Page last updated: 2024-08-05 15:10:42

EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor

A topoisomerase inhibitor that inhibits DNA topoisomerase (ATP-hydrolysing), EC 5.99.1.3 (also known as topoisomerase II and as DNA gyrase), which catalyses ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands.

ChEBI ID: 50750

Members (23)

MemberDefinitionClass
aclarubicinAn anthracycline antibiotic that is produced by Streptomyces galilaeus and also has potent antineoplastic activity.aclacinomycin A zwitterion; aclacinomycin A
aclarubicinA zwitterion obtained by transfer of a proton from the 5-hydroxy to the tertiary amino group of aclacinomycin A. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).aclacinomycin A zwitterion; aclacinomycin A
amsacrineA sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.amsacrine
betulinic acidA pentacyclic triterpenoid that is lupane having a double bond at position 20(29) as well as 3beta-hydroxy and 28-carboxy substituents. It is found in the bark and other plant parts of several species of plants including Syzygium claviflorum. It exhibits anti-HIV, antimalarial, antineoplastic and anti-inflammatory properties.betulinic acid
celastrolA pentacyclic triterpenoid that is 24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid bearing an oxo substituent at position 2, a hydroxy substituent at position 3 and two methyl groups at positions 9 and 13. An antioxidant and anti-inflammatory agent. Potently inhibits lipid peroxidation in mitochondria and inhibits TNF-alpha-induced NFkappaB activation. Also shown to inhibit topoisomerase II activity in vitro (IC50 = 7.41 muM).celastrol
ciprofloxacinA quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.ciprofloxacin zwitterion; ciprofloxacin
ciprofloxacin hydrochloride anhydrousThe anhydrous form of the monohydrochloride salt of ciprofloxacin.ciprofloxacin hydrochloride (anhydrous)
dihydrobetulinic acidA pentacyclic triterpenoid that is lupane having a 3beta-hydroxy and 28-carboxy substituents. Isolated from the leaves of Syzygium claviflorum, it exhibits anti-HIV and antileishmanial activity.dihydrobetulinic acid
ellagic acidAn organic heterotetracyclic compound resulting from the formal dimerisation of gallic acid by oxidative aromatic coupling with intramolecular lactonisation of both carboxylic acid groups of the resulting biaryl. It is found in many fruits and vegetables, including raspberries, strawberries, cranberries, and pomegranates.ellagic acid
epirubicinAn anthracycline that is the 4'-epi-isomer of doxorubicin.4'-epidoxorubicin
fisetinA 7-hydroxyflavonol with additional hydroxy groups at positions 3, 3' and 4'.fisetin
fleroxacinA fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.fleroxacin
gatifloxacinA monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.gatifloxacin
genisteinA 7-hydroxyisoflavone with additional hydroxy groups at positions 5 and 4'. It is a phytoestrogenic isoflavone with antioxidant properties.genistein
levofloxacinAn optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.levofloxacin
lucanthoneA thioxanthen-9-one compound having a methyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. Formerly used for the treatment of schistosomiasis. It is a prodrug, being metabolised to hycanthone.lucanthone
maleimideA cyclic dicarboximide in which the two carboacyl groups on nitrogen together with the nitogen itself form a 1H-pyrrole-2,5-dione structure.maleimide
manoalideA sesterterpenoid isolated from the marine sponge Luffariella variabilis and which has been shown to exhibit inhibitory activity towards phospholipase A2.manoalide
methyl brevifolincarboxylateAn organic heterotricyclic compound that is 1,2,3,5-tetrahydrocyclopenta[c]isochromene substituted by hydroxy groups at positions 7, 8 and 9, oxo groups at positions 3 and 5 and a methoxycarbonyl group at position 1. Isolated from Phyllanthus urinaria and Phyllanthus niruri, it exhibits vasorelaxant activity.methyl brevifolincarboxylate
novobiocinA coumarin-derived antibiotic obtained from Streptomyces niveus.novobiocin
teniposideA furonaphthodioxole that is a synthetic derivative of podophyllotoxin with anti-tumour activity; causes single- and double-stranded breaks in DNA and DNA-protein cross-links and prevents repair by topoisomerase II binding.teniposide
top 53A furonaphthodioxole that is 4'-demethyldeoxypodophyllotoxin which is substituted at position 4 of the C-ring by a 2-{[2-(dimethylamino)ethyl](methyl)amino}ethyl group. While structurally related to etoposide, TOP-53 is significantly more toxic to non-small cell lung cancer cells, more active at generating chromosomal breaks, and displays improved cellular uptake and pharmacokinetics in animal lung tissues.TOP-53
wedelolactoneA member of the class of coumestans that is coumestan with hydroxy substituents as positions 1, 8 and 9 and a methoxy substituent at position 3.wedelolactone

Research

Studies (40,681)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19904,239 (10.42)18.7374
1990's7,794 (19.16)18.2507
2000's11,340 (27.88)29.6817
2010's12,898 (31.71)24.3611
2020's4,410 (10.84)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,433 (9.91%)5.53%
Reviews2,122 (4.74%)6.00%
Case Studies3,410 (7.62%)4.05%
Observational127 (0.28%)0.25%
Other34,642 (77.44%)84.16%

Protein Targets (546)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency16.7340112
15-lipoxygenase, partialHomo sapiens (human)Potency13.924516
67.9K proteinVaccinia virusPotency17.947824
acetylcholinesteraseHomo sapiens (human)Potency73.378622
acid sphingomyelinaseHomo sapiens (human)Potency562.341011
activating transcription factor 6Homo sapiens (human)Potency35.648123
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.213015
alpha-galactosidaseHomo sapiens (human)Potency44.668412
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency0.794311
AR proteinHomo sapiens (human)Potency18.80861234
aryl hydrocarbon receptorHomo sapiens (human)Potency10.644636
ATAD5 protein, partialHomo sapiens (human)Potency15.009346
Ataxin-2Homo sapiens (human)Potency19.282426
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency16.944111
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency25.872428
Bloom syndrome protein isoform 1Homo sapiens (human)Potency7.048427
BRCA1Homo sapiens (human)Potency10.000011
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.794311
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency70.407211
caspase-1 isoform alpha precursorHomo sapiens (human)Potency18.938913
caspase-3Homo sapiens (human)Potency70.407211
Caspase-7Homo sapiens (human)Potency17.216813
Cellular tumor antigen p53Homo sapiens (human)Potency36.422428
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.2999210
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency12.387119
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency3.9411310
Chain A, Beta-lactamaseEscherichia coli K-12Potency30.928812
Chain A, CruzipainTrypanosoma cruziPotency25.118912
Chain A, Ferritin light chainEquus caballus (horse)Potency34.172923
Chain A, HADH2 proteinHomo sapiens (human)Potency19.3005213
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency44.916512
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency9.8898312
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency14.159626
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency15.447729
Chain B, HADH2 proteinHomo sapiens (human)Potency19.3005213
chromobox protein homolog 1Homo sapiens (human)Potency31.519423
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency14.197435
CREB-binding proteinHomo sapiens (human)Potency17.045324
cytochrome P450 2C19 precursorHomo sapiens (human)Potency20.525113
cytochrome P450 2C9 precursorHomo sapiens (human)Potency18.510116
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.212112
cytochrome P450 2D6Homo sapiens (human)Potency21.707812
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency21.0830210
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.729124
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.299614
D(1A) dopamine receptorHomo sapiens (human)Potency0.642822
D(1A) dopamine receptorSus scrofa (pig)Potency3.689811
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency6.309611
DNA polymerase betaHomo sapiens (human)Potency37.170014
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.794311
DNA polymerase III, partialBacillus subtilisPotency29.934911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency0.611012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency0.652417
endonuclease IVEscherichia coliPotency12.988414
estrogen nuclear receptor alphaHomo sapiens (human)Potency22.70971246
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency13.371139
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency13.96541029
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.913115
EWS/FLI fusion proteinHomo sapiens (human)Potency8.5180419
farnesoid X nuclear receptorHomo sapiens (human)Potency34.712737
flap endonuclease 1Homo sapiens (human)Potency24.697315
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency63.095711
Fumarate hydrataseHomo sapiens (human)Potency2.573013
GVesicular stomatitis virusPotency6.212112
GABA theta subunitRattus norvegicus (Norway rat)Potency21.083015
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency21.083015
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency21.083015
gemininHomo sapiens (human)Potency11.896926
GLI family zinc finger 3Homo sapiens (human)Potency10.0660210
glp-1 receptor, partialHomo sapiens (human)Potency13.351922
GLS proteinHomo sapiens (human)Potency5.469223
glucocerebrosidaseHomo sapiens (human)Potency17.655814
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency24.433627
glucokinase regulatory proteinHomo sapiens (human)Potency22.387211
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency1.790713
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency9.946327
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency1.790713
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency1.790713
glyceraldehyde-3-phosphate dehydrogenase isoform 1Homo sapiens (human)Potency79.432811
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency23.711726
heat shock protein beta-1Homo sapiens (human)Potency29.989322
hemoglobin subunit betaHomo sapiens (human)Potency20.811412
hexokinase-4 isoform 1Homo sapiens (human)Potency22.387211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.8340224
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency23.695213
histone deacetylase 9 isoform 3Homo sapiens (human)Potency8.984026
Histone H2A.xCricetulus griseus (Chinese hamster)Potency66.891429
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency11.220211
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.212112
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency19.415122
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency5.011924
IDH1Homo sapiens (human)Potency11.619612
importin subunit beta-1 isoform 1Homo sapiens (human)Potency70.870412
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.212114
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency13.534622
Integrin alpha-IIbHomo sapiens (human)Potency10.580115
Integrin beta-3Homo sapiens (human)Potency10.580115
Interferon betaHomo sapiens (human)Potency12.1160318
lamin isoform A-delta10Homo sapiens (human)Potency12.485026
lethal factor (plasmid)Bacillus anthracis str. A2012Potency14.450414
LuciferasePhotinus pyralis (common eastern firefly)Potency18.596039
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency4.466811
M-phase phosphoprotein 8Homo sapiens (human)Potency56.234111
Microtubule-associated protein tauHomo sapiens (human)Potency18.0599213
mitogen-activated protein kinase 1Homo sapiens (human)Potency9.128625
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency8.154822
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency79.432811
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency5.135812
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency13.0910415
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency20.024511
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency19.942124
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency19.7919312
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency25.118911
P53Homo sapiens (human)Potency2.511911
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency56.466713
ParkinHomo sapiens (human)Potency14.397822
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency1.258911
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.101422
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency16.944111
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency36.876449
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency37.533959
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency0.891311
phosphopantetheinyl transferaseBacillus subtilisPotency43.151215
plasminogen precursorMus musculus (house mouse)Potency10.610112
polyproteinZika virusPotency2.573013
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency15.848911
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency7.805813
PPM1D proteinHomo sapiens (human)Potency12.7194110
pregnane X nuclear receptorHomo sapiens (human)Potency41.971026
progesterone receptorHomo sapiens (human)Potency23.517814
putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)Potency44.668412
pyruvate kinaseLeishmania mexicana mexicanaPotency12.589322
pyruvate kinase PKM isoform bHomo sapiens (human)Potency25.118922
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency10.000011
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency59.976312
RAR-related orphan receptor gammaMus musculus (house mouse)Potency6.0918210
ras-related protein Rab-9AHomo sapiens (human)Potency29.882813
regulator of G-protein signaling 4Homo sapiens (human)Potency53.929013
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency4.2912313
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.3184411
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency14.197435
serine-protein kinase ATM isoform aHomo sapiens (human)Potency19.952611
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency1.447333
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency19.185812
shiga toxin 1 B subunitEscherichia coli O157:H7Potency7.980511
shiga toxin 1 variant A subunitEscherichia coli O157:H7Potency25.722033
signal transducer and activator of transcription 6, interleukin-4 inducedHomo sapiens (human)Potency25.118933
SMAD family member 2Homo sapiens (human)Potency34.608423
SMAD family member 3Homo sapiens (human)Potency34.608423
Smad3Homo sapiens (human)Potency25.118911
snurportin-1Homo sapiens (human)Potency70.870412
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency14.218428
survival motor neuron protein isoform dHomo sapiens (human)Potency25.230013
TDP1 proteinHomo sapiens (human)Potency15.1406224
thioredoxin glutathione reductaseSchistosoma mansoniPotency0.891311
thioredoxin reductaseRattus norvegicus (Norway rat)Potency26.578437
ThrombopoietinHomo sapiens (human)Potency2.048424
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency19.1567310
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency31.723936
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.750868
tyrosine-protein kinase YesHomo sapiens (human)Potency30.747511
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency1.122011
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency10.610112
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency10.610112
USP1 protein, partialHomo sapiens (human)Potency33.821623
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency39.954111
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency10.897346
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.810714
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency16.063014
VprHuman immunodeficiency virus 1Potency11.220211

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
[tau protein] kinase Oryctolagus cuniculus (rabbit)IC506.000011
1-deoxy-D-xylulose 5-phosphate reductoisomeraseEscherichia coli K-12IC503.500011
17-beta-hydroxysteroid dehydrogenase type 1Homo sapiens (human)IC502.210011
17-beta-hydroxysteroid dehydrogenase type 2Homo sapiens (human)IC5016.500022
3-oxoacyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC504.100011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC5010.469011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki2.991011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC501.106011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.704011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC5014.910011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki7.806011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC5014.910011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki7.806011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC505.000012
5'-nucleotidaseHomo sapiens (human)IC504.565022
5'-nucleotidaseMus musculus (house mouse)IC5034.415022
72 kDa type IV collagenaseHomo sapiens (human)IC509.900011
acetyl-CoA acetyltransferase/HMG-CoA reductaseEnterococcus faecalisIC501,265.390011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50132.920011
AcetylcholinesteraseRattus norvegicus (Norway rat)IC5050.000011
AcetylcholinesteraseHomo sapiens (human)Ki100.200011
Acidic phospholipase A2 2Naja naja (Indian cobra)IC5017.000011
Acidic phospholipase A2 betaCrotalus adamanteus (eastern diamondback rattlesnake)IC500.400011
Adenosine receptor A1Homo sapiens (human)IC5019.904011
Adenosine receptor A1Homo sapiens (human)Ki11.611011
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki10.570033
Adenosine receptor A2aHomo sapiens (human)IC5017.442011
Adenosine receptor A2aHomo sapiens (human)Ki9.792011
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki17.076733
Aldehyde oxidaseHomo sapiens (human)IC501.770012
Aldehyde oxidase 1Cavia porcellus (domestic guinea pig)Ki4.530011
Aldehyde oxidase 1Oryctolagus cuniculus (rabbit)Ki0.060011
Aldehyde oxidase 1 Rattus norvegicus (Norway rat)IC506.400011
Aldehyde oxidase 1 Rattus norvegicus (Norway rat)Ki3.000011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC5010.400023
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC502.000011
ALK tyrosine kinase receptorHomo sapiens (human)IC5040.000011
Alpha-amylase 1A Homo sapiens (human)IC5019.600022
Alpha-glucosidase MAL32Saccharomyces cerevisiae S288CIC5061.000012
Alpha-mannosidaseCanavalia ensiformis (jack bean)IC5049.000011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC504.184055
Amine oxidase [flavin-containing] A Bos taurus (cattle)IC5095.000011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC5040.000011
Amine oxidase [flavin-containing] BBos taurus (cattle)IC5095.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)IC503.933333
Amyloid-beta precursor proteinHomo sapiens (human)IC50200.000022
Androgen receptorHomo sapiens (human)IC501,300.000011
Androgen receptorRattus norvegicus (Norway rat)IC5085.113811
Angiopoietin-1 receptorHomo sapiens (human)IC500.260011
Angiotensin-converting enzyme Homo sapiens (human)IC505,000.000011
Angiotensin-converting enzyme Homo sapiens (human)Ki167.000011
Arachidonate 5-lipoxygenaseSus scrofa (pig)IC502,500.000011
AromataseHomo sapiens (human)Ki111.500022
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50114.266716
Aurora kinase AHomo sapiens (human)IC502.480011
Aurora kinase BHomo sapiens (human)IC502.565022
Beta-hydroxyacyl-ACP dehydratase precursor (Fatty acid synthesis protein)Plasmodium falciparum (malaria parasite P. falciparum)IC504.500012
Beta-secretase 1Homo sapiens (human)IC503.900011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC5020.700011
Bile salt export pumpHomo sapiens (human)IC50393.3000410
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
Botulinum neurotoxin type A Clostridium botulinumIC5020.000011
Botulinum neurotoxin type A Clostridium botulinumKi14.300011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5046.095677
C-C chemokine receptor type 6Homo sapiens (human)IC5022.800011
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC500.600011
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)IC5039.900039
cAMP-dependent protein kinase catalytic subunit betaHomo sapiens (human)IC502.050022
cAMP-dependent protein kinase catalytic subunit gammaHomo sapiens (human)IC502.050022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000016
Carbonic anhydrase 1Homo sapiens (human)Ki105.880034
Carbonic anhydrase 12Homo sapiens (human)Ki9.125022
Carbonic anhydrase 13Homo sapiens (human)Ki4.240011
Carbonic anhydrase 13Mus musculus (house mouse)Ki10.300011
Carbonic anhydrase 14Homo sapiens (human)Ki8.910011
Carbonic anhydrase 2Homo sapiens (human)Ki113.795034
Carbonic anhydrase 3Homo sapiens (human)Ki10.500011
Carbonic anhydrase 4Homo sapiens (human)Ki9.080011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki7.590011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki12.700011
Carbonic anhydrase 6Homo sapiens (human)Ki7.060011
Carbonic anhydrase 7Homo sapiens (human)Ki7.555022
Carbonic anhydrase 9Homo sapiens (human)Ki44.585022
Carbonyl reductase [NADPH] 1Homo sapiens (human)IC503.780011
Carbonyl reductase [NADPH] 1Homo sapiens (human)Ki0.600011
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC5050.000011
Casein kinase II subunit alphaHomo sapiens (human)IC500.303366
Casein kinase II subunit alphaHomo sapiens (human)Ki0.180023
Casein kinase II subunit alpha Rattus norvegicus (Norway rat)IC500.040011
Casein kinase II subunit alpha 3Homo sapiens (human)IC500.350011
Casein kinase II subunit alpha'Homo sapiens (human)IC500.356055
Casein kinase II subunit alpha'Homo sapiens (human)Ki0.170011
Casein kinase II subunit betaHomo sapiens (human)IC500.356055
Casein kinase II subunit betaRattus norvegicus (Norway rat)IC500.040011
Casein kinase II subunit betaHomo sapiens (human)Ki0.170011
Chain A, Casein kinase II subunit alphaHomo sapiens (human)Ki0.020011
Chain A, Estrogen receptor 1 (alpha)Homo sapiens (human)IC500.009011
Chain B, Cell division protein kinase 6Homo sapiens (human)IC500.850011
CruzipainTrypanosoma cruziIC50142.783366
Cyclin homologHerpesvirus saimiri (strain 11)IC500.657514
Cyclin-A1Homo sapiens (human)IC503.390011
Cyclin-A2Homo sapiens (human)IC503.390011
Cyclin-dependent kinase 1Homo sapiens (human)IC50185.395022
Cyclin-dependent kinase 1Oryzias latipes (Japanese medaka)IC500.657514
Cyclin-dependent kinase 2Homo sapiens (human)IC504.195022
Cyclin-dependent kinase 4Homo sapiens (human)IC50125.545022
Cyclin-dependent kinase 5 activator 1Homo sapiens (human)IC500.640025
Cyclin-dependent kinase 6Homo sapiens (human)IC500.696025
Cyclin-dependent-like kinase 5 Homo sapiens (human)IC500.640025
Cysteine protease ATG4BHomo sapiens (human)IC504.250022
Cytochrome P450 1A2Homo sapiens (human)IC5050.000011
Cytochrome P450 2C19Homo sapiens (human)IC5050.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5043.862822
Cytochrome P450 2D6Homo sapiens (human)IC5018.867534
Cytochrome P450 2D6Homo sapiens (human)Ki4.725022
Cytochrome P450 3A4Homo sapiens (human)IC5029.345233
Cytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)IC5067.990011
Death-associated protein kinase 1Homo sapiens (human)IC5098.000011
Dipeptidyl peptidase 3Homo sapiens (human)IC5030.750012
Dipeptidyl peptidase 4Homo sapiens (human)IC500.480011
Dipeptidyl peptidase 4Rattus norvegicus (Norway rat)IC5039.000011
DNA (cytosine-5)-methyltransferase 1Homo sapiens (human)IC5030.000011
DNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)IC50100.000011
DNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)IC50100.000011
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)IC500.450011
DNA gyrase subunit ABacillus subtilis subsp. subtilis str. 168IC506.300011
DNA gyrase subunit AEscherichia coli K-12IC503.89133438
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC5039.96051721
DNA gyrase subunit AStaphylococcus aureusIC5062.71123133
DNA gyrase subunit AEscherichia coli K-12Ki0.044713
DNA gyrase subunit AStaphylococcus aureusKi0.036024
DNA gyrase subunit BBacillus subtilis subsp. subtilis str. 168IC506.300011
DNA gyrase subunit BEscherichia coli K-12IC500.39823438
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC507.29011313
DNA gyrase subunit BMycolicibacterium smegmatisIC5025.852377
DNA gyrase subunit BMycolicibacterium smegmatis MC2 155IC500.046011
DNA gyrase subunit BStaphylococcus aureusIC5025.61383234
DNA gyrase subunit BStreptococcus pneumoniae TIGR4IC500.037011
DNA gyrase subunit BEscherichia coli K-12Ki0.035324
DNA gyrase subunit BStaphylococcus aureusKi0.036024
DNA polymerase betaHomo sapiens (human)IC5041.183333
DNA polymerase betaRattus norvegicus (Norway rat)IC5010.250022
DNA polymerase etaHomo sapiens (human)IC500.062011
DNA polymerase iotaHomo sapiens (human)IC500.062011
DNA polymerase kappaHomo sapiens (human)IC504.500022
DNA primaseMycobacterium tuberculosis CDC1551IC5087.500012
DNA topoisomerase Streptococcus pneumoniaeIC502.030011
DNA topoisomerase 2-alphaHomo sapiens (human)IC50106.905078
DNA topoisomerase 2-betaHomo sapiens (human)IC5022.153333
DNA topoisomerase 4 subunit ABacillus subtilis subsp. subtilis str. 168IC501.700011
DNA topoisomerase 4 subunit AEscherichia coli K-12IC5051.000011
DNA topoisomerase 4 subunit AStaphylococcus aureusIC5011.58811516
DNA topoisomerase 4 subunit AEscherichia coli K-12Ki0.044713
DNA topoisomerase 4 subunit BBacillus subtilis subsp. subtilis str. 168IC501.700011
DNA topoisomerase 4 subunit BStaphylococcus aureusIC5014.56751212
DNA topoisomerase 4 subunit BEscherichia coli K-12Ki0.044713
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)IC505.000022
Dual specificity mitogen-activated protein kinase kinase 4Homo sapiens (human)IC500.400011
dual specificity protein phosphatase 3Homo sapiens (human)IC501.105022
dual specificity protein phosphatase 6Rattus norvegicus (Norway rat)IC5039.500011
Dual specificity tyrosine-phosphorylation-regulated kinase 1AHomo sapiens (human)IC5040.000011
Ectonucleoside triphosphate diphosphohydrolase 1Mus musculus (house mouse)IC500.500011
ELAV-like protein 3Homo sapiens (human)IC500.600011
Enoyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC501.000022
Ephrin type-B receptor 4Homo sapiens (human)IC501.830011
Epidermal growth factor receptorHomo sapiens (human)IC5027.6436814
Estrogen receptorHomo sapiens (human)IC501.34772325
Estrogen receptorHomo sapiens (human)Ki0.204522
Estrogen receptor betaHomo sapiens (human)IC502.05692427
Estrogen receptor betaHomo sapiens (human)Ki0.012322
eukaryotic translation initiation factor 4 gamma 1 isoform 4Homo sapiens (human)IC5047.671411
eukaryotic translation initiation factor 4E isoform 1Mus musculus (house mouse)IC5047.671411
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)IC501,600.000022
Focal adhesion kinase 1Homo sapiens (human)IC503.110011
G-protein coupled receptor 35Homo sapiens (human)IC500.100011
G1/S-specific cyclin-D1Homo sapiens (human)IC50125.545022
G2/mitotic-specific cyclin-BMarthasterias glacialis (spiny starfish)IC500.657514
G2/mitotic-specific cyclin-B1Homo sapiens (human)IC50185.395022
G2/mitotic-specific cyclin-B2Homo sapiens (human)IC500.790011
G2/mitotic-specific cyclin-B3Homo sapiens (human)IC500.790011
GABA theta subunitRattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC5034.303336
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC5034.303336
Genome polyproteinHepatitis C virus (isolate BK)IC5036.000011
Genome polyprotein IC500.750011
Genome polyprotein Zika virusIC5014.200011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)IC505.180011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki4.865544
Glutathione reductase, mitochondrialHomo sapiens (human)IC5022.800011
Glutathione S-transferasePlasmodium falciparum 3D7IC5074.400011
Glutathione S-transferase Mu 1Mus musculus (house mouse)IC50100.000011
Glutathione S-transferase PHomo sapiens (human)IC5063.550022
Glycogen phosphorylase, muscle formOryctolagus cuniculus (rabbit)IC5042.914534
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC503.210022
Glycogen synthase kinase-3 betaHomo sapiens (human)IC504.640033
Glycogen synthase kinase-3 betaRattus norvegicus (Norway rat)IC500.657514
heat shock 70kDa protein 1AHomo sapiens (human)IC5066.920033
heat shock cognate 71 kDa protein isoform 1Homo sapiens (human)IC5099.600022
heat shock cognate 71 kDa protein isoform 2Homo sapiens (human)IC5099.600022
Heat shock protein HSP 90Oryctolagus cuniculus (rabbit)IC50382.000022
Heat shock protein HSP 90-betaHomo sapiens (human)IC50231.000011
Hepatocyte growth factor receptorHomo sapiens (human)IC500.580011
Hypoxia-inducible factor 1-alphaHomo sapiens (human)IC500.250011
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC508.410011
Inhibitor of nuclear factor kappa-B kinase subunit alphaHomo sapiens (human)IC5010.000011
Inhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)IC505.990022
Insulin receptorHomo sapiens (human)IC500.340011
Insulin-like growth factor 1 receptorHomo sapiens (human)IC500.250011
Integrase Human immunodeficiency virus 1IC5023.525088
L-ornithine N(5)-monooxygenaseAspergillus fumigatus Af293IC5011.000022
Lactoylglutathione lyaseHomo sapiens (human)Ki13.182611
LacZ protein (plasmid)Escherichia coliIC5066.600011
likely tRNA 2'-phosphotransferaseCandida albicans SC5314IC500.291322
M17 leucyl aminopeptidasePlasmodium falciparum 3D7IC50138.080011
Macrophage migration inhibitory factorHomo sapiens (human)IC504.770011
Macrophage migration inhibitory factorHomo sapiens (human)Ki1.950011
Maltase-glucoamylase, intestinalHomo sapiens (human)IC506.505022
Maltase-glucoamylase, intestinalHomo sapiens (human)Ki10.400011
Mcl-1Homo sapiens (human)IC5027.285022
Microtubule-associated proteins 1A/1B light chain 3AHomo sapiens (human)IC5042.900011
Microtubule-associated proteins 1A/1B light chain 3AHomo sapiens (human)Ki8.800011
Microtubule-associated proteins 1A/1B light chain 3BHomo sapiens (human)IC50172.000011
Microtubule-associated proteins 1A/1B light chain 3BHomo sapiens (human)Ki19.300011
Mitogen-activated protein kinase 10Homo sapiens (human)IC5022.233313
Mitogen-activated protein kinase 14Homo sapiens (human)IC5022.233313
Mitogen-activated protein kinase kinase kinase 8Homo sapiens (human)IC502.370011
MO15-related protein kinase Pfmrk Plasmodium falciparum (malaria parasite P. falciparum)IC5093.000011
mothers against decapentaplegic homolog 3 isoform 1Homo sapiens (human)IC500.142011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC500.500011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5017.900011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5095.721716
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.570014
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.570013
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.570013
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.570013
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.570013
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC5098.266733
Non-structural protein 1 Dengue virusIC501.700011
NUAK family SNF1-like kinase 1Homo sapiens (human)IC500.510011
NucleophosminHomo sapiens (human)IC5040.000011
Ornithine decarboxylaseHomo sapiens (human)IC5026.000011
Oxysterols receptor LXR-alphaHomo sapiens (human)IC5046.000034
Oxysterols receptor LXR-betaHomo sapiens (human)IC5048.000023
Pancreatic alpha-amylaseSus scrofa (pig)IC50200.000011
Pancreatic triacylglycerol lipaseSus scrofa (pig)IC50100.000011
Phosphatidylcholine 2-acylhydrolase Apis mellifera (honey bee)IC500.040011
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTENHomo sapiens (human)IC5013.300011
Phosphodiesterase isozyme 4 Homo sapiens (human)IC50125.000011
Phospholipase A2Apis mellifera (honey bee)IC5013.357177
Phospholipase A2Homo sapiens (human)IC503.900011
Phospholipase A2, membrane associatedHomo sapiens (human)IC50320.980055
Phospholipase A2, membrane associatedRattus norvegicus (Norway rat)IC501,019.200022
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC503.900011
Platelet-derived growth factor receptor betaHomo sapiens (human)IC501.300011
Polypeptide N-acetylgalactosaminyltransferase 2Homo sapiens (human)IC501.720022
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC502.500011
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC500.950011
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC501.400011
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC509.033011
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)IC50100.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC501,014.82871727
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki125.000012
Prostaglandin G/H synthase 1Homo sapiens (human)IC5080.000011
Protease Human immunodeficiency virus 1IC50219.000011
Proteasome subunit beta type-5Homo sapiens (human)IC5037.130022
Protein kinase C alpha typeHomo sapiens (human)IC5056.875028
Protein kinase C beta typeHomo sapiens (human)IC50150.000011
Protein kinase C epsilon typeHomo sapiens (human)IC50150.000011
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)IC5040.000011
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC5031.066766
Pyruvate kinase PKMHomo sapiens (human)IC500.900011
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)IC5036.670022
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC503.540011
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC5040.000011
Receptor-type tyrosine-protein phosphatase epsilonHomo sapiens (human)IC50500.000011
Receptor-type tyrosine-protein phosphatase etaHomo sapiens (human)IC50111.500011
Regulator of G-protein signaling 17Homo sapiens (human)IC5027.933855
ReninHomo sapiens (human)IC500.980011
Replicase polyprotein 1abBetacoronavirus England 1IC507.600011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5010.300011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5010.300022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki4.200011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi4.200022
Serine/threonine-protein kinase B-rafHomo sapiens (human)IC501.760011
Serine/threonine-protein kinase pim-1Homo sapiens (human)IC500.850011
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC503.340011
Serine/threonine-protein kinase PLK4Homo sapiens (human)IC502.970011
SialidaseClostridium perfringensIC5012.050011
Sialidase-2Homo sapiens (human)IC50380.000011
Signal transducer and activator of transcription 3Homo sapiens (human)IC5024.800011
Sodium-dependent dopamine transporter Homo sapiens (human)IC5016.918011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki13.442011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.395011
Solute carrier family 2, facilitated glucose transporter member 1Homo sapiens (human)Ki7.000033
Solute carrier family 2, facilitated glucose transporter member 4Mus musculus (house mouse)IC5020.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC505.000011
Solute carrier family 22 member 6Homo sapiens (human)IC500.270011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC509.120111
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki5.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC503.890411
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki2.960011
Squalene monooxygenase Rattus norvegicus (Norway rat)IC502.000011
Steroid hormone receptor ERR1Homo sapiens (human)IC500.010011
Steroid hormone receptor ERR2Homo sapiens (human)IC500.395011
Substance-K receptorCavia porcellus (domestic guinea pig)IC5077.100011
Substance-P receptorCavia porcellus (domestic guinea pig)IC5077.100011
SUMO-conjugating enzyme UBC9Homo sapiens (human)IC5011.200022
SUMO1 activating enzyme subunit 1Homo sapiens (human)IC5011.200022
TatHuman immunodeficiency virus 1IC501.669011
Telomerase reverse transcriptaseHomo sapiens (human)IC500.780011
Telomere resolvase ResTBorreliella burgdorferi B31IC508.670011
Testosterone 17-beta-dehydrogenase 3Homo sapiens (human)IC5031.350012
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)IC50176.800022
Thioredoxin reductase 2, mitochondrialHomo sapiens (human)IC50176.800022
Thioredoxin reductase 3Homo sapiens (human)IC50176.800022
Thromboxane-A synthase Homo sapiens (human)IC507.720011
Tissue alpha-L-fucosidaseBos taurus (cattle)IC5054.000011
Transcription factor p65Homo sapiens (human)IC5010.000011
Translin-associated protein XHomo sapiens (human)IC503.500011
TransthyretinHomo sapiens (human)IC507.800011
Triosephosphate isomeraseHomo sapiens (human)IC501,000.000011
Triosephosphate isomeraseOryctolagus cuniculus (rabbit)Ki123.000011
Triosephosphate isomerase, glycosomalTrypanosoma cruziIC506.500011
Tryptophan 2,3-dioxygenaseHomo sapiens (human)IC50100.000011
Tubulin alpha-1A chainHomo sapiens (human)IC5011.270011
Tubulin alpha-1B chainHomo sapiens (human)IC5011.270011
Tubulin alpha-1C chainHomo sapiens (human)IC5011.270011
Tubulin alpha-3C chainHomo sapiens (human)IC5011.270011
Tubulin alpha-3E chainHomo sapiens (human)IC5011.270011
Tubulin alpha-4A chainHomo sapiens (human)IC5011.270011
Tubulin beta chainHomo sapiens (human)IC5011.270011
Tubulin beta-1 chainHomo sapiens (human)IC5011.270011
Tubulin beta-2A chainHomo sapiens (human)IC5011.270011
Tubulin beta-2B chainHomo sapiens (human)IC5011.270011
Tubulin beta-3 chainHomo sapiens (human)IC5011.270011
Tubulin beta-4A chainHomo sapiens (human)IC5011.270011
Tubulin beta-4B chainHomo sapiens (human)IC5011.270011
Tubulin beta-6 chainHomo sapiens (human)IC5011.270011
Tubulin beta-8 chainHomo sapiens (human)IC5011.270011
TyrosinaseMus musculus (house mouse)IC50500.000011
Tyrosine-protein kinase ABL1Homo sapiens (human)IC5041.666739
Tyrosine-protein kinase ABL2Homo sapiens (human)IC5010.000011
Tyrosine-protein kinase CSKHomo sapiens (human)IC5050.714317
Tyrosine-protein kinase FgrRattus norvegicus (Norway rat)IC503.500011
Tyrosine-protein kinase FynHomo sapiens (human)IC5031.680522
Tyrosine-protein kinase Lyn Rattus norvegicus (Norway rat)IC507.500011
Tyrosine-protein kinase SYKHomo sapiens (human)IC5027.000022
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC505.400044
Tyrosine-protein phosphatase non-receptor type 11Homo sapiens (human)IC503.566733
Tyrosine-protein phosphatase non-receptor type 2Homo sapiens (human)IC5020.900022
Tyrosine-protein phosphatase non-receptor type 6Homo sapiens (human)IC5015.450022
Tyrosine-protein phosphatase non-receptor type 7Homo sapiens (human)IC5075.700011
Ubiquitin carboxyl-terminal hydrolase 15Homo sapiens (human)IC5031.400015
Ubiquitin carboxyl-terminal hydrolase 2Homo sapiens (human)IC5031.400015
Ubiquitin carboxyl-terminal hydrolase isozyme L1Homo sapiens (human)IC5031.400015
Ubiquitin carboxyl-terminal hydrolase isozyme L3Homo sapiens (human)IC5031.400015
Ubiquitin carboxyl-terminal hydrolase isozyme L5Homo sapiens (human)IC5031.400015
Ubiquitin-like modifier activating enzyme 2Homo sapiens (human)IC5011.200022
unnamed protein productAspergillus oryzae RIB40IC5052.719522
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC500.790011
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC501.540011
VifHuman immunodeficiency virus 1IC500.450011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC501.730011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC50412.276733
Zinc finger protein GLI1Homo sapiens (human)IC5032.000022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Kd4.598244
Amine oxidase [flavin-containing] AHomo sapiens (human)EC501.600011
ATP-dependent translocase ABCB1Homo sapiens (human)Kd26.302711
Chain A, GyraseEscherichia coliKd1.200011
Chain A, TransthyretinHomo sapiens (human)Kd2.150014
Cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)EC508.290055
Cystic fibrosis transmembrane conductance regulatorRattus norvegicus (Norway rat)Kd40.000011
DNA gyrase subunit BEscherichia coli K-12Kd0.017522
DNA topoisomerase 2-alphaHomo sapiens (human)EC500.720022
DNA topoisomerase 2-betaHomo sapiens (human)EC500.720022
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)Kd0.089011
Egl nine homolog 1Homo sapiens (human)EC5050.000011
Env polyprotein Human immunodeficiency virus 1EC50100.000011
Estrogen receptorHomo sapiens (human)EC500.998066
Estrogen receptor betaHomo sapiens (human)EC500.163599
G-protein coupled bile acid receptor 1Homo sapiens (human)EC501.040011
G-protein coupled receptor 35Homo sapiens (human)EC501.535022
Genome polyprotein Zika virusEC5024.800011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Kd3.640011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50300.000011
Heat shock factor protein 1Homo sapiens (human)EC501.850022
Heat shock protein HSP 90-alphaHomo sapiens (human)EC50700.000011
Heat shock protein HSP 90-alphaHomo sapiens (human)Kd500.000011
Heat shock protein HSP 90-betaHomo sapiens (human)EC50700.000011
Heat shock protein HSP 90-betaHomo sapiens (human)Kd500.000011
L-ornithine N(5)-monooxygenaseAspergillus fumigatus Af293Kd1.400022
Microtubule-associated proteins 1A/1B light chain 3AHomo sapiens (human)Kd7.500011
Microtubule-associated proteins 1A/1B light chain 3BHomo sapiens (human)Kd17.400011
Multidrug resistance protein MdtKEscherichia coli K-12Kd90.900011
Nuclear receptor subfamily 4 group A member 1Homo sapiens (human)Kd0.300033
Oxysterols receptor LXR-alphaHomo sapiens (human)EC5050.000011
Oxysterols receptor LXR-betaHomo sapiens (human)EC5050.000011
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC50100.000011
Polycomb protein EEDHomo sapiens (human)Kd2.813333
Polypeptide N-acetylgalactosaminyltransferase 2Homo sapiens (human)Kd0.371011
Prolyl hydroxylase EGLN2Homo sapiens (human)EC5050.000011
Prolyl hydroxylase EGLN3Homo sapiens (human)EC5050.000011
Sex hormone-binding globulinHomo sapiens (human)Kd39.810711
streptokinase A precursorStreptococcus pyogenes M1 GASEC501.107012
Transmembrane prolyl 4-hydroxylaseHomo sapiens (human)EC5050.000011
Triosephosphate isomerase, glycosomalTrypanosoma cruziKd10.400011
Tyrosine-protein kinase SYKHomo sapiens (human)EC5019.000011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)Kd6.080011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseElectrophorus electricus (electric eel)EC24250.000011
Androgen receptorHomo sapiens (human)EC1504.400011
ATP-dependent translocase ABCB1Homo sapiens (human)Km4,300.000022
CAAX prenyl protease 2 isoform 2Homo sapiens (human)AC5041.000011
Cell division inhibitor SulAEscherichia coli K-12Activity6.300011
CholinesteraseEquus caballus (horse)EC16250.000011
DNA gyrase subunit AEscherichia coli K-12Activity9.196055
DNA gyrase subunit AStaphylococcus aureusCC5056.950036
DNA gyrase subunit AEscherichia coli K-12EC1.200011
DNA gyrase subunit AStaphylococcus aureusMIC0.010011
DNA gyrase subunit BEscherichia coli K-12Activity0.400011
DNA gyrase subunit BStaphylococcus aureusCC502.850012
DNA gyrase subunit BEscherichia coli K-12EC1.200011
DNA gyrase subunit BStaphylococcus aureusMIC0.010011
DNA topoisomerase 2-alphaHomo sapiens (human)Activity56.250022
DNA topoisomerase 2-alphaHomo sapiens (human)CC50150.000012
DNA topoisomerase 2-alphaHomo sapiens (human)EC2150.000011
DNA topoisomerase 2-alphaHomo sapiens (human)IC9033.000022
DNA topoisomerase 2-alphaHomo sapiens (human)INH50.000011
DNA topoisomerase 2-betaHomo sapiens (human)IC9033.000022
DNA topoisomerase 4 subunit AStaphylococcus aureusCC500.300012
DNA topoisomerase 4 subunit BStaphylococcus aureusCC500.300012
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvMIC5.485022
Glucocorticoid receptorHomo sapiens (human)EC1504.400011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Km26.765044
Heat shock protein HSP 90-betaHomo sapiens (human)Activity700.000011
interferon gamma precursorHomo sapiens (human)AC5024.292524
LactoperoxidaseBos taurus (cattle)Km0.300011
Oxysterols receptor LXR-alphaHomo sapiens (human)LC5025.000011
Oxysterols receptor LXR-betaHomo sapiens (human)LC5025.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)INH18.000011
Prenyltransferase homologStreptomyces coelicolor A3(2)Km330.000011
Quinone oxidoreductaseMus musculus (house mouse)CD22.900011
Serine/threonine-protein kinase pim-1Homo sapiens (human)-Log IC500.070011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km149.000011