
ras-related protein Rab-9AHomo sapiens (human)Potency39.535913
regulator of G-protein signaling 4Homo sapiens (human)Potency1.590712
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency1.3921315
retinoid X nuclear receptor alphaHomo sapiens (human)Potency23.1885411
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency0.538022
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency0.736033
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency0.843711
SMAD family member 2Homo sapiens (human)Potency0.199511
SMAD family member 3Homo sapiens (human)Potency0.199511
Smad3Homo sapiens (human)Potency7.974412
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.794311
survival motor neuron protein isoform dHomo sapiens (human)Potency28.362713
TAR DNA-binding protein 43Homo sapiens (human)Potency3.981111
TDP1 proteinHomo sapiens (human)Potency4.3046214
thioredoxin glutathione reductaseSchistosoma mansoniPotency39.810711
thioredoxin reductaseRattus norvegicus (Norway rat)Potency10.142926
ThrombopoietinHomo sapiens (human)Potency0.398122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.3015311
thyroid stimulating hormone receptorHomo sapiens (human)Potency45.3385410
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency23.526723
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency11.220211
tyrosine-protein kinase YesHomo sapiens (human)Potency2.442411
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.294712
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.294712
USP1 protein, partialHomo sapiens (human)Potency29.349212
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency2.206526
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency18.6434510
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency5.392615
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency0.674415
VprHuman immunodeficiency virus 1Potency12.589311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC504.290522
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.171011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.966022
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC5034.547011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki11.051522
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.328011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC5016.001011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki7.429011
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.043011
Adenosine receptor A3Homo sapiens (human)IC500.356011
Adenosine receptor A3Homo sapiens (human)Ki0.201011
Aldehyde dehydrogenase, mitochondrialHomo sapiens (human)IC503.400011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC5070.370011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki69.812011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC501.178022
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
Alpha-1B adrenergic receptorHomo sapiens (human)IC508.330011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC501.178022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC502.000011
Alpha-2A adrenergic receptorHomo sapiens (human)IC504.904011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki1.839011
Alpha-2B adrenergic receptorHomo sapiens (human)IC503.218011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.469011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5036.357022
Amine oxidase [flavin-containing] AMus musculus (house mouse)Ki19.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)IC500.766522
Amine oxidase [flavin-containing] BMus musculus (house mouse)Ki3.190011
Angiotensin-converting enzyme 2 Homo sapiens (human)IC509.350011
apelin receptorHomo sapiens (human)IC502.630011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent translocase ABCB1Homo sapiens (human)IC5044.800022
bifunctional UDP-N-acetylglucosamine pyrophosphorylase/glucosamine-1-phosphate N-acetyltransferaseMycobacterium tuberculosis H37RvIC5085.030011
Bile salt export pumpHomo sapiens (human)IC5071.500022
C-C chemokine receptor type 2Homo sapiens (human)IC503.322512
C-C chemokine receptor type 2Homo sapiens (human)Ki1.284012
C-C chemokine receptor type 4Homo sapiens (human)IC508.395011
C-C chemokine receptor type 4Homo sapiens (human)Ki4.397011
C-C chemokine receptor type 5Homo sapiens (human)IC5023.661011
C-C chemokine receptor type 5Homo sapiens (human)Ki18.284011
C-X-C chemokine receptor type 2Homo sapiens (human)IC506.013011
C-X-C chemokine receptor type 2Homo sapiens (human)Ki4.209011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Carbamate kinaseGiardia intestinalisIC500.600011
Carbonic anhydrase 1Homo sapiens (human)IC5031,000.000012
Carbonic anhydrase 2Homo sapiens (human)IC5031,000.000012
Caspase-1Homo sapiens (human)IC501.800011
Cytochrome P450 1A2Homo sapiens (human)IC504.000011
Cytochrome P450 2C19Homo sapiens (human)IC5012.444612
DRattus norvegicus (Norway rat)Ki2.900011
D-amino-acid oxidaseHomo sapiens (human)IC502.000011
D-amino-acid oxidaseSus scrofa (pig)IC502.000011
D(1A) dopamine receptorHomo sapiens (human)IC503.285012
D(1A) dopamine receptorHomo sapiens (human)Ki1.642512
D(2) dopamine receptorHomo sapiens (human)IC5023.018011
D(2) dopamine receptorHomo sapiens (human)Ki7.673011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki2.800011
D(3) dopamine receptorHomo sapiens (human)IC502.272012
D(3) dopamine receptorHomo sapiens (human)Ki0.771512
D(4) dopamine receptorHomo sapiens (human)IC503.150011
D(4) dopamine receptorHomo sapiens (human)Ki1.105011
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC500.880011
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)Ki0.710011
DNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)IC507.000022
Dual specificity mitogen-activated protein kinase kinase 1Homo sapiens (human)IC500.029633
Dual specificity mitogen-activated protein kinase kinase 4Homo sapiens (human)IC503.000011
Dual specificity mitogen-activated protein kinase kinase 7Homo sapiens (human)IC500.800022
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50363.078011
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC50101.23801010
Gasdermin-DHomo sapiens (human)IC500.400011
Gasdermin-DMus musculus (house mouse)IC500.400011
glucose-6-phosphate 1-dehydrogenase isoform bHomo sapiens (human)IC5080.000011
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonasePlasmodium bergheiIC5056.700033
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC501.600011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC500.600011
Kappa-type opioid receptorHomo sapiens (human)IC506.103011
Kappa-type opioid receptorHomo sapiens (human)Ki2.441011
large T antigenBetapolyomavirus macacaeIC5010.730011
Lysine-specific demethylase 5AHomo sapiens (human)IC5010.000011
Lysyl oxidase homolog 2Homo sapiens (human)IC500.150011
Lysyl oxidase homolog 3Homo sapiens (human)IC500.093011
Lysyl oxidase homolog 4Homo sapiens (human)IC500.059011
Mitogen-activated protein kinase 1Homo sapiens (human)IC502.539333
Mitogen-activated protein kinase 3 Homo sapiens (human)IC501.510011
Mitogen-activated protein kinase kinase kinase 7Homo sapiens (human)IC500.017088
Monoglyceride lipaseHomo sapiens (human)IC500.809522
Mu-type opioid receptorHomo sapiens (human)IC503.511011
Mu-type opioid receptorHomo sapiens (human)Ki1.425011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC503.000011
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC5035.850022
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC5035.850022
Nuclear receptor subfamily 2 group C member 2Homo sapiens (human)IC500.009011
perilipin-1Homo sapiens (human)IC506.959011
perilipin-5Homo sapiens (human)IC501.622011
Phospholipase A-2-activating proteinHomo sapiens (human)IC500.011011
Polymerase acidic proteinInfluenza A virus (A/Puerto Rico/8/1934(H1N1))IC5012.444612
Polyphenol oxidase 1Agaricus bisporusIC5020.135022
Polyphenol oxidase 1Agaricus bisporusKi12.200011
Polyphenol oxidase 2Agaricus bisporusIC5063.2557107108
Polyphenol oxidase 2Agaricus bisporusKi82.327899
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC5052.000022
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC5016.066011
Procathepsin LHomo sapiens (human)IC509.350011
Prostaglandin E synthaseHomo sapiens (human)IC5011.000011
Prostaglandin G/H synthase 2Ovis aries (sheep)IC501.700011
Protein-lysine 6-oxidaseHomo sapiens (human)IC500.320011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC509.350011
Replicase polyprotein 1abBetacoronavirus England 1IC5015.383323
Replicase polyprotein 1abHuman coronavirus 229EIC509.350011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.3094910
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC509.350022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki3.710011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi3.710011
Retinal dehydrogenase 1Homo sapiens (human)IC500.130011
Sodium-dependent dopamine transporter Homo sapiens (human)IC504.637011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki3.684011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC5070.370011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki69.812011
Spike glycoproteinBetacoronavirus England 1IC509.350011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC509.350011
TGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)IC500.008733
Transcription factor p65Homo sapiens (human)IC5023.983333
Transmembrane protease serine 2Homo sapiens (human)IC509.350011
type-1 angiotensin II receptorHomo sapiens (human)IC506.637011
TyrosinaseHomo sapiens (human)IC501,014.74151920
TyrosinaseMus musculus (house mouse)IC50716.900033
TyrosinasePriestia megateriumIC5052.000011
TyrosinaseHomo sapiens (human)Ki350.000011
TyrosinaseMus musculus (house mouse)Ki5,500.000011
Tyrosinase Danio rerio (zebrafish)IC5012,550.000022
Uncharacterized protein YOR062CSaccharomyces cerevisiae S288CIC5019.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
BMP-2-inducible protein kinaseHomo sapiens (human)Kd0.003811
DNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)Kd1.300066
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC5029.100022
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC5029.100022
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC5029.100022
LacZ protein (plasmid)Escherichia coliEC5040.000011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC503.000011
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)EC503.162311
TyrosinasePriestia megateriumKd377.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
H3 histone acetyltransferaseCandida albicans SC5314AC503.260011
heat shock protein 90, putativePlasmodium falciparum 3D7AC504.554011
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC505.178011
hypothetical protein CAALFM_CR05890CACandida albicans SC5314AC503.260011
NAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)EC1.5227.500011
Nuclear receptor subfamily 2 group C member 2Homo sapiens (human)INH0.006011
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Activity10.000011
TyrosinaseHomo sapiens (human)Km79.000044