Page last updated: 2024-08-05 15:19:21

EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor

An EC 3.4.22.* (cysteine endopeptidase) inhibitor that interferes with the action of SARS coronavirus main proteinase (EC 3.4.22.69).

ChEBI ID: 147285

Members (16)

MemberDefinitionClass
(-)-gallocatechin gallateA gallate ester obtained by formal condensation of the carboxy group of gallic acid with the (3R)-hydroxy group of (-)-gallocatechin. A natural product found in found in green tea.(-)-gallocatechin gallate
3-fluoro-Nalpha-(1H-indol-2-ylcarbonyl)-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-phenylalaninamideA secondary carboxamide resulting from the formal condensation of the carboxy group of 1H-indole-2-carboxylic acid with the primary amino group of 3-fluoro-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-phenylalaninamide. It is an inhibitor of SARS coronavirus main proteinase and inhibits SARS-CoV-2 replication in cell culture (EC50 = 0.72 muM).3-fluoro-Nalpha-(1H-indol-2-ylcarbonyl)-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-phenylalaninamide
anacardic acidA hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities.anacardic acid
baicaleinA trihydroxyflavone with the hydroxy groups at positions C-5, -6 and -7.baicalein
cinanserinAn aryl sulfide that is (2E)-3-phenyl-N-(2-sulfanylphenyl)prop-2-enamide in which the hydrogen of the thiol group is substituted by a 3-(dimethylamino)propyl group. It is a 5-hydroxytryptamine receptor antagonist and an inhibitor of SARS-CoV replication.cinanserin
ebselenA benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.ebselen
herbacetinA pentahydroxyflavone that is kaempferol substituted by a hydroxy group at position 8. It is a natural flavonoid from flaxseed which exerts antioxidant, anti-inflammatory and anticancer activities.herbacetin
N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamideA secondary carboxamide resulting from the formal condensation of the carboxy group of 1H-indole-2-carboxylic acid with the primary amino group of 3-cyclohexyl-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-alaninamide. It is an inhibitor of SARS coronavirus main proteinase and inhibits SARS-CoV-2 replication in cell culture (EC50 = 0.53 muM).N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamide
N-[(5-methyl-1,2-oxazol-3-yl)carbonyl]-L-alanyl-L-valyl-N-{(2S,3E)-5-(benzyloxy)-5-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]pent-3-en-2-yl}-L-leucinamideA tripeptide resulting from the formal condensation of the carboxy group of N-[(5-methyl-1,2-oxazol-3-yl)carbonyl]-L-alanyl-L-valine with the amino group of benzyl (2E,4S)-4-(L-leucylamino)-5-[(3S)-2-oxopyrrolidin-3-yl]pent-2-enoate. It is an inhibitor of the main protease of SARS-CoV-2.N-[(5-methyl-1,2-oxazol-3-yl)carbonyl]-L-alanyl-L-valyl-N-{(2S,3E)-5-(benzyloxy)-5-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]pent-3-en-2-yl}-L-leucinamide
narlaprevirAn azabicyclohexane that is (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane substituted by [(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]aminoacyl and N-({1-[(tert-butylsulfonyl)methyl]cyclohexyl}carbamoyl)-3-methyl-L-valyl groups at positions 2S and 3, respectively. It is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor (Ki = 6 nM) that is used for the treatment of chronic hepatitis C.narlaprevir
nirmatrelvirAn azabicyclohexane that is (1R,5S)-3-azabicyclo[3.1.0]hexane substituted by {(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl}aminoacyl, 3-methyl-N-(trifluoroacetyl)-L-valinamide, methyl and methyl groups at positions 2S, 3, 6 and 6, respectively. It is the first orally administered inhibitor of SARS-CoV-2 main protease developed by Pfizer and used in combination with ritonavir for the treatment of COVID-19.nirmatrelvir
pectolinarinA disaccharide derivative that consists of pectolinarigenin substituted by a 6-O-(6-deoxy-alpha-L-mannopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.pectolinarin
PF-00835231A primary alcohol resulting from the cleavage of the phosphate group of the prodrug PF-07304814. It is an inhibitor of SARS-CoV-1 and -2 main protease (3CLpro) and exhibits potent in vitro antiviral activity.PF-00835231
PF-07304814An indolecarboxamide resulting from the formal condensation of the carboxy group of 4-methoxy-1H-indole-2-carboxylic acid with the primary amino group of N-[(2S)-3-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]-4-(phosphonooxy)butan-2-yl]-L-leucinamide. It is the phosphate prodrug of PF-00835231, an anticoronaviral agent.PF-07304814
savininA lignan that is dihydrofuran-2(3H)-one (gamma-butyrolactone) substituted by a 1,3-benzodioxol-5-ylmethylidene group at position 3 and a 1,3-benzodioxol-5-ylmethyl group at position 4 (the 3E,4R-isomer). It exhibits antiviral activity against SARS-CoV-2.savinin
vitamin k 3A member of the class of 1,4-naphthoquinones that is 1,4-naphthoquinone which is substituted at position 2 by a methyl group. It is used as a nutritional supplement and for the treatment of hypoprothrombinemia.menadione

Research

Studies (3,984)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990309 (7.76)18.7374
1990's275 (6.90)18.2507
2000's1,162 (29.17)29.6817
2010's1,527 (38.33)24.3611
2020's711 (17.85)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials50 (1.18%)5.53%
Reviews203 (4.80%)6.00%
Case Studies25 (0.59%)4.05%
Observational11 (0.26%)0.25%
Other3,941 (93.17%)84.16%

Protein Targets (423)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency11.542017
15-lipoxygenase, partialHomo sapiens (human)Potency0.818813
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency7.568611
acetylcholinesteraseHomo sapiens (human)Potency0.776211
activating transcription factor 6Homo sapiens (human)Potency57.132422
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency6.559618
alpha-galactosidaseHomo sapiens (human)Potency32.464822
Alpha-synucleinHomo sapiens (human)Potency4.478013
Amyloid-beta precursor proteinHomo sapiens (human)Potency16.360111
AR proteinHomo sapiens (human)Potency27.8744712
aryl hydrocarbon receptorHomo sapiens (human)Potency18.713727
ATAD5 protein, partialHomo sapiens (human)Potency7.908133
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency5.519756
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency6.745611
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.121611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency13.313813
BRCA1Homo sapiens (human)Potency10.882012
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency5.706212
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency76.958811
caspase-3Homo sapiens (human)Potency76.958811
Cellular tumor antigen p53Homo sapiens (human)Potency35.736025
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.043926
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency4.754416
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency16.348213
Chain A, Beta-lactamaseEscherichia coli K-12Potency39.955823
Chain A, CruzipainTrypanosoma cruziPotency26.651422
Chain A, Ferritin light chainEquus caballus (horse)Potency12.589311
Chain A, HADH2 proteinHomo sapiens (human)Potency2.406828
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency32.573312
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency5.761727
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency13.1300311
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.057616
Chain B, HADH2 proteinHomo sapiens (human)Potency2.406828
chromobox protein homolog 1Homo sapiens (human)Potency13.815422
cytochrome P450 2C19 precursorHomo sapiens (human)Potency2.308614
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.100214
cytochrome P450 2C9, partialHomo sapiens (human)Potency38.901811
cytochrome P450 2D6Homo sapiens (human)Potency7.916912
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.641514
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency25.133428
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.096411
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency21.380213
D(1A) dopamine receptorHomo sapiens (human)Potency22.387211
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency3.470312
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency35.481311
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency22.387211
DNA polymerase betaHomo sapiens (human)Potency3.162311
DNA polymerase eta isoform 1Homo sapiens (human)Potency35.796323
DNA polymerase III, partialBacillus subtilisPotency4.744411
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency29.318426
DNA polymerase kappa isoform 1Homo sapiens (human)Potency6.345514
endonuclease IVEscherichia coliPotency7.943311
Endothelin receptor type BRattus norvegicus (Norway rat)Potency22.387211
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency22.387211
estrogen nuclear receptor alphaHomo sapiens (human)Potency33.2169921
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency21.171425
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency30.5202611
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.521617
EWS/FLI fusion proteinHomo sapiens (human)Potency25.700548
farnesoid X nuclear receptorHomo sapiens (human)Potency37.652424
flap endonuclease 1Homo sapiens (human)Potency53.032414
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency14.348412
Fumarate hydrataseHomo sapiens (human)Potency25.118911
GVesicular stomatitis virusPotency38.901811
GABA theta subunitRattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency25.133414
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency25.133414
gemininHomo sapiens (human)Potency17.0494413
GLI family zinc finger 3Homo sapiens (human)Potency20.332024
glp-1 receptor, partialHomo sapiens (human)Potency22.874112
GLS proteinHomo sapiens (human)Potency5.402523
glucocerebrosidaseHomo sapiens (human)Potency35.586914
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency48.966233
glucokinase regulatory proteinHomo sapiens (human)Potency14.125411
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency0.631011
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency20.372723
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency0.631011
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency0.631011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Potency5.798811
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Potency5.798811
glyceraldehyde-3-phosphate dehydrogenase isoform 1Homo sapiens (human)Potency10.000011
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.481311
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency12.589311
heat shock protein beta-1Homo sapiens (human)Potency32.371224
hemoglobin subunit betaHomo sapiens (human)Potency22.106022
hexokinase-4 isoform 1Homo sapiens (human)Potency14.125411
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.0752218
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency0.449614
histone deacetylase 9 isoform 3Homo sapiens (human)Potency12.826923
Histone H2A.xCricetulus griseus (Chinese hamster)Potency37.219824
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency44.668411
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency38.901811
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypothetical protein, conservedTrypanosoma bruceiPotency15.202846
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency25.496024
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency15.902726
IDH1Homo sapiens (human)Potency21.852812
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency38.901812
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency4.564012
Integrin alpha-IIbHomo sapiens (human)Potency13.033313
Integrin beta-3Homo sapiens (human)Potency13.033313
Interferon betaHomo sapiens (human)Potency24.744227
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency20.546224
lethal factor (plasmid)Bacillus anthracis str. A2012Potency5.354715
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency15.848911
LuciferasePhotinus pyralis (common eastern firefly)Potency17.121635
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency18.078935
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency56.234122
M-phase phosphoprotein 8Homo sapiens (human)Potency4.002712
Microtubule-associated protein tauHomo sapiens (human)Potency12.6434216
mitogen-activated protein kinase 1Homo sapiens (human)Potency13.815412
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency14.125411
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency56.234111
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency56.234111
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.000011
NFKB1 protein, partialHomo sapiens (human)Potency12.589322
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency2.115412
Nrf2Homo sapiens (human)Potency29.295322
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency14.782024
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency16.360111
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency34.748723
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency18.7986215
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency32.656136
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency10.000011
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency104.959913
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency14.125411
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency25.744512
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency33.807811
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.541523
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency21.824824
phosphopantetheinyl transferaseBacillus subtilisPotency12.524418
plasminogen precursorMus musculus (house mouse)Potency11.726213
polyproteinZika virusPotency25.118911
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency3.074113
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency3.025213
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency19.629213
PPM1D proteinHomo sapiens (human)Potency22.384614
pregnane X nuclear receptorHomo sapiens (human)Potency21.802023
progesterone receptorHomo sapiens (human)Potency61.130611
pyruvate kinaseLeishmania mexicana mexicanaPotency15.551355
pyruvate kinase PKM isoform aHomo sapiens (human)Potency8.695546
pyruvate kinase PKM isoform bHomo sapiens (human)Potency10.000022
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency28.370812
RAR-related orphan receptor gammaMus musculus (house mouse)Potency20.781424
regulator of G-protein signaling 4Homo sapiens (human)Potency15.913913
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency35.917037
retinoid X nuclear receptor alphaHomo sapiens (human)Potency20.816324
RGS12Homo sapiens (human)Potency12.589311
serine-protein kinase ATM isoform aHomo sapiens (human)Potency39.810711
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency20.405422
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency2.993511
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Potency5.798811
SMAD family member 2Homo sapiens (human)Potency37.556423
SMAD family member 3Homo sapiens (human)Potency37.556423
Smad3Homo sapiens (human)Potency27.662513
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)Potency5.798811
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency7.087112
TAR DNA-binding protein 43Homo sapiens (human)Potency10.505113
TDP1 proteinHomo sapiens (human)Potency15.4407225
thioredoxin glutathione reductaseSchistosoma mansoniPotency32.657013
thioredoxin reductaseRattus norvegicus (Norway rat)Potency14.771523
ThrombopoietinHomo sapiens (human)Potency3.162322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency20.114228
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency44.668422
thyroid stimulating hormone receptorHomo sapiens (human)Potency35.481434
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency31.622811
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency3.470312
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.726213
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.726213
USP1 protein, partialHomo sapiens (human)Potency31.906425
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency17.736024
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency16.844035
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency13.890617
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency30.243612
WRNHomo sapiens (human)Potency5.323311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC505.468524
1-deoxy-D-xylulose 5-phosphate reductoisomeraseEscherichia coli K-12IC502.200011
10 kDa chaperonin Escherichia coliIC505.750022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC5015.000011
3-oxoacyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC501.100011
4-aminobutyrate aminotransferase, mitochondrialHomo sapiens (human)IC5012,800.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki3.500011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki2.250022
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki3.500011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki3.500011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.002011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.019044
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.004033
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.002011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.004033
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.002011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.200011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.004033
5-hydroxytryptamine receptor 7Homo sapiens (human)IC50350.000011
6-phosphogluconate dehydrogenase, decarboxylatingHomo sapiens (human)IC501.450011
60 kDa chaperoninEscherichia coli K-12IC50250.000011
60 kDa chaperonin Escherichia coliIC505.750022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC5015.000011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC5028.005022
AcetylcholinesteraseHomo sapiens (human)IC5015.000011
Aldehyde oxidaseHomo sapiens (human)IC500.200011
Aldehyde oxidase 1Macaca fascicularis (crab-eating macaque)IC500.110011
Aldehyde oxidase 1Mus musculus (house mouse)IC500.150011
Aldehyde oxidase 1Oryctolagus cuniculus (rabbit)IC502.000011
Aldehyde oxidase 1Cavia porcellus (domestic guinea pig)Ki7.230011
Aldehyde oxidase 1 Rattus norvegicus (Norway rat)IC500.190011
Alpha-synucleinHomo sapiens (human)IC508.933323
Amine oxidase [flavin-containing] AHomo sapiens (human)IC506.610012
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki26.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki0.400011
Angiotensin-converting enzyme 2 Homo sapiens (human)IC506.440014
Arrestin, beta 1Homo sapiens (human)IC501.524011
ATP-dependent translocase ABCB1Homo sapiens (human)IC5041.000011
Aurora kinase BHomo sapiens (human)IC504.060011
Beta-hydroxyacyl-ACP dehydratase precursor (Fatty acid synthesis protein)Plasmodium falciparum (malaria parasite P. falciparum)IC500.600011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC500.757544
Bile salt export pumpHomo sapiens (human)IC5010.000011
Calpain-1 catalytic subunitHomo sapiens (human)IC500.291815
Casein kinase II subunit alphaHomo sapiens (human)IC5010.000011
Casein kinase II subunit alpha 3Homo sapiens (human)IC5010.000011
Casein kinase II subunit alpha'Homo sapiens (human)IC5010.000011
Casein kinase II subunit betaHomo sapiens (human)IC5010.000011
Caspase-1Homo sapiens (human)IC504.040011
Caspase-2Homo sapiens (human)IC5010.000011
Cathepsin BHomo sapiens (human)IC500.579937
Cathepsin DHomo sapiens (human)IC5010.000011
Cathepsin KHomo sapiens (human)IC500.291815
Chain A, RNA-directed RNA polymerase NS5Dengue virus 2 16681-PDK53IC5035.060011
CholinesteraseEquus caballus (horse)IC5010.474022
Cyclin-dependent kinase 1Homo sapiens (human)IC506.530011
Cytochrome P450 11B1, mitochondrialRattus norvegicus (Norway rat)IC5050.000011
Cytochrome P450 1A1Homo sapiens (human)Ki1.220011
Cytochrome P450 1B1Homo sapiens (human)Ki0.260011
Cytochrome P450 2C9 Homo sapiens (human)IC5018.850012
Cytochrome P450 3A4Homo sapiens (human)IC509.200011
Death-associated protein kinase 1Homo sapiens (human)IC50120.000011
Dipeptidyl peptidase 4Homo sapiens (human)IC50200.000011
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50200.000022
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50200.000011
Dual specificity protein phosphatase 1Mus musculus (house mouse)IC5024.000011
Dual specificity protein phosphatase 6Rattus norvegicus (Norway rat)IC5020.500011
Dual specificity tyrosine-phosphorylation-regulated kinase 1AHomo sapiens (human)IC500.121011
Enoyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC500.500011
eukaryotic translation initiation factor 4 gamma 1 isoform 4Homo sapiens (human)IC501.150011
eukaryotic translation initiation factor 4E isoform 1Mus musculus (house mouse)IC501.150011
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC5018.850012
G protein-coupled receptor kinase 6Homo sapiens (human)IC508.700011
G-protein coupled receptor 35Homo sapiens (human)IC5028.200011
G2/mitotic-specific cyclin-B1Homo sapiens (human)IC506.530011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki5.623411
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki5.623411
Gamma-butyrobetaine dioxygenaseHomo sapiens (human)IC500.742055
Genome polyprotein Zika virusIC5099.000011
Genome polyprotein Ki0.006011
Glucocorticoid receptorHomo sapiens (human)IC5019.000011
Glucose-6-phosphate 1-dehydrogenaseSaccharomyces cerevisiae S288CIC500.230011
glucose-6-phosphate 1-dehydrogenase isoform bHomo sapiens (human)IC5013.200011
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonasePlasmodium bergheiIC5015.086733
Glutathione reductase, mitochondrialHomo sapiens (human)Ki14.100022
Heat shock protein HSP 90-betaHomo sapiens (human)IC5034.000011
Hepatocyte growth factor receptorHomo sapiens (human)IC5010.000011
hexokinaseTrypanosoma brucei brucei TREU927IC500.900911
Histone acetyltransferase KAT2BHomo sapiens (human)IC5019.450044
Histone acetyltransferase KAT5Homo sapiens (human)IC5064.000011
Histone acetyltransferase KAT8Homo sapiens (human)IC5043.000011
Histone acetyltransferase KAT8Homo sapiens (human)Ki64.000011
Histone acetyltransferase p300Homo sapiens (human)IC507.412544
Histone deacetylase 5Homo sapiens (human)IC503.400011
Histone deacetylase 6Homo sapiens (human)IC506.533333
Histone deacetylase 9Homo sapiens (human)IC503.700011
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC500.730011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC500.400011
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC500.892544
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)Ki0.094033
Insulin-degrading enzymeHomo sapiens (human)IC5033.352033
Integrase Human immunodeficiency virus 1IC503.296055
Lactoylglutathione lyaseHomo sapiens (human)IC5011.000011
large T antigenBetapolyomavirus macacaeIC5013.910011
Linoleate 9S-lipoxygenase-4Glycine max (soybean)IC5022.000011
Lysine-specific demethylase 4EHomo sapiens (human)IC503.000011
Lysine-specific demethylase 4EHomo sapiens (human)Ki4.330011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC5012.500011
Lysosomal alpha-glucosidaseHomo sapiens (human)IC50500.000011
M-phase inducer phosphatase 1Homo sapiens (human)IC504.550022
M-phase inducer phosphatase 2Homo sapiens (human)IC503.160033
M-phase inducer phosphatase 3Homo sapiens (human)IC5018.900022
Macrophage migration inhibitory factorHomo sapiens (human)IC502.400011
Macrophage migration inhibitory factorHomo sapiens (human)Ki0.570022
Methionine aminopeptidase 2Homo sapiens (human)IC502.430011
MPI proteinHomo sapiens (human)IC500.290522
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC508.900011
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))Ki13.700011
neutrophil cytosol factor 1Homo sapiens (human)IC500.390011
Neutrophil cytosol factor 1Homo sapiens (human)Ki125.000033
Neutrophil elastaseHomo sapiens (human)IC5010.000011
Non-structural protein 4A Ki0.006011
perilipin-1Homo sapiens (human)IC505.652512
perilipin-5Homo sapiens (human)IC505.284512
phosphoethanolamine/phosphocholine phosphatase isoform 1Homo sapiens (human)IC500.111011
phosphomannomutase 2Homo sapiens (human)IC500.672011
Platelet glycoprotein VIHomo sapiens (human)IC5037.500022
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC5050.425012
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC5010.000022
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC5031.532025
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Ki1.600011
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC5033.180025
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)Ki0.600011
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)IC5051.092937
Polyunsaturated fatty acid lipoxygenase ALOX15BRattus norvegicus (Norway rat)IC500.260011
Probable linoleate 9S-lipoxygenase 5Solanum tuberosum (potato)IC5043.000011
Procathepsin LHomo sapiens (human)IC502.7365310
Progesterone receptorHomo sapiens (human)IC5015.000011
Prolyl endopeptidaseHomo sapiens (human)IC5036.000011
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50150.000011
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC502.100011
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC5050.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC50150.000011
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC5050.000011
Protease Human immunodeficiency virus 1IC5010.000011
Proteasome subunit beta type-5Homo sapiens (human)IC500.187011
Protein kinase C alpha typeHomo sapiens (human)IC502.200011
Protein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)IC502.200011
ProthrombinHomo sapiens (human)IC5010.000011
Pyruvate kinase PKMHomo sapiens (human)IC50150.000011
Receptor protein-tyrosine kinase Homo sapiens (human)IC502.200011
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC5010.000011
Receptor-type tyrosine-protein phosphatase etaHomo sapiens (human)IC502.200011
Receptor-type tyrosine-protein phosphatase SHomo sapiens (human)IC5010.300011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC506.440014
Replicase polyprotein 1abBetacoronavirus England 1IC506.845538
Replicase polyprotein 1abHuman coronavirus 229EIC505.181025
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC507.04454378
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC502.5060520
Replicase polyprotein 1abAvian infectious bronchitis virus (strain Beaudette CK)Ki0.0009112
Replicase polyprotein 1abFeline infectious peritonitis virus (strain 79-1146)Ki0.0009112
Replicase polyprotein 1abHuman coronavirus 229EKi0.0009112
Replicase polyprotein 1abHuman coronavirus HKU1 (isolate N5)Ki0.0009112
Replicase polyprotein 1abHuman coronavirus NL63Ki0.0009112
Replicase polyprotein 1abHuman coronavirus OC43Ki0.0009112
Replicase polyprotein 1abMurine hepatitis virus strain A59Ki0.0009112
Replicase polyprotein 1abPipistrellus bat coronavirus HKU5Ki0.0009112
Replicase polyprotein 1abPorcine epidemic diarrhea virus CV777Ki0.0009112
Replicase polyprotein 1abRousettus bat coronavirus HKU9Ki0.0009112
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki0.9503921
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi5.450012
Replicase polyprotein 1abTylonycteris bat coronavirus HKU4Ki0.0009112
RNA polymerase beta subunit (EC 2.7.7.6), partialEscherichia coliIC5011.687211
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC5037.250022
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC509.000011
Serine/threonine-protein kinase PLK2Homo sapiens (human)IC50314.000011
Serine/threonine-protein kinase PLK3Homo sapiens (human)IC5040.000011
SialidaseClostridium perfringensIC501.400011
Sialidase-2Homo sapiens (human)IC50130.000011
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC5010.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.182011
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC5050.000011
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC5050.000011
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC5050.000011
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC5050.000011
Spike glycoproteinBetacoronavirus England 1IC506.440014
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC506.440014
Structural capsid protein Human immunodeficiency virus 1IC500.046711
Sucrase-isomaltase, intestinalHomo sapiens (human)IC5043.500022
Sucrase-isomaltase, intestinalRattus norvegicus (Norway rat)IC50156.000022
Sulfhydryl oxidase 1Homo sapiens (human)IC505.400011
SUMO-activating enzyme subunit 1Homo sapiens (human)IC502.200011
Testosterone 17-beta-dehydrogenase 3Homo sapiens (human)IC5097.610022
Thiosulfate sulfurtransferaseHomo sapiens (human)IC501.000011
Toxin BClostridioides difficileIC500.017211
TPA: protein transporter TIM10Saccharomyces cerevisiae S288CIC505.290022
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC500.880011
Transmembrane protease serine 2Homo sapiens (human)IC506.440014
Trypanothione reductaseTrypanosoma cruziIC5055.000022
Trypsin-1Homo sapiens (human)IC503.700011
Trypsin-2Homo sapiens (human)IC503.700011
Trypsin-3Homo sapiens (human)IC503.700011
Tyrosine-protein kinase JAK3Homo sapiens (human)IC502.200011
Tyrosine-protein kinase YesHomo sapiens (human)IC503.300011
Ubiquitin carboxyl-terminal hydrolase isozyme L1Homo sapiens (human)IC50290.000011
Ubiquitin carboxyl-terminal hydrolase isozyme L1Mus musculus (house mouse)IC50180.500012
Ubiquitin carboxyl-terminal hydrolase isozyme L3Homo sapiens (human)IC5071.000022
Ubiquitin carboxyl-terminal hydrolase isozyme L3Mus musculus (house mouse)IC50180.500012
UDP-glucose 4-epimeraseHomo sapiens (human)IC500.014011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC505.700022
Urease subunit alphaHelicobacter pylori 26695IC5082.578055
Urease subunit alphaHelicobacter pylori 26695Ki0.226011
Urease subunit betaHelicobacter pylori 26695IC5082.578055
Urease subunit betaHelicobacter pylori 26695Ki0.226011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC5037.400022
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC502.790011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiotensin-converting enzyme 2 Homo sapiens (human)EC501.806713
G-protein coupled receptor 35Homo sapiens (human)EC5016.500022
Gamma-butyrobetaine dioxygenaseHomo sapiens (human)Kd4.100022
hexokinase HKDC1Homo sapiens (human)EC5038.800011
hexokinase-1 isoform HKIHomo sapiens (human)EC5041.900011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC503.500011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC5017.000011
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC50100.000011
Procathepsin LHomo sapiens (human)EC501.806713
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC501.806713
Replicase polyprotein 1abBetacoronavirus England 1EC501.806713
Replicase polyprotein 1abHuman coronavirus 229EEC501.806713
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC503.1823713
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC502.040027
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Kd18.400033
Spike glycoproteinBetacoronavirus England 1EC501.806713
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC501.806713
streptokinase A precursorStreptococcus pyogenes M1 GASEC501.519011
Transmembrane protease serine 2Homo sapiens (human)EC501.806713

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Androgen receptorHomo sapiens (human)EC15018.900011
Cyclic AMP-responsive element-binding protein 1Homo sapiens (human)AC5013.500011
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)Km72.000011
dual specificity tyrosine-phosphorylation-regulated kinase 1ARattus norvegicus (Norway rat)AC507.385512
Glucocorticoid receptorHomo sapiens (human)EC15018.900011
Glutathione reductasePlasmodium falciparum 3D7Km82.200011
Glutathione reductase, mitochondrialHomo sapiens (human)Km31.200011
H3 histone acetyltransferaseCandida albicans SC5314AC501.550011
Histone acetyltransferase KAT8Homo sapiens (human)K0.5205.000033
Histone acetyltransferase KAT8Homo sapiens (human)Km1.766733
Histone acetyltransferase p300Homo sapiens (human)INH8.500011
hypothetical protein CAALFM_CR05890CACandida albicans SC5314AC501.550011
NADHomo sapiens (human)Km1.300033
NADHomo sapiens (human)Vmax7,286.000011
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)Emax68.000011
Plasma kallikreinHomo sapiens (human)K0.5514.000011
Platelet-activating factor acetylhydrolaseHomo sapiens (human)Km72.000015
Trypanothione reductaseTrypanosoma cruziKm21.000011
Trypanothione reductaseTrypanosoma cruzix fold375.000011