Page last updated: 2024-08-05 15:18:42

EC 5.99.1.2 (DNA topoisomerase) inhibitor

A topoisomerase inhibitor that inhibits the bacterial enzymes of the DNA topoisomerases, Type I class (EC 5.99.1.2) that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. These bacterial enzymes reduce the topological stress in the DNA structure by relaxing negatively, but not positively, supercoiled DNA.

ChEBI ID: 50276

Members (19)

MemberDefinitionClass
amarogentinA secoiridoid glycoside that consists of (4aS,5R,6R)-5-ethenyl-6-hydroxy-4,4a,5,6-tetrahydro-1H,3H-pyrano[3,4-c]pyran-1-one having a 2-O-[(3,3',5-trihydroxybiphenyl-2-yl)carbonyl]-beta-D-glucopyranosyl group attached at position 6 via a glycosidic linkage.amarogentin
camptothecinA pyranoindolizinoquinoline that is pyrano[3',4':6,7]indolizino[1,2-b]quinoline which is substituted by oxo groups at positions 3 and 14, and by an ethyl group and a hydroxy group at position 4 (the S enantiomer).camptothecin
diflomotecanAn organic heteropentacyclic compound that is (5R)-8-[(6,7-difluoroquinolin-3-yl)methyl]-5-ethyl-5-hydroxy-1,4,5,8-tetrahydrooxepino[3,4-c]pyridine-3,9-dione in which position 7 of the oxepinopyridine moiety is joined to position 3 of the difluoroquinoine ring by a single bond. An E-ring modified camptothecin analogue that has greater lactone stability in plasma compared with other topoisomerase I inhibitors.diflomotecan
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
discretamineA berberine alkaloid isolated from Corydalis saxicola.(S)-scoulerine
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
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
homocamptothecinAn organic heteropentacyclic compound that is (5R)-5-ethyl-5-hydroxy-8-(quinolin-3-ylmethyl)-1,4,5,8-tetrahydrooxepino[3,4-c]pyridine-3,9-dione in which position 7 of the oxepinopyridine group has been joined to position 2 of the quinoline ring by a single bond. A semisynthetic analogue of camptothecin, it is an inhibitor of topoisomerase I.(R)-homocamptothecin
irinotecanA member of the class of pyranoindolizinoquinolines that is the carbamate ester obtained by formal condensation of the carboxy group of [1,4'-bipiperidine]-1'-carboxylic acid with the phenolic hydroxy group of (4S)-4,11-diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2- hydrochloride]quinoline-3,14-dione. Used (in the form of its hydrochloride salt trihydrate) in combination with fluorouracil and leucovorin, for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy. It is converted via hydrolysis of the carbamate linkage to its active metabolite, SN-38, which is ~1000 times more active.irinotecan
irinotecan hydrochlorideA hydrochloride obtained by combining irinotecan with one molar equivalent of hydrochloric acid. Used (in the form of its trihydrate) in combination with fluorouracil and leucovorin, for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy. It is converted via hydrolysis of the carbamate linkage to its active metabolite, SN-38, which is ~1000 times more active.irinotecan hydrochloride (anhydrous)
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
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
morinA pentahydroxyflavone that is 7-hydroxyflavonol bearing three additional hydroxy substituents at positions 2' 4' and 5.morin
rubitecanA pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.rubitecan
saintopinA member of the class of tetracenequinones that is tetracene-5,12-dione in which the hydrogens at positions 1, 3, 8, 10, and 11 have been replaced by hydroxy groups. Isolated from Paecilomyces.saintopin
sn 38A member of the class of pyranoindolizinoquinolines that is (4S)-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione bearing two additional ethyl substituents at positions 4 and 11 as well as two additional hydroxy substituents at positions 4 and 9. It is the active metabolite of irinotecan and is ~1000 times more active than irinotecan itself.SN-38
topopyrone cA naphthochromene that is 4H-naphtho[2,3-h]chromene-4,7,12-trione substituted by hydroxy groups at positions 5, 9 and 11 and a methyl group at position 2. It is isolated from fungal strains Phoma and Penicillium and acts as an inhibitor of the enzyme topoisomerase I.topopyrone C
topotecanA pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.topotecan

Research

Studies (21,648)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,650 (12.24)18.7374
1990's2,309 (10.67)18.2507
2000's6,356 (29.36)29.6817
2010's7,651 (35.34)24.3611
2020's2,682 (12.39)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,989 (16.50%)5.53%
Reviews3,219 (10.65%)6.00%
Case Studies2,039 (6.74%)4.05%
Observational118 (0.39%)0.25%
Other19,865 (65.71%)84.16%

Protein Targets (509)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency10.7701115
15-lipoxygenase, partialHomo sapiens (human)Potency10.272316
67.9K proteinVaccinia virusPotency15.302628
acetylcholinesteraseHomo sapiens (human)Potency41.7205410
activating transcription factor 6Homo sapiens (human)Potency0.627013
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency10.2478111
alpha-galactosidaseHomo sapiens (human)Potency18.1258313
Alpha-synucleinHomo sapiens (human)Potency5.173511
Amyloid-beta precursor proteinHomo sapiens (human)Potency5.173511
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency7.459812
AR proteinHomo sapiens (human)Potency2.6413832
aryl hydrocarbon receptorHomo sapiens (human)Potency39.325234
ATAD5 protein, partialHomo sapiens (human)Potency10.238637
Ataxin-2Homo sapiens (human)Potency25.382325
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency14.299825
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency29.249327
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency2.393411
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency5.211911
beta-2 adrenergic receptorHomo sapiens (human)Potency0.651311
Bloom syndrome protein isoform 1Homo sapiens (human)Potency18.547727
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency25.456512
C-terminal-binding protein 1Homo sapiens (human)Potency16.946911
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency16.032114
caspase-1 isoform alpha precursorHomo sapiens (human)Potency39.810711
caspase-3Cricetulus griseus (Chinese hamster)Potency10.559012
caspase-3Homo sapiens (human)Potency16.032114
Caspase-7Cricetulus griseus (Chinese hamster)Potency10.559012
Caspase-7Homo sapiens (human)Potency15.848911
Cellular tumor antigen p53Homo sapiens (human)Potency10.501428
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency11.717628
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency14.9712113
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency11.977028
Chain A, Beta-lactamaseEscherichia coli K-12Potency62.619023
Chain A, CruzipainTrypanosoma cruziPotency13.942229
Chain A, Ferritin light chainEquus caballus (horse)Potency19.486226
Chain A, HADH2 proteinHomo sapiens (human)Potency9.8294215
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency40.070412
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.1645410
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency12.939826
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.084925
Chain B, HADH2 proteinHomo sapiens (human)Potency9.8294215
chromobox protein homolog 1Homo sapiens (human)Potency27.379225
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency0.449234
cytochrome P450 2C19 precursorHomo sapiens (human)Potency14.345414
cytochrome P450 2C9 precursorHomo sapiens (human)Potency13.180214
cytochrome P450 2C9, partialHomo sapiens (human)Potency12.276213
cytochrome P450 2D6Homo sapiens (human)Potency16.280111
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency13.9336210
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency14.852613
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.843315
D(1A) dopamine receptorHomo sapiens (human)Potency1.683612
D(1A) dopamine receptorSus scrofa (pig)Potency0.104011
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency11.836222
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency11.868522
DNA polymerase betaHomo sapiens (human)Potency1.729213
DNA polymerase eta isoform 1Homo sapiens (human)Potency32.620913
DNA polymerase III, partialBacillus subtilisPotency18.887611
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency34.796017
DNA polymerase kappa isoform 1Homo sapiens (human)Potency5.059417
endonuclease IVEscherichia coliPotency11.750422
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.9360836
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency0.190425
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency2.83391032
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.5622110
EWS/FLI fusion proteinHomo sapiens (human)Potency1.0017421
eyes absent homolog 2 isoform aHomo sapiens (human)Potency8.493611
farnesoid X nuclear receptorHomo sapiens (human)Potency2.074026
flap endonuclease 1Homo sapiens (human)Potency36.004528
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency63.095711
Fumarate hydrataseHomo sapiens (human)Potency9.329019
GVesicular stomatitis virusPotency12.276213
GABA theta subunitRattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency13.933615
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency13.933615
gemininHomo sapiens (human)Potency12.1749416
GLI family zinc finger 3Homo sapiens (human)Potency0.623739
glp-1 receptor, partialHomo sapiens (human)Potency10.000011
GLS proteinHomo sapiens (human)Potency15.004926
glucocerebrosidaseHomo sapiens (human)Potency14.719315
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency17.739936
glucokinase regulatory proteinHomo sapiens (human)Potency10.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency0.014111
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency4.880225
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency0.014111
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency0.014111
glyceraldehyde-3-phosphate dehydrogenase isoform 1Homo sapiens (human)Potency79.432811
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency22.387211
heat shock protein beta-1Homo sapiens (human)Potency0.181426
hemoglobin subunit betaHomo sapiens (human)Potency3.668333
hexokinase-4 isoform 1Homo sapiens (human)Potency10.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency10.1828224
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.454917
histone deacetylase 9 isoform 3Homo sapiens (human)Potency11.125511
Histone H2A.xCricetulus griseus (Chinese hamster)Potency12.286829
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency28.837413
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency12.276213
huntingtin isoform 2Homo sapiens (human)Potency8.790113
hypothetical protein, conservedTrypanosoma bruceiPotency9.942924
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency0.406224
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency0.102624
IDH1Homo sapiens (human)Potency0.912013
importin subunit beta-1 isoform 1Homo sapiens (human)Potency15.848911
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency12.276216
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency10.671323
Integrin alpha-IIbHomo sapiens (human)Potency12.572012
Integrin beta-3Homo sapiens (human)Potency12.572012
Interferon betaHomo sapiens (human)Potency12.9539319
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency1.161729
lethal factor (plasmid)Bacillus anthracis str. A2012Potency7.539914
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency15.848911
LuciferasePhotinus pyralis (common eastern firefly)Potency14.493339
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency18.683324
M-phase phosphoprotein 8Homo sapiens (human)Potency42.750714
Microtubule-associated protein tauHomo sapiens (human)Potency13.8110219
mitogen-activated protein kinase 1Homo sapiens (human)Potency19.952611
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.304612
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency29.461015
neuropeptide S receptor isoform AHomo sapiens (human)Potency19.783012
NFKB1 protein, partialHomo sapiens (human)Potency7.182126
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency3.311712
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency8.799239
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency10.537923
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)Potency2.2032222
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency6.309611
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency1.8583312
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency25.118911
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency2.526122
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.477625
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency6.117412
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency12.9709310
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.313825
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency12.412722
phosphopantetheinyl transferaseBacillus subtilisPotency28.564616
plasminogen precursorMus musculus (house mouse)Potency8.528012
polyproteinZika virusPotency9.329019
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)Potency7.185516
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency2.990412
PPM1D proteinHomo sapiens (human)Potency12.5525110
pregnane X nuclear receptorHomo sapiens (human)Potency26.199224
progesterone receptorHomo sapiens (human)Potency1.707324
putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)Potency15.848911
pyruvate kinaseLeishmania mexicana mexicanaPotency17.900824
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)Potency19.952611
RAR-related orphan receptor gammaMus musculus (house mouse)Potency7.350129
ras-related protein Rab-9AHomo sapiens (human)Potency23.253612
regulator of G-protein signaling 4Homo sapiens (human)Potency23.153115
relaxin receptor 1 isoform 1Homo sapiens (human)Potency12.589311
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency1.0709310
retinoid X nuclear receptor alphaHomo sapiens (human)Potency18.358238
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency0.449234
serine-protein kinase ATM isoform aHomo sapiens (human)Potency19.952611
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency0.471745
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency4.640212
SMAD family member 2Homo sapiens (human)Potency0.199511
SMAD family member 3Homo sapiens (human)Potency0.199511
Smad3Homo sapiens (human)Potency0.100011
snurportin-1Homo sapiens (human)Potency15.848911
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency6.957023
survival motor neuron protein isoform dHomo sapiens (human)Potency1.601214
TAR DNA-binding protein 43Homo sapiens (human)Potency3.981111
TDP1 proteinHomo sapiens (human)Potency1.9581225
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.8128415
ThrombopoietinHomo sapiens (human)Potency1.228826
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency8.3655312
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency32.464812
thyroid stimulating hormone receptorHomo sapiens (human)Potency41.4446511
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency23.526723
tyrosine-protein kinase YesHomo sapiens (human)Potency61.349411
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency9.807422
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency8.528012
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency8.528012
USP1 protein, partialHomo sapiens (human)Potency40.991527
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency7.383428
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency18.6434510
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency12.092815
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency6.096714
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
10 kDa chaperonin Escherichia coliIC506.850022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC5011.000011
3-oxoacyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC502.300011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC5017.758512
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki11.300512
5-hydroxytryptamine receptor 6Homo sapiens (human)IC5016.001011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki7.429011
5'-nucleotidaseHomo sapiens (human)IC501.850011
5'-nucleotidaseMus musculus (house mouse)IC500.040011
60 kDa chaperoninEscherichia coli K-12IC50250.000011
60 kDa chaperonin Escherichia coliIC506.850022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC5011.000011
acetyl-CoA acetyltransferase/HMG-CoA reductaseEnterococcus faecalisIC501,265.390011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50132.920011
AcetylcholinesteraseHomo sapiens (human)IC501.827011
AcetylcholinesteraseHomo sapiens (human)Ki0.050511
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.026411
Acidic phospholipase A2 2Naja naja (Indian cobra)IC5017.000011
Acidic phospholipase A2 betaCrotalus adamanteus (eastern diamondback rattlesnake)IC500.400011
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki10.570033
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki7.615022
Adenosine receptor A3Homo sapiens (human)IC500.356011
Adenosine receptor A3Homo sapiens (human)Ki17.100522
Aldehyde dehydrogenase, mitochondrialHomo sapiens (human)IC503.400011
Aldehyde oxidase 1Cavia porcellus (domestic guinea pig)Ki4.530011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC500.200011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC5070.370011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki69.812011
ALK tyrosine kinase receptorHomo sapiens (human)IC5040.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.356011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.356011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
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
Alpha-2C adrenergic receptorHomo sapiens (human)IC503.171011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.461011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5013.734011
Amyloid-beta precursor proteinHomo sapiens (human)IC5093.820055
Angiopoietin-1 receptorHomo sapiens (human)IC500.260011
Angiotensin-converting enzyme Homo sapiens (human)IC505,000.000011
Angiotensin-converting enzyme 2 Homo sapiens (human)IC509.350011
apelin receptorHomo sapiens (human)IC502.630011
Apoptotic peptidase activating factor 1Homo sapiens (human)IC5058.150022
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5092.066713
Aurora kinase AHomo sapiens (human)IC502.480011
Aurora kinase BHomo sapiens (human)IC503.605022
Beta-hydroxyacyl-ACP dehydratase precursor (Fatty acid synthesis protein)Plasmodium falciparum (malaria parasite P. falciparum)IC508.000011
Beta-secretase 1Homo sapiens (human)IC508.100022
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC5020.700011
bifunctional UDP-N-acetylglucosamine pyrophosphorylase/glucosamine-1-phosphate N-acetyltransferaseMycobacterium tuberculosis H37RvIC5085.030011
Bile salt export pumpHomo sapiens (human)IC50108.800035
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5017.586534
C-C chemokine receptor type 2Homo sapiens (human)IC502.468011
C-C chemokine receptor type 2Homo sapiens (human)Ki0.954011
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
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC500.600011
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)IC502.050022
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)IC50108.833313
Carbamate kinaseGiardia intestinalisIC500.600011
Carbonic anhydrase 1Homo sapiens (human)Ki59.715048
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)Ki63.672548
Carbonic anhydrase 3Bos taurus (cattle)Ki13.550014
Carbonic anhydrase 3Homo sapiens (human)Ki10.500011
Carbonic anhydrase 4Homo sapiens (human)Ki12.656025
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
Casein kinase II subunit alphaHomo sapiens (human)IC504.024055
Casein kinase II subunit alphaHomo sapiens (human)Ki0.020011
Casein kinase II subunit alpha Rattus norvegicus (Norway rat)IC500.040011
Casein kinase II subunit alpha 3Homo sapiens (human)IC5010.000011
Casein kinase II subunit alpha'Homo sapiens (human)IC505.020044
Casein kinase II subunit betaHomo sapiens (human)IC505.020044
Casein kinase II subunit betaRattus norvegicus (Norway rat)IC500.040011
Caspase-1Homo sapiens (human)IC501.800011
caspase-3 isoform a preproproteinHomo sapiens (human)IC504.300011
caspase-9 isoform alpha precursorHomo sapiens (human)IC504.300011
Cationic trypsinBos taurus (cattle)IC50110.800011
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.026411
Chain A, Casein kinase II subunit alphaHomo sapiens (human)Ki0.020011
Class A sortase SrtA Staphylococcus aureusIC5031.260033
CruzipainTrypanosoma cruziIC50142.000022
Cyclin-A1Homo sapiens (human)IC503.390011
Cyclin-A2Homo sapiens (human)IC503.390011
Cyclin-dependent kinase 2Homo sapiens (human)IC503.390011
Cyclin-dependent kinase 4Homo sapiens (human)IC501.090011
Cysteine protease ATG4BHomo sapiens (human)IC504.250022
Cytochrome P450 1A2Homo sapiens (human)IC504.000011
Cytochrome P450 2D6Homo sapiens (human)IC504.770011
Cytochrome P450 2D6Homo sapiens (human)Ki1.950011
Cytochrome P450 3A4Homo sapiens (human)IC501.521111
Cytochrome P450 3A4Homo sapiens (human)Ki25.000012
D(1A) dopamine receptorHomo sapiens (human)IC502.158011
D(1A) dopamine receptorHomo sapiens (human)Ki0.550522
D(2) dopamine receptorHomo sapiens (human)IC5023.018011
D(2) dopamine receptorHomo sapiens (human)Ki3.943522
D(3) dopamine receptorHomo sapiens (human)IC501.084011
D(3) dopamine receptorHomo sapiens (human)Ki0.368011
D(4) dopamine receptorHomo sapiens (human)IC503.150011
D(4) dopamine receptorHomo sapiens (human)Ki1.105011
Death-associated protein kinase 1Homo sapiens (human)IC506.300022
Deoxyribonuclease-1Bos taurus (cattle)IC50300.000011
Deoxyribonuclease-2-alphaSus scrofa (pig)IC50300.000011
Dipeptidyl peptidase 3Homo sapiens (human)IC5085.000011
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)IC500.450011
DNA ligaseTequatrovirus T4IC50300.000011
DNA polymerase etaHomo sapiens (human)IC500.062011
DNA polymerase iotaHomo sapiens (human)IC500.062011
DNA polymerase kappaHomo sapiens (human)IC504.500022
DNA primaseMycobacterium tuberculosis CDC1551IC50100.000011
DNA topoisomerase Bos taurus (cattle)IC5017.000011
DNA topoisomerase 1Chlorocebus aethiops (grivet)IC5027.000011
DNA topoisomerase 1Homo sapiens (human)IC5023.26782433
DNA topoisomerase 1Mus musculus (house mouse)IC5019.000024
DNA topoisomerase 2-alphaHomo sapiens (human)IC50161.868356
DNA topoisomerase 2-betaHomo sapiens (human)IC500.605022
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)IC505.000022
DNA-3-methyladenine glycosylaseHomo sapiens (human)IC502.600011
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)IC505.000011
Ephrin type-B receptor 4Homo sapiens (human)IC501.830011
Epidermal growth factor receptorHomo sapiens (human)IC500.690011
estrogen receptor beta isoform 1Homo sapiens (human)IC502.927212
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 1Homo sapiens (human)IC50363.078011
Focal adhesion kinase 1Homo sapiens (human)IC503.110011
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC50101.23801010
G-protein coupled receptor 35Homo sapiens (human)IC500.850012
G1/S-specific cyclin-D1Homo sapiens (human)IC501.090011
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
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 synthase kinase-3 betaHomo sapiens (human)IC507.500011
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
Hepatocyte growth factor receptorHomo sapiens (human)IC500.580011
Histone deacetylase 1Homo sapiens (human)IC500.050011
Histone deacetylase 11 Homo sapiens (human)IC500.050011
Histone deacetylase 2Homo sapiens (human)IC500.050011
Histone deacetylase 3Homo sapiens (human)IC500.050011
Histone deacetylase 4Homo sapiens (human)IC500.050011
Histone deacetylase 5Homo sapiens (human)IC500.050011
Histone deacetylase 6Homo sapiens (human)IC500.050011
Histone deacetylase 7Homo sapiens (human)IC500.050011
Histone deacetylase 8Homo sapiens (human)IC500.050011
Histone deacetylase 9Homo sapiens (human)IC500.050011
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC501.600011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC500.600011
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC506.020011
Hypoxia-inducible factor 1-alphaHomo sapiens (human)IC501.530022
Inhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)IC501.980011
Insulin receptorHomo sapiens (human)IC500.340011
Insulin-like growth factor 1 receptorHomo sapiens (human)IC500.250011
Integrase Human immunodeficiency virus 1IC5043.680055
Interstitial collagenaseHomo sapiens (human)IC505.455022
Islet amyloid polypeptideHomo sapiens (human)IC507.800011
Kappa-type opioid receptorHomo sapiens (human)IC506.103011
Kappa-type opioid receptorHomo sapiens (human)Ki2.441011
Lactoylglutathione lyaseHomo sapiens (human)Ki30.199511
large T antigenBetapolyomavirus macacaeIC5010.730011
likely tRNA 2'-phosphotransferaseCandida albicans SC5314IC500.291322
Low molecular weight phosphotyrosine protein phosphataseBos taurus (cattle)IC5010.000011
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
M17 leucyl aminopeptidasePlasmodium falciparum 3D7IC50138.080011
Macrophage migration inhibitory factorHomo sapiens (human)IC504.770011
Macrophage migration inhibitory factorHomo sapiens (human)Ki1.950011
Mcl-1Homo sapiens (human)IC5019.186123
microphthalmia-associated transcription factor isoform 9Homo sapiens (human)IC506.381033
Mitogen-activated protein kinase 10Homo sapiens (human)IC5019.100012
Mitogen-activated protein kinase 14Homo sapiens (human)IC5019.100012
Mitogen-activated protein kinase 3 Homo sapiens (human)IC501.510011
Mitogen-activated protein kinase kinase kinase 8Homo sapiens (human)IC502.370011
Monoglyceride lipaseHomo sapiens (human)IC500.809522
mothers against decapentaplegic homolog 3 isoform 1Homo sapiens (human)IC500.142011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC500.500011
Mu-type opioid receptorHomo sapiens (human)IC503.511011
Mu-type opioid receptorHomo sapiens (human)Ki1.425011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC503.900034
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5031.700023
Multidrug resistance-associated protein 4Homo sapiens (human)IC5048.500013
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 M4Homo sapiens (human)IC501.556011
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.570013
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.217011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.570013
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC503.000011
NUAK family SNF1-like kinase 1Homo sapiens (human)IC500.510011
NucleophosminHomo sapiens (human)IC5040.000011
Pancreatic triacylglycerol lipaseSus scrofa (pig)IC50100.000011
perilipin-1Homo sapiens (human)IC506.959011
perilipin-5Homo sapiens (human)IC501.622011
Phosphatidylcholine 2-acylhydrolase Apis mellifera (honey bee)IC500.040011
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
Polyamine deacetylase HDAC10Homo sapiens (human)IC500.050011
Polypeptide N-acetylgalactosaminyltransferase 2Homo sapiens (human)IC501.720022
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC5016.066011
Procathepsin LHomo sapiens (human)IC509.350011
Protein E6Human papillomavirus 16IC504.000011
Protein-lysine 6-oxidaseHomo sapiens (human)IC500.320011
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)IC5040.000011
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC500.466733
putative polyproteinIC5030.573733
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)IC503.340011
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 SHomo sapiens (human)IC504.300011
ReninHomo sapiens (human)IC500.980011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC509.350011
Replicase polyprotein 1abBetacoronavirus England 1IC5018.075022
Replicase polyprotein 1abHuman coronavirus 229EIC509.350011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.917199
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
Ribonuclease pancreaticBos taurus (cattle)IC50300.000011
Serine/threonine-protein kinase B-rafHomo sapiens (human)IC501.760011
Serine/threonine-protein kinase pim-1Homo sapiens (human)IC502.700011
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC507.970022
Serine/threonine-protein kinase PLK4Homo sapiens (human)IC502.970011
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
Solute carrier family 22 member 1 Homo sapiens (human)IC5020.800011
Solute carrier family 22 member 12Homo sapiens (human)IC502.000011
Solute carrier family 22 member 12Rattus norvegicus (Norway rat)IC5018.000011
Solute carrier family 22 member 12Homo sapiens (human)Ki5.740011
Solute carrier family 22 member 2Homo sapiens (human)IC5031.850012
Solute carrier family 22 member 3Homo sapiens (human)IC5074.600011
Solute carrier family 22 member 6Homo sapiens (human)IC500.270011
Somatostatin receptor type 1Homo sapiens (human)IC500.002211
Somatostatin receptor type 2Homo sapiens (human)IC500.002211
Somatostatin receptor type 3Homo sapiens (human)IC500.002211
Somatostatin receptor type 4Homo sapiens (human)IC500.002211
Somatostatin receptor type 5Homo sapiens (human)IC500.002211
Sortase AStreptococcus mutansIC5027.200011
Spike glycoproteinBetacoronavirus England 1IC509.350011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC509.350011
Squalene monooxygenase Rattus norvegicus (Norway rat)IC502.000011
TatHuman immunodeficiency virus 1IC501.669011
Telomerase reverse transcriptaseHomo sapiens (human)IC50300.000011
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)IC50176.800022
Thioredoxin reductase 2, mitochondrialHomo sapiens (human)IC50176.800022
Thioredoxin reductase 3Homo sapiens (human)IC50176.800022
Thiosulfate sulfurtransferaseHomo sapiens (human)IC5057.000011
Translin-associated protein XHomo sapiens (human)IC503.500011
Transmembrane protease serine 2Homo sapiens (human)IC509.350011
Triosephosphate isomeraseHomo sapiens (human)IC501,000.000011
Triosephosphate isomerase, glycosomalTrypanosoma cruziIC506.500011
type-1 angiotensin II receptorHomo sapiens (human)IC506.637011
Type-2 restriction enzyme BamHIBacillus amyloliquefaciensIC50300.000011
Type-2 restriction enzyme EcoRIEscherichia coliIC50300.000011
Type-2 restriction enzyme HindIIIHaemophilus influenzae Rd KW20IC50300.000011
Type-2 restriction enzyme PstIProvidencia stuartiiIC50300.000011
Type-2 restriction enzyme ScaIStreptomyces caespitosusIC50300.000011
Tyrosine-protein kinase FgrRattus norvegicus (Norway rat)IC503.500011
Tyrosine-protein kinase Lyn Rattus norvegicus (Norway rat)IC507.500011
Tyrosine-protein kinase SYKHomo sapiens (human)IC5028.000011
Tyrosine-protein kinase YesHomo sapiens (human)Ki7.900011
Tyrosyl-DNA phosphodiesterase 1Homo sapiens (human)IC50111.000011
tyrosyl-DNA phosphodiesterase 2Homo sapiens (human)IC50119.666022
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50360.000011
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/oxidaseHomo sapiens (human)IC5010.100011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Amine oxidase [flavin-containing] AHomo sapiens (human)EC501.600011
DNA topoisomerase 1Homo sapiens (human)EC500.173135
DNA topoisomerase 1Homo sapiens (human)Kd0.026511
DNA topoisomerase type IB small subunit Leishmania majorEC500.670011
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)Kd0.089011
Endothelial PAS domain-containing protein 1Homo sapiens (human)EC500.071311
eukaryotic translation initiation factor 2-alpha kinase 3 isoform 1 precursorHomo sapiens (human)EC5055.700022
G-protein coupled receptor 35Homo sapiens (human)EC503.900024
Heterogeneous nuclear ribonucleoprotein A1Homo sapiens (human)Kd0.082711
Hypoxia-inducible factor 1-alphaHomo sapiens (human)EC500.071311
LacZ protein (plasmid)Escherichia coliEC5040.000011
NPYLR7BAedes aegypti (yellow fever mosquito)EC500.769012
Polypeptide N-acetylgalactosaminyltransferase 2Homo sapiens (human)Kd0.371011
Serine/threonine-protein kinase Chk1Homo sapiens (human)EC500.002111
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC503.000011
Triosephosphate isomerase, glycosomalTrypanosoma cruziKd10.400011
Tubulin alpha-1A chainHomo sapiens (human)Kd149.763012
Tubulin alpha-1B chainHomo sapiens (human)Kd149.763012
Tubulin alpha-1C chainHomo sapiens (human)Kd149.763012
Tubulin alpha-3C chainHomo sapiens (human)Kd149.763012
Tubulin alpha-3E chainHomo sapiens (human)Kd149.763012
Tubulin alpha-4A chainHomo sapiens (human)Kd149.763012
Tubulin beta chainHomo sapiens (human)Kd149.763012
Tubulin beta-1 chainHomo sapiens (human)Kd149.763012
Tubulin beta-2A chainHomo sapiens (human)Kd149.763012
Tubulin beta-2B chainHomo sapiens (human)Kd149.763012
Tubulin beta-3 chainHomo sapiens (human)Kd149.763012
Tubulin beta-4A chainHomo sapiens (human)Kd149.763012
Tubulin beta-4B chainHomo sapiens (human)Kd149.763012
Tubulin beta-6 chainHomo sapiens (human)Kd149.763012
Tubulin beta-8 chainHomo sapiens (human)Kd149.763012
Tyrosine-protein kinase SYKHomo sapiens (human)EC50300.000011
Wee1-like protein kinaseHomo sapiens (human)Kd0.001411

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseElectrophorus electricus (electric eel)EC24250.000011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)Km4.000011
CholinesteraseEquus caballus (horse)EC16250.000011
DNA topoisomerase 1Homo sapiens (human)CC5021.124025
DNA topoisomerase 1Homo sapiens (human)IC100.000211
DNA topoisomerase 1Homo sapiens (human)Inhibition100.000011
DNA topoisomerase 1Homo sapiens (human)MIC0.010011
DNA topoisomerase 1Mus musculus (house mouse)MIC0.086011
DNA topoisomerase 2-betaHomo sapiens (human)MIC100.000011
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
interferon gamma precursorHomo sapiens (human)AC5022.855022
LactoperoxidaseBos taurus (cattle)Km0.300011
Liver carboxylesterase 1Homo sapiens (human)Km1,453.000011
ProthrombinHomo sapiens (human)MIC100.000011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)Km97.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km24.500022
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km147.000011
UDP-glucuronosyltransferase 1A7Homo sapiens (human)Km5.000011
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km13.000011
UDP-glucuronosyltransferase 2B15Homo sapiens (human)Km186.000011