Page last updated: 2024-08-05 14:55:15

EC 3.1.1.7 (acetylcholinesterase) inhibitor

An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid.

ChEBI ID: 38462

Members (101)

MemberDefinitionClass
11-hydroxysugiolAn abietane diterpenoid that is sugiol in which the hydrogen ortho to the phenolic hydroxy group has been replaced by a hydroxy group.11-hydroxysugiol
acephateA phosphoramide that is methamidophos in which one of the hydrogens is replaced by an acetyl group.acephate
aminocarbA carbamate ester that is phenyl methylcarbamate substituted by a dimethylamino group at position 4 and a methyl group at position 3.aminocarb
ar-turmeroneA sesquiterpenoid that is 2-methylhept-2-en-4-one substituted by a 4-methylphenyl group at position 6. It has been isolated from Peltophorum dasyrachis.(+)-(S)-ar-turmerone
arisugacinAn organic heterotetracyclic compound that is 4a,12a-dihydroxy-4,4,6a,12b-tetramethyl-4a,6,6a,12,12a,12b-hexahydro-4H,11H-benzo[f]pyrano[4,3-b]chromene-1,11(5H)-dione substituted by 3,4-dimethoxyphenyl group at position 9 (the 4aR,6aR,12aS,12bS steroisomer). Isolated from the culture broth of Penicillium, it acts as a selective inhibitor of acetylcholinesterase.arisugacin A
azamethiphosazamethiphos
azinphos ethylazinphos-ethyl
azinphosmethylA member of the class of benzotriazines that is 1,2,3-benzotriazine substituted by an oxo group at position 4 and a [(dimethoxyphosphorothioyl)sulfanyl]methyl group at position 3.azinphos-methyl
bambuterolA carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.bambuterol
bambuterol hydrochlorideThe hydrochloride salt of bambuterol. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.bambuterol hydrochloride
bay 93820isocarbophos
bellidifolinA member of the xanthone family that is bellidin substituted with a methyl group at O-3. A natural product found particularly in Swertia chirata and Gentianella campestris.bellidifolin
bendiocarbbendiocarb
benfuracarbbenfuracarb
berberineberberine
bis(7)-tacrineA secondary amino compound consisting of two molecules of tacrine that are linked together through their exocyclic amino groups by a heptane-1,7-diyl chain. Bis(7)-tacrine is an acetylcholinesterase (AChE)inhibitor (IC50 0.40 nM, >1,000 times more potent than tacrine). It has also been found to protect against H2O2 -induced apoptosis in rat pheochromocytoma cells.bis(7)-tacrine
bpmcA carbamate ester obtained by the formal condensation of 2-sec-butylphenol with methylcarbamic acid.fenobucarb
cadusafoscadusafos
carbarylA carbamate ester obtained by the formal condensation of 1-naphthol with methylcarbamic acid.carbaryl
carbofurancarbofuran
chlorfenvinphoschlorfenvinfos
chlorpyrifosAn organic thiophosphate that is O,O-diethyl hydrogen phosphorothioate in which the hydrogen of the hydroxy group has been replaced by a 3,5,6-trichloropyridin-2-yl group.chlorpyrifos
chlorpyrifos-methylAn organic thiophosphate that is O,O-dimethyl hydrogen phosphorothioate in which the hydrogen of the hydroxy group has been replaced by a 3,5,6-trichloropyridin-2-yl group.chlorpyrifos-methyl
corynolineA benzophenanthridine alkaloid that is chelidonine substituted by a methyl group at position 13. Isolated from the aerial parts of Corydalis incisa, it acts as an acetylcholinesterase inhibitor and also exhibits antineoplastic and hepatoprotective activity.corynoline
cronetonethiofencarb
cyanophoscyanophos
cyclanolineA charged berberine alkaloid obtained by N-methylation of (S)-scoulerine.cyclanoline
decursinolAn organic heterotricyclic compound that is 7,8-dihydro-2H,6H-pyrano[3,2-g]chromen-2-one substituted by a beta-hydroxy group at position 7 and two methyl groups at position 8. It is isolated from the roots of Angelica gigas and has been found to possess significant inhibitory activity against acetylcholinesterase enzyme (EC 3.1.1.7).decursinol
deltanitfurathiocarb
demethylbellidifolinA member of the class of xanthones that is xanthone which is substituted by hydroxy groups at positions 1, 3, 5, and 8. A natural product found particularly in Iris nigricans and Gentiana campestris.bellidin
demeton-s-methyldemeton-S-methyl
diazinonA member of the class of pyrimidines that is pyrimidine carrying an isopropyl group at position 2, a methyl group at position 6 and a (diethoxyphosphorothioyl)oxy group at position 4.diazinon
dibutylaminosulfenylcarbofurancarbosulfan
dichlorvosAn alkenyl phosphate that is the 2,2-dichloroethenyl ester of dimethyl phosphate.dichlorvos
dicrotophosdicrotophos
dimethoateA monocarboxylic acid amide that is N-methylacetamide in which one of the hydrogens of the methyl group attached to the carbonyl moiety is replaced by a (dimethoxyphosphorothioyl)sulfanediyl group.dimethoate
dimethoxonomethoate
disulfotonAn organic thiophosphate that is the diethyl ester of S-[2-(ethylsulfanyl)ethyl] dihydrogen phosphorodithioate.disulfoton
donepezilA racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one; donepezil
edifenphosAn organic thiophosphate that is the O-ethyl-S,S-diphenyl ester of phosphorodithioic acid. Used to control a variety of fungal diseases on rice including blast, ear blight and stem rot. Edifenphos is moderately toxic to mammals and fish but poses more of a risk to aquatic invertebrates.edifenphos
erucyl amideA primary fatty amide resulting from the formal condensation of the carboxy group of erucic acid with ammonia. It is commonly used as a slip additive in the plastic manufacturing industry.erucamide
ethionAn organic thiophosphate that is S,S'-methanediyl bis[dihydrogen (phosphorodithioate)] in which all the hydroxy groups have been converted to their corresponding ethyl esters respectively. Ethion is an organophosphate insecticide with inhibitory activity towards the enzyme acetylcholinesterase ( EC 3.1.1.7).ethion
ethoprophosethoprophos
famophosfamphur
fenamiphosfenamiphos
fenitrothionAn organic thiophosphate that is O,O-dimethyl O-phenyl phosphorothioate substituted by a methyl group at position 3 and a nitro group at position 4.fenitrothion
fensulfothionfensulfothion
fenthionAn organic thiophosphate that is O,O-dimethyl hydrogen phosphorothioate in which the hydrogen atom of the hydroxy group is replaced by a 3-methyl-4-(methylsulfanyl)phenyl group. It exhibits acaricidal and insecticidal activities.fenthion
fonofosfonofos
formetanateformetanate
fosthiazatefosthiazate
galantamineA benzazepine alkaloid isolated from certain species of daffodils.galanthamine
geissospermineA indole alkaloid comprising two indole-derived polycyclic moieties joined by a cyclic ether linkage.geissospermine
heptenophosheptenophos
huperzine aA sesquiterpene alkaloid isolated from a club moss Huperzia serrata that has been shown to exhibit neuroprotective activity. It is also an effective inhibitor of acetylcholinesterase and has attracted interest as a therapeutic candidate for Alzheimer's disease.huperzine A
hypochlorous acidA chlorine oxoacid with formula HOCl; a weak, unstable acid, it is the active form of chlorine in water.hypochlorous acid
imperatorinA member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 8. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.imperatorin
isofenphosisofenphos
isoimperatorinA member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 5. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.isoimperatorin
isoprocarbisoprocarb
liriodenineAn oxoaporphine alkaloid that is 4,5,6,6a-tetradehydronoraporphin-7-one substituted by a methylenedioxy group across positions 1 and 2. It is isolated from Annona glabra and has been shown to exhibit antimicrobial and cytotoxic activities.liriodenine
loganinAn iridoid monoterpenoid with formula C17H26O10 that is isolated from several plant species and exhibits neuroprotective and anti-inflammatory properties.loganin
lycojapodine aAn alkaloid isolated from the club moss Lycopodium japonicum and has been shown to exhibit acetylcholinesterase inhibitory and anti-HIV-1 activity.lycojapodine A
mecarbamAn organic thiophosphate that is O,O-diethyl hydrogen phosphorodithioate in which the hydrogen attached to a sulfur is replaced by a 2-[(ethoxycarbonyl)(methyl)amino]-2-oxoethyl group.mecarbam
methidathionmethidathion
methiocarbA carbamate ester obtained by the formal condensation of the phenolic group of 3,5-dimethyl-4-(methylsulfanyl)phenol with the carboxy group of methylcarbamic acid.methiocarb
methomylA carbamate ester obtained by the formal condensation of methylcarbamic acid with the hydroxy group of 1-(methylsulfanyl)acetaldoxime.methomyl
methyl parathionA C-nitro compound that is 4-nitrophenol substituted by a (dimethoxyphosphorothioyl)oxy group at position 4.parathion-methyl
metolcarbmetolcarb
monocrotophosAn alkenyl phosphate that is the 4-(methylamino)-4-oxobut-2-en-2-yl ester of dimethyl phosphate.monocrotophos
naledAn dialkyl phosphate resulting from the formal condensation of the acidic hydroxy group of dimethyl hydrogen phosphate with the alcoholic hydroxy group of 1,2-dibromo-2,2-dichloroethanol. An organophosphate insecticide, it is no longer approved for use within the European Union.naled
neostigmineA quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor.neostigmine
norswertianolinA beta-D-glucoside that is bellidin in which a beta-D-glucopyranosyl residue is attached at position O-8. A natural product found particularly in Gentiana campestris and Gentiana germanica.norswertianolin
paraoxonAn aryl dialkyl phosphate where both the alkyl groups are ethyl and the aryl group is 4-nitrophenyl.paraoxon
parathionparathion
phenthoate, (+-)-isomerAn organic thiophosphate that is ethyl mandelate in which the hydroxy group has been replaced by a (dimethoxyphosphorothioyl)sulfanediyl group.phenthoate
phenylphosphonothioic acid, 2-ethyl 2-(4-nitrophenyl) esterEPN
phoratephorate
phosaloneA member of the class of 1,3-benzoxazoles carrying a [(diethoxyphosphorothioyl)sulfanyl]methyl group at the nitrogen atom, an oxo group at position 2 and a chloro group at position 6. It is an organothiophosphate insecticide.phosalone
phosmetphosmet
pirimicarbAn aminopyrimidine that is N,N,4,5-tetramethylpyrimidin-2-amine substituted by a (dimethylcarbamoyl)oxy group at position 4.pirimicarb
pirimiphos methylAn organic thiophosphate that is O,O-dimethyl O-pyrimidin-4-yl phosphorothioate substituted by a methyl group at position 6 and a diethylamino group at position 2.pirimiphos-methyl
profenofosprofenofos
propetamphospropetamphos
propoxurA carbamate ester that is phenyl methylcarbamate substituted at position 2 by a propan-2-yloxy group.propoxur
prothiophosAn organic thiophosphate that is the 2,4-dichlorophenyl ester of O-ethyl S-propyl dithiophosphoric acid.prothiofos
pyraclofospyraclofos
pyridafenthionpyridaphenthion
quinalphosquinalphos
sulfoteppsulfotep
sulprofossulprofos
tacrineA member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.tacrine
temefosAn organic sulfide that is diphenyl sulfide in which the hydrogen at the para position of each of the phenyl groups has been replaced by a (dimethoxyphosphorothioyl)oxy group.temephos
terbufosterbufos
terbutalineA member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.terbutaline
tetrachlorvinphostetrachlorvinphos
thiometonthiometon
triazophostriazophos
trichlorfonA phosphonic ester that is dimethyl phosphonate in which the hydrogen atom attched to the phosphorous is substituted by a 2,2,2-trichloro-1-hydroxyethyl group.trichlorfon
vxA organic thiophosphate that is the ethyl ester of S-{2-[di(propan-2-yl)amino]ethyl} O hydrogen methylphosphonothioate. A toxic nerve agent used in chemical warfare.VX nerve agent
xyloketal aA xyloketal with formula C27H36O6. It was initially isolated from the mangrove fungus Xylaria sp. from the South China sea coast.xyloketal A

Research

Studies (39,975)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199010,650 (26.64)18.7374
1990's5,152 (12.89)18.2507
2000's8,043 (20.12)29.6817
2010's10,793 (27.00)24.3611
2020's5,337 (13.35)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,635 (5.56%)5.53%
Reviews2,281 (4.81%)6.00%
Case Studies1,543 (3.25%)4.05%
Observational95 (0.20%)0.25%
Other40,878 (86.18%)84.16%

Protein Targets (346)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency19.848215
15-lipoxygenase, partialHomo sapiens (human)Potency27.284615
67.9K proteinVaccinia virusPotency0.449622
acetylcholinesteraseHomo sapiens (human)Potency29.10274230
activating transcription factor 6Homo sapiens (human)Potency21.4212119
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency29.0548125
Alpha-synucleinHomo sapiens (human)Potency10.000011
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency22.387211
AR proteinHomo sapiens (human)Potency34.450812234
aryl hydrocarbon receptorHomo sapiens (human)Potency29.2654392
arylsulfatase AHomo sapiens (human)Potency13.871713
ATAD5 protein, partialHomo sapiens (human)Potency14.168623
Ataxin-2Homo sapiens (human)Potency26.886028
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency12.180057
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency34.956229
beta-2 adrenergic receptorHomo sapiens (human)Potency10.322511
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.118713
caspase-3Cricetulus griseus (Chinese hamster)Potency54.884213
Caspase-7Cricetulus griseus (Chinese hamster)Potency54.884213
Cellular tumor antigen p53Homo sapiens (human)Potency42.3487339
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency18.915623
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.665112
Chain A, Beta-lactamaseEscherichia coli K-12Potency23.474224
Chain A, Ferritin light chainEquus caballus (horse)Potency29.666715
Chain A, HADH2 proteinHomo sapiens (human)Potency28.1234213
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency55.535418
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency2.581016
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency14.497517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency46.144614
Chain B, HADH2 proteinHomo sapiens (human)Potency28.1234213
chromobox protein homolog 1Homo sapiens (human)Potency87.4351211
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.848911
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.980419
cytochrome P450 2D6Homo sapiens (human)Potency14.066017
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency17.067412
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency9.1692230
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency11.5215211
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency45.2793128
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency3.162311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency58.163014
DNA polymerase kappa isoform 1Homo sapiens (human)Potency24.745213
estrogen nuclear receptor alphaHomo sapiens (human)Potency38.361211203
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency42.4187230
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency39.16319161
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency21.6152110
EWS/FLI fusion proteinHomo sapiens (human)Potency12.321448
eyes absent homolog 2 isoform aHomo sapiens (human)Potency100.000011
farnesoid X nuclear receptorHomo sapiens (human)Potency30.7762541
flap endonuclease 1Homo sapiens (human)Potency25.118911
Fumarate hydrataseHomo sapiens (human)Potency44.703812
GVesicular stomatitis virusPotency6.980419
GABA theta subunitRattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency9.1692115
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency9.1692115
gemininHomo sapiens (human)Potency9.5001214
GLI family zinc finger 3Homo sapiens (human)Potency29.2461374
glp-1 receptor, partialHomo sapiens (human)Potency6.083733
GLS proteinHomo sapiens (human)Potency21.925614
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency31.6143434
glucokinase regulatory proteinHomo sapiens (human)Potency22.387211
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency51.2755117
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Potency31.622811
Glycoprotein hormones alpha chainHomo sapiens (human)Potency31.622811
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency3.078313
Guanine nucleotide-binding protein GHomo sapiens (human)Potency20.783424
heat shock protein beta-1Homo sapiens (human)Potency34.1929227
hexokinase-4 isoform 1Homo sapiens (human)Potency22.387211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency8.759116
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency34.075917
histone deacetylase 9 isoform 3Homo sapiens (human)Potency51.072623
Histone H2A.xCricetulus griseus (Chinese hamster)Potency82.2143230
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.980419
hypothetical protein, conservedTrypanosoma bruceiPotency24.961833
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency33.5929215
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency18.380833
importin subunit beta-1 isoform 1Homo sapiens (human)Potency24.590024
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.9804118
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency16.348223
Integrin alpha-IIbHomo sapiens (human)Potency15.813912
Integrin beta-3Homo sapiens (human)Potency15.813912
Interferon betaHomo sapiens (human)Potency9.8018313
interleukin 8Homo sapiens (human)Potency51.593413
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency32.983812
lamin isoform A-delta10Homo sapiens (human)Potency18.5079110
lethal factor (plasmid)Bacillus anthracis str. A2012Potency16.809012
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency51.2193227
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency30.616333
Microtubule-associated protein tauHomo sapiens (human)Potency24.419429
mitogen-activated protein kinase 1Homo sapiens (human)Potency18.541516
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency10.337424
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.316211
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency28.183811
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency28.183811
NFKB1 protein, partialHomo sapiens (human)Potency28.183822
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency19.952611
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency34.87594105
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency21.837012
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency7.765013
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency25.5059117
Nuclear receptor ROR-gammaHomo sapiens (human)Potency39.361815
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency22.6431211
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency27.96173174
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency54.937913
ParkinHomo sapiens (human)Potency39.810711
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency59.858524
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.466829
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency33.2443548
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency30.7260424
phosphopantetheinyl transferaseBacillus subtilisPotency35.3977114
PINK1Homo sapiens (human)Potency39.810711
plasminogen precursorMus musculus (house mouse)Potency11.220211
polyproteinZika virusPotency44.703812
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency39.810711
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency8.759113
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency30.434617
PPM1D proteinHomo sapiens (human)Potency10.435312
pregnane X nuclear receptorHomo sapiens (human)Potency42.1192286
pregnane X receptorRattus norvegicus (Norway rat)Potency42.0490111
progesterone receptorHomo sapiens (human)Potency26.7975241
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency23.466715
RAR-related orphan receptor gammaMus musculus (house mouse)Potency31.9612248
regulator of G-protein signaling 4Homo sapiens (human)Potency36.907516
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency43.8645382
retinoid X nuclear receptor alphaHomo sapiens (human)Potency26.9036483
serine-protein kinase ATM isoform aHomo sapiens (human)Potency39.810711
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency24.326917
SMAD family member 2Homo sapiens (human)Potency39.584828
SMAD family member 3Homo sapiens (human)Potency39.584828
Smad3Homo sapiens (human)Potency20.552312
snurportin-1Homo sapiens (human)Potency24.590024
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810712
survival motor neuron protein isoform dHomo sapiens (human)Potency21.280412
TAR DNA-binding protein 43Homo sapiens (human)Potency19.081713
TDP1 proteinHomo sapiens (human)Potency23.5829233
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.527036
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency53.8329365
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency16.8580719
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.9904688
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency44.668411
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.220211
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.220211
USP1 protein, partialHomo sapiens (human)Potency45.290128
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency36.5991245
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency31.0651527
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency42.9286127
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency51.2755117
VprHuman immunodeficiency virus 1Potency33.552012
WRNHomo sapiens (human)Potency35.481311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
[Tau protein] kinase Sus scrofa (pig)IC5010.000011
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC5016.187022
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC507.420011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.078011
Acetylcholine receptor subunit epsilonHomo sapiens (human)IC500.038222
Acetylcholine receptor subunit epsilonHomo sapiens (human)Ki0.152311
AcetylcholinesteraseAnopheles gambiae (African malaria mosquito)IC500.152424
AcetylcholinesteraseElectrophorus electricus (electric eel)IC503.6249324445
AcetylcholinesteraseHomo sapiens (human)IC506.1796319440
AcetylcholinesteraseMus musculus (house mouse)IC502.26701518
AcetylcholinesteraseRattus norvegicus (Norway rat)IC500.49576386
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC500.24531826
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki0.47071315
AcetylcholinesteraseHomo sapiens (human)Ki1.86662943
AcetylcholinesteraseMus musculus (house mouse)Ki0.018011
AcetylcholinesteraseRattus norvegicus (Norway rat)Ki0.000211
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki6.497025
Acetylcholinesterase Bos taurus (cattle)IC500.40232639
Acetylcholinesterase Drosophila melanogaster (fruit fly)IC501.830011
Acetylcholinesterase Bos taurus (cattle)Ki0.014649
Acyl-CoA desaturase 1Rattus norvegicus (Norway rat)IC500.047011
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC500.137512
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.517011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.513011
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC506.710011
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC504.990022
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50317.276756
Amine oxidase [flavin-containing] A Bos taurus (cattle)IC50414.023512
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50214.733438
Amine oxidase [flavin-containing] BHomo sapiens (human)IC5026.640055
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50108.885958
Amyloid-beta precursor proteinHomo sapiens (human)IC502.128334
AromataseHomo sapiens (human)IC502.900013
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000015
ATP-dependent translocase ABCB1Homo sapiens (human)IC5034.850011
Beta-secretase 1Homo sapiens (human)IC5087.50251013
Bile salt export pumpHomo sapiens (human)IC50321.5214414
Bile salt export pumpRattus norvegicus (Norway rat)IC50759.650012
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC5036.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000015
Cannabinoid receptor 1Homo sapiens (human)Ki1.000011
Cannabinoid receptor 2 Homo sapiens (human)Ki1.000011
Carbonic anhydrase 1Homo sapiens (human)IC500.338011
Carbonic anhydrase 13Mus musculus (house mouse)IC501.021011
Carbonic anhydrase 2Homo sapiens (human)IC500.059011
Carboxylic ester hydrolase Equus caballus (horse)IC505.56761621
Carboxylic ester hydrolase Musca domestica (house fly)IC509.510011
Carboxylic ester hydrolase Plutella xylostella (diamondback moth)IC501,355.500022
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC5012.21012430
Carboxylic ester hydrolase Equus caballus (horse)Ki1.034149
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50100.000011
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC500.340113
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.250011
Chain A, Histamine N-methyltransferaseHomo sapiens (human)Ki0.038218
Chain A, liver Carboxylesterase IHomo sapiens (human)Ki100.000011
Choline O-acetyltransferase Rattus norvegicus (Norway rat)IC500.005311
Choline O-acetyltransferase Rattus norvegicus (Norway rat)Ki0.000211
CholinesteraseCanis lupus familiaris (dog)IC5010,000.000011
CholinesteraseEquus caballus (horse)IC504.9084238300
CholinesteraseHomo sapiens (human)IC50140.9477198279
CholinesteraseMus musculus (house mouse)IC500.687923
CholinesteraseEquus caballus (horse)Ki1.975245
CholinesteraseHomo sapiens (human)Ki6.60641218
Coagulation factor XIIHomo sapiens (human)Ki100.000012
Cyclin-dependent kinase 5 activator 1Homo sapiens (human)IC505.100022
Cyclin-dependent-like kinase 5 Homo sapiens (human)IC503.633333
Cyclin-dependent-like kinase 5 Homo sapiens (human)Ki0.170012
Cytochrome P450 1A2Homo sapiens (human)IC500.787522
Cytochrome P450 1A2Homo sapiens (human)Ki1.940011
Cytochrome P450 1B1Homo sapiens (human)IC504.541044
Cytochrome P450 1B1Homo sapiens (human)Ki2.808825
Cytochrome P450 2C19Homo sapiens (human)IC500.059812
Cytochrome P450 2D6Homo sapiens (human)IC501.150012
Cytochrome P450 2E1Homo sapiens (human)IC500.075011
Cytochrome P450 3A4Homo sapiens (human)IC5016.4874610
DRattus norvegicus (Norway rat)IC5075.000011
D(2) dopamine receptorRattus norvegicus (Norway rat)IC5059.000011
Delta-type opioid receptorMus musculus (house mouse)IC508.397312
Dipeptidyl peptidase 4Homo sapiens (human)IC500.001011
Dual specificity protein phosphatase 3Homo sapiens (human)IC50100.000011
Fatty-acid amide hydrolase 1Homo sapiens (human)IC5030.000022
Fatty-acid amide hydrolase 1Mus musculus (house mouse)IC505.900011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC506.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC506.000011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC5031.916766
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC5025.875044
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)IC5044.000022
Glycogen synthase kinase-3 betaHomo sapiens (human)IC5035.500046
Glycogen synthase kinase-3 beta Sus scrofa (pig)IC5010.000011
Histamine H3 receptorHomo sapiens (human)IC500.350011
Histamine N-methyltransferase Rattus norvegicus (Norway rat)IC500.110011
Hormone-sensitive lipaseRattus norvegicus (Norway rat)IC500.370011
kallikrein-5 preproproteinHomo sapiens (human)IC5050.000011
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC503.200011
Liver carboxylesterase 1Homo sapiens (human)IC50100.000012
Liver carboxylesterase 1Homo sapiens (human)Ki100.000012
Lysine-specific histone demethylase 1AHomo sapiens (human)IC506.970011
Microtubule-associated protein tauRattus norvegicus (Norway rat)IC500.200011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC501.100011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50100.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5099.120015
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki100.000022
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC5013.000011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC506.600022
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC506.600022
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki5.800011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC506.600022
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC506.600022
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC506.600022
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC5035.350022
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki14.300011
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50119.100033
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.045711
Neuronal acetylcholine receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50119.100033
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.045711
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC50119.100033
Nitric oxide synthase, endothelial Rattus norvegicus (Norway rat)IC502.900011
perilipin-1Homo sapiens (human)IC5020.463011
perilipin-5Homo sapiens (human)IC5011.911011
polyadenylate-binding protein 1Homo sapiens (human)IC5066.000024
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5023.642236
Prolyl endopeptidaseHomo sapiens (human)IC50162.333323
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.014622
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.014622
Signal transducer and activator of transcription 3Homo sapiens (human)IC5014.105022
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC506.371012
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC5026.500022
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.517011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.513011
Sodium-dependent serotonin transporterHomo sapiens (human)IC501,000.000011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC5019.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC5052.360022
Solute carrier family 22 member 2Homo sapiens (human)IC500.680011
Sterol O-acyltransferase 1Homo sapiens (human)IC5050.000011
Telomerase reverse transcriptaseHomo sapiens (human)IC5037.000011
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)IC503.885022
TransporterRattus norvegicus (Norway rat)IC5016.500022
Trypanothione reductaseTrypanosoma cruziKi140.000011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5067.000011
Tyrosine-protein phosphatase non-receptor type 7Homo sapiens (human)IC50100.000011
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC500.590011
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC500.590011
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC500.590011
Voltage-dependent calcium channel gamma-1 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-2 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-3 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-4 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-5 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-6 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-7 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel gamma-8 subunitHomo sapiens (human)IC5017.000011
Voltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)IC5017.000011
Voltage-dependent calcium channel subunit alpha-2/delta-2Homo sapiens (human)IC5017.000011
Voltage-dependent calcium channel subunit alpha-2/delta-3Homo sapiens (human)IC5017.000011
Voltage-dependent calcium channel subunit alpha-2/delta-4Homo sapiens (human)IC5017.000011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5025.650022
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC5025.650022
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC5025.650022
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC5025.650022
Voltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)IC5017.000011
Voltage-dependent L-type calcium channel subunit beta-2Homo sapiens (human)IC5017.000011
Voltage-dependent L-type calcium channel subunit beta-3Homo sapiens (human)IC5017.000011
Voltage-dependent L-type calcium channel subunit beta-4Homo sapiens (human)IC5017.000011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5017.000011
Voltage-dependent P/Q-type calcium channel subunit alpha-1AHomo sapiens (human)IC5017.000011
Voltage-dependent R-type calcium channel subunit alpha-1EHomo sapiens (human)IC5017.000011
Voltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)IC5017.000011
Voltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)IC5017.000011
Voltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)IC5017.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC5076.083011
AcetylcholinesteraseHomo sapiens (human)EC500.571512
AcetylcholinesteraseElectrophorus electricus (electric eel)Kd85.008022
AcetylcholinesteraseHomo sapiens (human)Kd0.012512
AcetylcholinesteraseMus musculus (house mouse)Kd0.018011
Beta-1 adrenergic receptorHomo sapiens (human)Kd101.385214
Beta-2 adrenergic receptorHomo sapiens (human)EC503.162311
Beta-2 adrenergic receptorHomo sapiens (human)Kd68.427136
Beta-2 adrenergic receptor Bos taurus (cattle)Kd3.980011
Beta-3 adrenergic receptorHomo sapiens (human)Kd101.385214
Beta-adrenergic receptor kinase 1Homo sapiens (human)Kd7.400011
Fatty acid-binding protein, liverHomo sapiens (human)Kd900.000011
GastrotropinHomo sapiens (human)Kd200.000011
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.470011
Muscarinic acetylcholine receptor M2Sus scrofa (pig)EC506.304812
ORF73Human gammaherpesvirus 8EC5075.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseHomo sapiens (human)MIC0.000011
Beta-2 adrenergic receptor Bos taurus (cattle)Concentration1,000,000.000011
Beta-2 adrenergic receptor Bos taurus (cattle)KD app4.480011
Carbonic anhydrase 1Homo sapiens (human)Km1,683.000011
Carbonic anhydrase 13Mus musculus (house mouse)Km2,202.000011
Carbonic anhydrase 2Homo sapiens (human)Km1,645.000011
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)INH0.081011
Histamine N-methyltransferaseHomo sapiens (human)Activity0.010011
prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Active Concentration20.000011
Xaa-Pro dipeptidaseAlteromonas sp.Km7,600.000011