Page last updated: 2024-08-05 14:36:22

EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor

An EC 1.8.1.* (oxidoreductase acting on sulfur group of donors, NAD+ or NADP+ as acceptor) inhibitor that interferes with the action of trypanothione-disulfide reductase (EC 1.8.1.12).

ChEBI ID: 77402

Members (5)

MemberDefinitionClass
clomipramineA dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.clomipramine
ebselenA benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.ebselen
quinacrineA member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.quinacrine
thioridazineA phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.thioridazine
trifluoperazineA member of the class of phenothiazines that is phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.trifluoperazine

Research

Studies (12,728)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19907,367 (57.88)18.7374
1990's2,404 (18.89)18.2507
2000's1,547 (12.15)29.6817
2010's1,104 (8.67)24.3611
2020's306 (2.40)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,027 (7.33%)5.53%
Reviews663 (4.73%)6.00%
Case Studies1,089 (7.77%)4.05%
Observational4 (0.03%)0.25%
Other11,233 (80.14%)84.16%

Protein Targets (371)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency0.564613
15-lipoxygenase, partialHomo sapiens (human)Potency6.804613
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency4.324913
67.9K proteinVaccinia virusPotency18.979224
acetylcholinesteraseHomo sapiens (human)Potency28.725822
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency8.146615
alpha-galactosidaseHomo sapiens (human)Potency32.464822
Alpha-synucleinHomo sapiens (human)Potency4.478013
Amyloid-beta precursor proteinHomo sapiens (human)Potency16.360111
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency11.220211
AR proteinHomo sapiens (human)Potency27.0655714
aryl hydrocarbon receptorHomo sapiens (human)Potency21.974422
arylsulfatase AHomo sapiens (human)Potency16.279113
ATAD5 protein, partialHomo sapiens (human)Potency12.278328
Ataxin-2Homo sapiens (human)Potency18.425925
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency11.776435
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency30.433222
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency3.796013
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency18.311614
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency1.412511
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491512
caspase-3Cricetulus griseus (Chinese hamster)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491512
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency25.535124
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency19.064025
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency2.655513
Chain A, Beta-lactamaseEscherichia coli K-12Potency57.122022
Chain A, CruzipainTrypanosoma cruziPotency28.183811
Chain A, Ferritin light chainEquus caballus (horse)Potency12.589311
Chain A, HADH2 proteinHomo sapiens (human)Potency1.827526
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency12.380712
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency9.649613
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency22.665535
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency3.637817
Chain B, HADH2 proteinHomo sapiens (human)Potency1.827526
chromobox protein homolog 1Homo sapiens (human)Potency64.967127
cytochrome P450 2C19 precursorHomo sapiens (human)Potency4.847715
cytochrome P450 2C9 precursorHomo sapiens (human)Potency0.539712
cytochrome P450 2D6Homo sapiens (human)Potency0.490212
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency3.076518
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency18.4944215
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency22.458612
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency31.670412
D(1A) dopamine receptorHomo sapiens (human)Potency6.420338
D(1A) dopamine receptorSus scrofa (pig)Potency20.405412
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency35.481311
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency22.387211
DNA polymerase betaHomo sapiens (human)Potency3.162311
DNA polymerase III, partialBacillus subtilisPotency4.744411
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency39.984713
DNA polymerase kappa isoform 1Homo sapiens (human)Potency35.564013
dopamine D1 receptorHomo sapiens (human)Potency16.360111
Endothelin receptor type BRattus norvegicus (Norway rat)Potency22.387211
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency22.387211
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.039069
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency20.881923
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.5968610
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.0361212
EWS/FLI fusion proteinHomo sapiens (human)Potency8.325248
farnesoid X nuclear receptorHomo sapiens (human)Potency33.488923
flap endonuclease 1Homo sapiens (human)Potency39.415825
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency22.387211
Fumarate hydrataseHomo sapiens (human)Potency35.019715
GABA theta subunitRattus norvegicus (Norway rat)Potency18.329118
GALC proteinHomo sapiens (human)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency18.329118
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency18.329118
gemininHomo sapiens (human)Potency21.5204414
GLI family zinc finger 3Homo sapiens (human)Potency9.166424
glp-1 receptor, partialHomo sapiens (human)Potency11.519012
GLS proteinHomo sapiens (human)Potency6.856924
glucocerebrosidaseHomo sapiens (human)Potency30.699514
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.832533
glucokinase regulatory proteinHomo sapiens (human)Potency14.125411
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Potency5.798811
Glycoprotein hormones alpha chainHomo sapiens (human)Potency14.125412
Guanine nucleotide-binding protein GHomo sapiens (human)Potency25.118911
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency12.589311
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency35.306012
heat shock protein beta-1Homo sapiens (human)Potency33.488911
hexokinase-4 isoform 1Homo sapiens (human)Potency14.125411
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency4.6568218
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency7.638516
Histone H2A.xCricetulus griseus (Chinese hamster)Potency59.103824
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency44.668411
huntingtin isoform 2Homo sapiens (human)Potency27.717012
hypothetical protein, conservedTrypanosoma bruceiPotency11.147145
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency17.559424
IDH1Homo sapiens (human)Potency23.527013
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency0.929612
Integrin alpha-IIbHomo sapiens (human)Potency19.952611
Integrin beta-3Homo sapiens (human)Potency19.952611
Interferon betaHomo sapiens (human)Potency16.199824
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency5.611112
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.366116
LuciferasePhotinus pyralis (common eastern firefly)Potency23.810737
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency18.078935
M-phase phosphoprotein 8Homo sapiens (human)Potency19.229815
Microtubule-associated protein tauHomo sapiens (human)Potency13.276929
mitogen-activated protein kinase 1Homo sapiens (human)Potency25.118912
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency5.378124
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.000011
NFKB1 protein, partialHomo sapiens (human)Potency11.904824
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency2.115412
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047913
Nrf2Homo sapiens (human)Potency29.295322
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency29.847011
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency25.373512
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency24.028527
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency31.857123
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency10.000011
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency125.892012
ParkinHomo sapiens (human)Potency23.109311
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency26.854511
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency27.905414
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency33.807811
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency7.612823
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency29.354523
phosphopantetheinyl transferaseBacillus subtilisPotency16.461316
plasminogen precursorMus musculus (house mouse)Potency12.589311
polyproteinZika virusPotency35.019715
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency2.837112
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency6.715316
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency16.443213
PPM1D proteinHomo sapiens (human)Potency11.708612
pregnane X nuclear receptorHomo sapiens (human)Potency5.955711
progesterone receptorHomo sapiens (human)Potency29.981323
pyruvate kinaseLeishmania mexicana mexicanaPotency15.551355
pyruvate kinase PKM isoform aHomo sapiens (human)Potency5.118944
pyruvate kinase PKM isoform bHomo sapiens (human)Potency10.000022
RAR-related orphan receptor gammaMus musculus (house mouse)Potency13.370223
ras-related protein Rab-9AHomo sapiens (human)Potency54.068313
regulator of G-protein signaling 4Homo sapiens (human)Potency13.999215
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency25.493836
retinoid X nuclear receptor alphaHomo sapiens (human)Potency15.089011
RGS12Homo sapiens (human)Potency12.589311
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency17.8382414
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency2.993511
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Potency5.798811
Smad3Homo sapiens (human)Potency27.662513
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency19.702012
survival motor neuron protein isoform dHomo sapiens (human)Potency31.622811
TAR DNA-binding protein 43Homo sapiens (human)Potency6.309611
TDP1 proteinHomo sapiens (human)Potency10.0305224
thioredoxin glutathione reductaseSchistosoma mansoniPotency44.668411
thioredoxin reductaseRattus norvegicus (Norway rat)Potency11.507025
ThrombopoietinHomo sapiens (human)Potency10.533526
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency14.350526
thyroid stimulating hormone receptorHomo sapiens (human)Potency20.483448
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency31.622811
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency50.118711
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency14.689211
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency12.589311
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency12.589311
USP1 protein, partialHomo sapiens (human)Potency51.752929
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency11.334024
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency26.832512
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency18.371615

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC502.255522
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.008011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.032522
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki2.517022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.032522
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki2.517022
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki5.000011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki5.000011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.911513
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.027733
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.216324
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.008311
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.184012
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.027733
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.117012
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.008311
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.039012
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.027733
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.020512
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.008311
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.039012
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.020512
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.158012
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC500.005011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.082534
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5019.300012
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.125522
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC500.005011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC5028.005022
AcetylcholinesteraseHomo sapiens (human)IC508.833522
Acidic phospholipase A2 2Naja naja (Indian cobra)IC502,155.000022
AlbuminHomo sapiens (human)IC503.500012
Aldehyde oxidaseHomo sapiens (human)IC503.300011
Aldehyde oxidase 1Oryctolagus cuniculus (rabbit)IC5010.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC501.506013
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.493313
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.120034
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.075011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.160023
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.075011
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.750313
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.160023
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.368613
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.075011
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.956824
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.478313
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.051012
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.576524
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.351013
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.051012
Alpha-2C adrenergic receptorHomo sapiens (human)IC501.360324
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.035511
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.263313
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.051012
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC503.907012
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.200912
Angiotensin-converting enzyme 2 Homo sapiens (human)IC500.670011
Arrestin, beta 1Homo sapiens (human)IC501.524011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent translocase ABCB1Homo sapiens (human)IC508.133333
ATP-dependent translocase ABCB1Homo sapiens (human)Ki6.500011
Beta-glucuronidaseRattus norvegicus (Norway rat)IC507.800011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC500.757544
Bile salt export pumpHomo sapiens (human)IC5057.603848
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC506.600011
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi0.500011
Calcium-dependent protein kinase 4Plasmodium falciparum 3D7Ki150.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Caspase-1Homo sapiens (human)IC504.040011
Cathepsin D Bos taurus (cattle)IC500.060011
CholinesteraseEquus caballus (horse)IC508.482733
Cyclic GMP-AMP synthaseHomo sapiens (human)IC507.000022
cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC5019.880011
Cytochrome P450 1A2Homo sapiens (human)IC509.332311
Cytochrome P450 2C19Homo sapiens (human)IC506.377811
Cytochrome P450 2D6Homo sapiens (human)IC502.859612
DRattus norvegicus (Norway rat)IC500.304645
D(1A) dopamine receptorHomo sapiens (human)IC500.653512
D(1A) dopamine receptorHomo sapiens (human)Ki0.327012
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.085012
D(2) dopamine receptorHomo sapiens (human)IC500.224012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.053648
D(2) dopamine receptorHomo sapiens (human)Ki0.046334
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.041522
D(3) dopamine receptorHomo sapiens (human)IC500.489013
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.085012
D(3) dopamine receptorHomo sapiens (human)Ki0.166113
D(4) dopamine receptorHomo sapiens (human)IC501.468011
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.085012
D(4) dopamine receptorHomo sapiens (human)Ki0.515011
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC50100.000011
DNA-directed RNA polymerase subunit alphaEscherichia coli K-12IC5020.000011
DNA-directed RNA polymerase subunit betaEscherichia coli K-12IC5020.000011
DNA-directed RNA polymerase subunit beta'Escherichia coli K-12IC5020.000011
DNA-directed RNA polymerase subunit omegaEscherichia coli K-12IC5020.000011
Emopamil-binding protein-likeHomo sapiens (human)Ki0.003911
Epidermal growth factor receptorHomo sapiens (human)IC502.947011
eukaryotic translation initiation factor 4 gamma 1 isoform 4Homo sapiens (human)IC501.150011
eukaryotic translation initiation factor 4E isoform 1Mus musculus (house mouse)IC501.150011
GABA theta subunitRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.000014
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.000011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.000011
Gamma-butyrobetaine dioxygenaseHomo sapiens (human)IC500.742055
Genome polyprotein IC500.700011
glucose-6-phosphate 1-dehydrogenase isoform bHomo sapiens (human)IC5013.200011
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonasePlasmodium bergheiIC5015.086733
Glutathione reductase, mitochondrialHomo sapiens (human)IC501,000.000011
hexokinaseTrypanosoma brucei brucei TREU927IC500.900911
Histamine H1 receptorHomo sapiens (human)IC500.078512
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.033123
Histamine H1 receptorHomo sapiens (human)Ki0.009112
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC500.720011
Histamine H2 receptorHomo sapiens (human)IC502.178013
Histamine H2 receptorHomo sapiens (human)Ki2.141713
Histidine-rich protein PFHRP-IIPlasmodium falciparum (malaria parasite P. falciparum)IC50292.000011
Histone deacetylase 5Homo sapiens (human)IC503.400011
Histone deacetylase 6Homo sapiens (human)IC506.533333
Histone deacetylase 9Homo sapiens (human)IC503.700011
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC500.730011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC500.400011
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)Ki0.094033
Insulin-degrading enzymeHomo sapiens (human)IC5033.352033
Kappa-type opioid receptorHomo sapiens (human)IC502.490011
Kappa-type opioid receptorHomo sapiens (human)Ki0.996011
large T antigenBetapolyomavirus macacaeIC5013.910011
Lysozyme C-1Rattus norvegicus (Norway rat)IC509.000011
Macrophage migration inhibitory factorHomo sapiens (human)IC502.400011
Macrophage migration inhibitory factorHomo sapiens (human)Ki0.570022
Major prion proteinMus musculus (house mouse)IC500.095111
Methionine aminopeptidase 2Homo sapiens (human)IC502.430011
MPI proteinHomo sapiens (human)IC500.290522
Mucosa-associated lymphoid tissue lymphoma translocation protein 1Homo sapiens (human)IC503.765022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.529013
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC502.303022
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.127613
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.437013
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC502.303022
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.155713
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.505013
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC502.303022
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.107013
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.718013
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC502.303022
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.100313
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC501.266113
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC502.303022
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.909513
NLeishmania infantumIC5013.530011
NADPH oxidase 1Homo sapiens (human)IC5017.000011
neutrophil cytosol factor 1Homo sapiens (human)IC500.390011
Neutrophil cytosol factor 1Homo sapiens (human)Ki125.000033
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC503.907012
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki3.200912
perilipin-1Homo sapiens (human)IC503.410011
perilipin-5Homo sapiens (human)IC501.101011
phosphoethanolamine/phosphocholine phosphatase isoform 1Homo sapiens (human)IC500.111011
Phospholipase A2, membrane associatedHomo sapiens (human)IC5076,000.000011
Phospholipase A2, membrane associatedRattus norvegicus (Norway rat)IC50320,000.000011
phosphomannomutase 2Homo sapiens (human)IC500.672011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC501.350012
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC500.70951113
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki2.423623
Procathepsin LHomo sapiens (human)IC500.670011
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC502.100011
Protein kinase C alpha typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C beta typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C delta typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C epsilon typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C eta typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C gamma typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C theta typeRattus norvegicus (Norway rat)IC50500.000011
Protein kinase C zeta typeRattus norvegicus (Norway rat)IC50500.000011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC500.670011
Replicase polyprotein 1abBetacoronavirus England 1IC505.335022
Replicase polyprotein 1abHuman coronavirus 229EIC500.670011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC504.23691416
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC500.620023
Riboflavin-binding proteinGallus gallus (chicken)Ki6.700011
RNA polymerase beta subunit (EC 2.7.7.6), partialEscherichia coliIC5011.687211
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1Oryctolagus cuniculus (rabbit)IC5045.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.862512
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.750011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.246723
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC501.830011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC500.035512
Sodium-dependent dopamine transporter Homo sapiens (human)IC502.633023
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.035012
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.145624
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.493313
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.273723
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.133123
Solute carrier family 22 member 1 Homo sapiens (human)IC5019.300011
Spike glycoproteinBetacoronavirus England 1IC500.670011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC500.670011
Structural capsid protein Human immunodeficiency virus 1IC500.046711
Sulfhydryl oxidase 1Homo sapiens (human)IC505.400011
Toxin BClostridioides difficileIC500.017211
TPA: protein transporter TIM10Saccharomyces cerevisiae S288CIC505.290022
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC500.880011
Transmembrane protease serine 2Homo sapiens (human)IC500.670011
Trypanothione reductaseTrypanosoma brucei bruceiIC503.400011
Trypanothione reductaseTrypanosoma cruziIC5058.125044
Trypanothione reductaseTrypanosoma cruziKi12.500077
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)IC500.060011
Tyrosine-protein kinase FynHomo sapiens (human)IC505.050011
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC508.000011
UDP-glucose 4-epimeraseHomo sapiens (human)IC500.014011
Urease subunit alphaHelicobacter pylori 26695IC5030.472544
Urease subunit alphaHelicobacter pylori 26695Ki0.226011
Urease subunit betaHelicobacter pylori 26695IC5030.472544
Urease subunit betaHelicobacter pylori 26695Ki0.226011
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC501.320013
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC502.410022
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC503.500011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC503.500011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC503.500011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC509.000011
WD repeat-containing protein 48Homo sapiens (human)IC508.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd0.001011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd0.001011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd0.001011
AlbuminRattus norvegicus (Norway rat)Kd10.345012
Angiotensin-converting enzyme 2 Homo sapiens (human)EC509.076713
ATP-dependent translocase ABCB1Homo sapiens (human)EC5014.400011
Calmodulin Bos taurus (cattle)Kd3.400011
Calmodulin-1Homo sapiens (human)Kd1.000011
D(2) dopamine receptorRattus norvegicus (Norway rat)Kd0.000511
Envelope glycoproteinEbola virus - Mayinga, Zaire, 1976Kd118.000011
Gamma-butyrobetaine dioxygenaseHomo sapiens (human)Kd4.100022
hexokinase HKDC1Homo sapiens (human)EC5038.800011
hexokinase-1 isoform HKIHomo sapiens (human)EC5041.900011
Major prion proteinHomo sapiens (human)EC500.300011
NPYLR7BAedes aegypti (yellow fever mosquito)EC503.150012
Procathepsin LHomo sapiens (human)EC509.076713
Proteasome subunit alpha type-6Homo sapiens (human)EC5012.200012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC509.076713
Replicase polyprotein 1abBetacoronavirus England 1EC509.076713
Replicase polyprotein 1abHuman coronavirus 229EEC509.076713
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC507.975024
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC507.975024
Riboflavin-binding proteinGallus gallus (chicken)Kd0.264011
Spike glycoproteinBetacoronavirus England 1EC509.076713
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC509.076713
streptokinase A precursorStreptococcus pyogenes M1 GASEC501.519011
Transmembrane protease serine 2Homo sapiens (human)EC509.076713

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aldehyde oxidaseHomo sapiens (human)Kii1.300011
Aldehyde oxidaseHomo sapiens (human)Kis1.300011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5013.000011
H3 histone acetyltransferaseCandida albicans SC5314AC501.550011
hypothetical protein CAALFM_CR05890CACandida albicans SC5314AC501.550011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH12.650012
Snq2pSaccharomyces cerevisiae EC1118INH13.150012