Page last updated: 2024-08-05 15:06:35

hypoglycemic agent

A drug which lowers the blood glucose level.

ChEBI ID: 35526

Members (67)

MemberDefinitionClass
1-deoxynojirimycinAn optically active form of 2-(hydroxymethyl)piperidine-3,4,5-triol having 2R,3R,4R,5S-configuration.duvoglustat
3,3',4,5'-tetrahydroxystilbeneA stilbenol that is trans-stilbene in which one of the phenyl groups is substituted by hydroxy groups at positions 3 and 4, while the other phenyl group is substituted by hydroxy groups at positions 3 and 5.piceatannol
5-methoxyindole-2-carboxylic acidAn indolecarboxylic acid that is indole-2-carboxylic acid carrying an additional methoxy substituent at position 5.5-methoxyindole-2-carboxylic acid
9-PAHSAA FAHFA (fatty acid ester of a hydroxy fatty acid) obtained by formal condensation of the carboxy group of palmitic acid with the hydroxy group of 9-hydroxyoctadecanoic acid (9-hydroxystearic acid).9-PAHSA
acarboseA tetrasaccharide derivative consisting of a dideoxy-4-{[4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl C7 cyclitol moiety [called valienol (or valienamine)] linked via nitrogen to isomaltotriose.acarbose
acetohexamideAn N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is replaced by a p-acetylphenylsulfonyl group, while a hydrogen attached to the other nitrogen is replaced by a cyclohexyl group.acetohexamide
alogliptinA piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes.alogliptin
ambreinA triterpenoid alcohol that is a constituent of ambergris, an intestinal secretion of the sperm whale Physeter catodon.ambrein
as 1842856A quinolone that is 4-quinolone substituted at positions 1, 3, 5, 6 and 7 by ethyl, carboxy, amino, fluorine, and cyclohexylamino groups, respectively. It can directly bind to and block the transcription activity of the active forkhead box protein O1 (Foxo1), but not the Ser256-phosphorylated form. It induces cell death and growth arrest in Burkitt lymphoma cell lines at low concentrations.AS1842856
aspalathinA member of the class of dihydrochalcones that is the 2-C-beta-D-glucopyranide of phloroglucinol and which is substituted at position 4 by a 3-(3,4-dihydroxyphenyl)propanoyl group. A metabolite of red bush, Aspalathus linearis (and present in the herbal tea made from the leaves), aspalathin exhibits significant hypoglycemic activity.aspalathin
azd 7545A sulfone that is benzene substituted by [4-(dimethylcarbamoyl)phenyl]sulfonyl, chloro and [(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino groups at positions 1, 3 and 4, respectively. It is a potent and non-ATP-competitive inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC50 of 6.4 nM and exhibits glucose-lowering activity. Also inhibits PDHK1 at higher levels (IC50 = 36.8 nM).AZD7545
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
berberineberberine
bms 477118A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2S)-amino(3-hydroxyadamantan-1-yl)acetic acid with the amino group of (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile. Used in its monohydrate form for the treatment of Type II diabetes.saxagliptin
buforminA member of the class of biguanides that is biguanide substituted by a butyl group at position 1. It is an antidiabetic drug with potential antitumor effect.buformin
buteinA chalcone that is (E)-chalcone bearing four additional hydroxy substituents at positions 2', 3, 4 and 4'.butein
butylidenephthalideA gamma-lactone that is phthalide substituted by a butylidene group at position 3. Isolated from Ligusticum porteri, it exhibits hypoglycemic activity.(Z)-3-butylidenephthalide
cafestolAn organic heteropentacyclic compound and furan diterpenoid with formula C20H28O3 obtained from the unsaponifiable fraction of coffee oil (a lipid fraction obtained from coffee beans by organic solvent extraction).cafestol
canagliflozinA C-glycosyl compound that is used (in its hemihydrate form) for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.canagliflozin
capsiateA carboxylic ester obtained by formal condensation of the carboxy group of (6E)-8-methylnon-6-enoic acid with the benzylic hydroxy group of vanillyl alcohol. A non-pungent analogue of capsaicin with a similar biological profile.capsiate
chir 98014A member of the class of aminopyrimidines that is pyrimidine substituted by {2-[(6-amino-5-nitropyridin-2-yl)amino]ethyl}amino, 2,4-dichlorophenyl, and 1H-imidazol-1-yl groups at positions 2, 4 and 5, respectively. It is a potent ATP-competitive inhibitor of GSK3alpha and GSK3beta (IC50 values of 0.65 and 0.58 nM, respectively).CHIR-98014
chlorpropamideAn N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.chlorpropamide
chromium tripicolinatetris(picolinato)chromium
cinnamaldehydeThe E (trans) stereoisomer of cinnamaldehyde, the parent of the class of cinnamaldehydes.(E)-cinnamaldehyde
dapagliflozinA C-glycosyl comprising beta-D-glucose in which the anomeric hydroxy group is replaced by a 4-chloro-3-(4-ethoxybenzyl)phenyl group. Used (in the form of its propanediol monohydrate) to improve glycemic control, along with diet and exercise, in adults with type 2 diabetes.dapagliflozin
empagliflozinA C-glycosyl compound consisting of a beta-glucosyl residue having a (4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl group at the anomeric centre. A sodium-glucose co-transporter 2 inhibitor used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.empagliflozin
fraxetinA hydroxycoumarin that is 6-methoxycoumarin in which the hydrogens at positions 7 and 8 have been replaced by hydroxy groups.fraxetin
ginsenoside rb2A ginsenoside found in Panax ginseng that is dammarane which is substituted by hydroxy groups at the 3beta, 12beta and 20 pro-S positions, in which the hydroxy groups at positions 3 and 20 have been converted to the corresponding beta-D-glucopyranosyl-(1->2)-beta-D-glucopyranoside and alpha-L-arabinopyranosyl-(1->6)-beta-D-glucopyranoside respectively, and in which a double bond has been introduced at the 24-25 position.ginsenoside Rb2
ginsenoside rcA ginsenoside found in Panax ginseng that is dammarane which is substituted by hydroxy groups at the 3beta, 12beta and 20 pro-S positions, in which the hydroxy groups at positions 3 and 20 have been converted to the corresponding beta-D-glucopyranosyl-(1->2)-beta-D-glucopyranoside and alpha-L-arabinofuranosyl-(1->6)-beta-D-glucopyranoside respectively, and in which a double bond has been introduced at the 24-25 position.ginsenoside Rc
gliclazidegliclazide
glipizideAn N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.glipizide
glyburideAn N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.glyburide
glymidineA sulfonamide that is N-(pyrimidin-2-yl)benzenesulfonamide which is substituted at position 5 of the pyrimidine ring by a 2-methoxyethoxy group. It is a hypoglycemic drug used for the treatment of diabetes mellitus.glymidine
guanidinopropionic acidA guanidine compound bearing an N-(2-carboxyethyl) substituent. It is a creatine analogue that has been found to decreases plasma glucose levels3-guanidinopropanoic acid zwitterion; 3-guanidinopropanoic acid
lespenefrilA glycosyloxyflavone that is kaempferol attached to alpha-L-rhamnopyranosyl residues at positions 3 and 7 respectively via glycosidic linkages. It has been isolated from the aerial parts of Vicia faba and Lotus edulis.kaempferol 3,7-di-O-alpha-L-rhamnoside
linagliptinA xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes.linagliptin
mangiferinA C-glycosyl compound consisting of 1,3,6,7-tetrahydroxyxanthen-9-one having a beta-D-glucosyl residue at the 6-position.mangiferin
marsupsinA member of the class of 1-benzofurans that is 1-benzofuran-3(2H)-one, substituted by hydroxy groups at positions 2 and 6, a 4-hydroxybenzyl group at position 2 and a methoxy group at position 4. Isolated from the heartwood of Pterocarpus marsupium, it exhibits antihyperglycemic and antihyperlipidemic activities.marsupsin
masoprocolThe meso-form of nordihydroguaiaretic acid. An antioxidant found in the creosote bush, Larrea divaricata, it is a potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. It also inhibits (though to a lesser extent) formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase.masoprocol
medica 16An alpha,omega-dicarboxylic acid that is hexadecanedioic acid carrying methyl groups at positions 3 and 14. It is a free fatty acid 1 (FFA1/GPR40) receptor agonist and an ATP citrate lyase inhibitor, and exhibits hypolipidemic and antidiabetogenic properties.MEDICA 16
metforminA member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.metformin
metformin hydrochlorideA hydrochloride resulting from the reaction of metformin with one molar equivalent of hydrogen chloride.metformin hydrochloride
myricetinA hexahydroxyflavone that is flavone substituted by hydroxy groups at positions 3, 3', 4', 5, 5' and 7. It has been isolated from the leaves of Myrica rubra and other plants.myricetin
norvalineA 2-aminopentanoic acid that has S-configuration.L-2-aminopentanoic acid zwitterion; L-2-aminopentanoic acid
octyl gallateA gallate ester obtained by condensation of the carboxy group of gallic acid with the hydroxy group of octanol.octyl gallate
phenforminA member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.phenformin
pinoresinolAn enantiomer of pinoresinol having (+)-1S,3aR,4S,6aR-configuration.(+)-pinoresinol
pioglitazoneA member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.pioglitazone
prunin protein, prunusA flavanone 7-O-beta-D-glucoside that is (S)-naringenin substituted by a beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.naringenin 7-O-beta-D-glucoside
pterostilbeneA stilbenol that consists of trans-stilbene bearing a hydroxy group at position 4 as well as two methoxy substituents at positions 3' and 5'.pterostilbene
rhapontinA rhaponticin in which the double bond adopts a trans-configuration. It possesses a range of pharmacological activities including antitumour, antiinflammatory, antilipemic and neuroprotective activities.trans-rhaponticin
salicylsalicylic acidA dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes.salsalate
salvianolic acid BA member of the class of 1-benzofurans that is an antioxidant and free radical scavenging compound extracted from S. miltiorrhizasalvianolic acid B
salvigeninA trimethoxyflavone that is scutellarein in which the hydroxy groups at positions 4', 6, and 7 are replaced by methoxy groups.salvigenin
saroglitazarA monocarboxylic acid that is (2S)-2-ethoxy-3-(p-ethoxyphenyl)propanoic acid in which one of the methyl hydrogens of the p-ethoxy substituent has been replaced by the nitrogen of 2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrole. An agonist at the subtypes alpha and gamma of the peroxisome proliferator-activated receptor (PPAR) with predominant PPARalpha activity, it is used in the treatment of type 2 diabetes.saroglitazar
semaglutideA polypeptide that contains a linear sequence of 31 amino acids joined together by peptide linkages. It is an agonist of glucagon-like peptide-1 receptors (GLP-1 AR) and used for the treatment of type 2 diabetes.semaglutide
sitagliptinA triazolopyrazine that exhibits hypoglycemic activity.sitagliptin
steviosideA diterpene glycoside that is rubusoside in which the hydroxy group at position 2 of the allylic beta-D-glucoside has been converted to the corresponding beta-D-glucoside. It is a natural herbal sweetener that is 250-300 times sweeter than sucrose (though with a bitter aftertaste), extracted from the Stevia rebaudiana plant native to South America.stevioside
swerchirinA member of the class of xanthones that is the 5-O-methyl derivative of bellidifolin. Isolated from Centaurium erythraea and Swertia chirayita, it exhibits hypoglycemic activity.swerchirin
swertisinA flavone C-glycoside that is 7-O-methylapigenin in which the hydrogen at position 6 has been replaced by a beta-D-glucosyl residue.swertisin
synthalin aA member of the class of guanidines that is decane having guanidino groups at the 1- and 10-positions.synthalin A
syringaldehydeA hydroxybenzaldehyde that is 4-hydroxybenzaldehyde substituted by methoxy groups at positions 3 and 5. Isolated from Pisonia aculeata and Panax japonicus var. major, it exhibits hypoglycemic activity.syringaldehyde
terbutalineA member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.terbutaline
theasinensin aA biflavonoid that is obtained by coupling of two molecules of (-)-epigallocatechin 3-gallate resulting in a bond between positions C-2 of the hydroxyphenyl ring. It is a natural product found in oolong tea.theasinensin A
tolazamideAn N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.tolazamide
tolbutamideAn N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.tolbutamide
troglitazonetroglitazone

Research

Studies (56,726)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19909,624 (16.97)18.7374
1990's6,081 (10.72)18.2507
2000's10,623 (18.73)29.6817
2010's20,264 (35.72)24.3611
2020's10,134 (17.86)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials8,100 (12.49%)5.53%
Reviews6,322 (9.75%)6.00%
Case Studies2,185 (3.37%)4.05%
Observational427 (0.66%)0.25%
Other47,804 (73.73%)84.16%

Protein Targets (559)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency13.754619
15-lipoxygenase, partialHomo sapiens (human)Potency3.514626
67.9K proteinVaccinia virusPotency13.699622
acetylcholinesteraseHomo sapiens (human)Potency60.205426
acid sphingomyelinaseHomo sapiens (human)Potency25.118911
activating transcription factor 6Homo sapiens (human)Potency49.592423
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.7705224
alpha-galactosidaseHomo sapiens (human)Potency18.884813
Alpha-synucleinHomo sapiens (human)Potency29.092911
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency3.839613
AR proteinHomo sapiens (human)Potency26.75151147
aryl hydrocarbon receptorHomo sapiens (human)Potency38.891026
arylsulfatase AHomo sapiens (human)Potency22.778816
ATAD5 protein, partialHomo sapiens (human)Potency12.482047
Ataxin-2Homo sapiens (human)Potency15.167413
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.8972414
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency22.632712
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.481611
beta-2 adrenergic receptorHomo sapiens (human)Potency10.322511
Bloom syndrome protein isoform 1Homo sapiens (human)Potency30.8540215
BRCA1Homo sapiens (human)Potency17.782812
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency46.474315
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency76.958811
caspase-1 isoform alpha precursorHomo sapiens (human)Potency23.735812
caspase-3Cricetulus griseus (Chinese hamster)Potency1.535511
caspase-3Homo sapiens (human)Potency76.958811
Caspase-7Cricetulus griseus (Chinese hamster)Potency1.535511
Caspase-7Homo sapiens (human)Potency17.900812
Cellular tumor antigen p53Homo sapiens (human)Potency49.8227310
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency19.220323
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency17.0251111
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency21.4105311
Chain A, Beta-lactamaseEscherichia coli K-12Potency45.554014
Chain A, CruzipainTrypanosoma cruziPotency20.599024
Chain A, Ferritin light chainEquus caballus (horse)Potency15.148624
Chain A, HADH2 proteinHomo sapiens (human)Potency4.6509213
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency43.830216
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.8103323
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency14.4183114
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency21.8299111
Chain B, HADH2 proteinHomo sapiens (human)Potency4.6509213
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency35.5300210
ClpPBacillus subtilisPotency0.631011
cytochrome P450 2C19 precursorHomo sapiens (human)Potency16.246119
cytochrome P450 2C9 precursorHomo sapiens (human)Potency11.2635111
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.9822112
cytochrome P450 2D6Homo sapiens (human)Potency22.579618
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency17.899016
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.3983223
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency7.744719
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency25.062419
D(1A) dopamine receptorHomo sapiens (human)Potency6.794334
D(1A) dopamine receptorSus scrofa (pig)Potency19.881212
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency16.440812
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency35.481311
DNA polymerase betaHomo sapiens (human)Potency2.979013
DNA polymerase eta isoform 1Homo sapiens (human)Potency4.921325
DNA polymerase III, partialBacillus subtilisPotency13.460212
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency32.0013213
DNA polymerase kappa isoform 1Homo sapiens (human)Potency14.1797221
endonuclease IVEscherichia coliPotency0.112211
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.55011166
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency17.278425
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.18011027
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency6.6897125
EWS/FLI fusion proteinHomo sapiens (human)Potency16.5274439
farnesoid X nuclear receptorHomo sapiens (human)Potency37.562335
flap endonuclease 1Homo sapiens (human)Potency6.3726315
Fumarate hydrataseHomo sapiens (human)Potency29.423414
GVesicular stomatitis virusPotency8.9822112
GABA theta subunitRattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.0476112
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.0476112
gemininHomo sapiens (human)Potency4.7069314
GLI family zinc finger 3Homo sapiens (human)Potency17.7752219
glp-1 receptor, partialHomo sapiens (human)Potency8.376023
GLS proteinHomo sapiens (human)Potency9.7694213
glucocerebrosidaseHomo sapiens (human)Potency21.225217
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency25.0067416
glucokinase regulatory proteinHomo sapiens (human)Potency7.079511
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency7.079511
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency21.549426
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency7.079511
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency7.079511
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency31.622811
Guanine nucleotide-binding protein GHomo sapiens (human)Potency8.912511
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency10.000011
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency20.095824
heat shock protein beta-1Homo sapiens (human)Potency56.617024
hexokinase-4 isoform 1Homo sapiens (human)Potency7.079511
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency9.2440245
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency27.5506110
Histone H2A.xCricetulus griseus (Chinese hamster)Potency76.712323
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency31.622811
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.9822112
huntingtin isoform 2Homo sapiens (human)Potency11.220211
hypothetical protein, conservedTrypanosoma bruceiPotency22.0112410
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency29.450223
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency3.9863212
IDH1Homo sapiens (human)Potency26.101112
importin subunit beta-1 isoform 1Homo sapiens (human)Potency38.145622
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.9822124
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.7173210
Integrin alpha-IIbHomo sapiens (human)Potency25.118911
Integrin beta-3Homo sapiens (human)Potency25.118911
Interferon betaHomo sapiens (human)Potency10.5720320
interleukin 8Homo sapiens (human)Potency70.901112
lamin isoform A-delta10Homo sapiens (human)Potency4.3320212
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.143916
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency10.739823
LuciferasePhotinus pyralis (common eastern firefly)Potency25.076847
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency12.589311
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency4.1719811
M-phase phosphoprotein 8Homo sapiens (human)Potency20.774416
Microtubule-associated protein tauHomo sapiens (human)Potency15.4259218
mitogen-activated protein kinase 1Homo sapiens (human)Potency27.936525
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.316025
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency35.332513
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency4.466811
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency4.466811
neuropeptide S receptor isoform AHomo sapiens (human)Potency5.011911
NFKB1 protein, partialHomo sapiens (human)Potency6.546028
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.246013
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency4.512512
Nrf2Homo sapiens (human)Potency32.642711
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency37.7534424
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency32.642711
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency50.118711
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency47.136425
Nuclear receptor ROR-gammaHomo sapiens (human)Potency37.578011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.590925
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency36.330239
P53Homo sapiens (human)Potency10.000011
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency76.675813
ParkinHomo sapiens (human)Potency10.515425
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency42.582024
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency9.249427
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency71.223914
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency12.9017414
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency21.790648
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency10.499435
phosphopantetheinyl transferaseBacillus subtilisPotency35.8029113
plasminogen precursorMus musculus (house mouse)Potency9.581812
polyproteinZika virusPotency29.423414
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency7.122514
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency3.343027
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481313
PPM1D proteinHomo sapiens (human)Potency12.587814
pregnane X nuclear receptorHomo sapiens (human)Potency45.9632311
progesterone receptorHomo sapiens (human)Potency27.046024
pyruvate kinaseLeishmania mexicana mexicanaPotency1.995322
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency15.848911
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency29.515612
RAR-related orphan receptor gammaMus musculus (house mouse)Potency19.6100215
ras-related protein Rab-9AHomo sapiens (human)Potency51.070013
regulator of G-protein signaling 4Homo sapiens (human)Potency10.473518
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency33.8122319
retinoid X nuclear receptor alphaHomo sapiens (human)Potency27.2963414
RGS12Homo sapiens (human)Potency10.000011
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency20.963425
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency9.466211
shiga toxin 1 B subunitEscherichia coli O157:H7Potency10.023822
shiga toxin 1 variant A subunitEscherichia coli O157:H7Potency10.023822
Single-stranded DNA cytosine deaminaseHomo sapiens (human)Potency44.668413
SMAD family member 2Homo sapiens (human)Potency26.839329
SMAD family member 3Homo sapiens (human)Potency26.839329
Smad3Homo sapiens (human)Potency3.162311
snurportin-1Homo sapiens (human)Potency38.145622
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency13.790025
survival motor neuron protein isoform dHomo sapiens (human)Potency12.447119
TAR DNA-binding protein 43Homo sapiens (human)Potency14.591912
TDP1 proteinHomo sapiens (human)Potency21.6421233
thioredoxin glutathione reductaseSchistosoma mansoniPotency12.967612
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.1618324
ThrombopoietinHomo sapiens (human)Potency7.506024
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency16.0131310
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency28.572735
thyroid stimulating hormone receptorHomo sapiens (human)Potency16.2648415
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency25.118911
tyrosine-protein kinase YesHomo sapiens (human)Potency1.729111
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.697923
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency9.581812
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency9.581812
USP1 protein, partialHomo sapiens (human)Potency52.458427
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency32.266123
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency31.735034
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency31.884517
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency24.443415
WRNHomo sapiens (human)Potency1.122011

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrialHomo sapiens (human)IC500.041011
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)IC500.080011
1-deoxy-D-xylulose 5-phosphate reductoisomeraseEscherichia coli K-12IC501.500011
17-beta-hydroxysteroid dehydrogenase type 2Homo sapiens (human)IC507.300011
2-5A-dependent ribonucleaseHomo sapiens (human)IC50264.000011
3-oxoacyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC5014.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50100.000011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50100.000011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC501.312011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.835011
5-hydroxytryptamine receptor 7Homo sapiens (human)IC50126.600011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC500.782733
AcetylcholinesteraseHomo sapiens (human)IC500.400022
AcetylcholinesteraseHomo sapiens (human)Ki37.800011
Adenosine receptor A3Homo sapiens (human)IC505.208011
Adenosine receptor A3Homo sapiens (human)Ki2.943011
ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1Homo sapiens (human)IC5062.400012
AlbuminHomo sapiens (human)Ki44,441,533,333.333313
Aldo-keto reductase family 1 member A1Homo sapiens (human)IC50100.000011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC5064.500022
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC503.200011
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC50100.000011
Aldo-keto reductase family 1 member C1Homo sapiens (human)IC50152.740022
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC50338.663333
Aldo-keto reductase family 1 member C21Mus musculus (house mouse)IC5012.300011
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC508.040044
Aldo-keto reductase family 1 member C4Homo sapiens (human)IC504.040011
alkaline phosphatase, tissue-nonspecific isozyme isoform 1 preproproteinHomo sapiens (human)IC5033.200011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC503.254022
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki2.943011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC503.254022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.943011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC501.300011
Alpha-amylaseAcarus siroIC503.800011
Alpha-amylase Geobacillus stearothermophilusIC501.670011
Alpha-amylase 1A Homo sapiens (human)IC5020.465323
Alpha-galactosidase AHomo sapiens (human)Ki18.000011
Alpha-glucosidase Blautia obeumIC501,030.000011
Alpha-glucosidase MAL12Saccharomyces cerevisiae S288CIC50303.540035
Alpha-glucosidase MAL12Saccharomyces cerevisiae S288CKi18.000011
Alpha-glucosidase MAL32Saccharomyces cerevisiae S288CIC50267.322045
Alpha-glucosidase MAL62Saccharomyces cerevisiae (brewer's yeast)IC50212,855.000022
Alpha-mannosidaseCanavalia ensiformis (jack bean)Ki270.000011
Alpha-mannosidase 2Rattus norvegicus (Norway rat)Ki50.000011
Alpha-synucleinHomo sapiens (human)IC506.760022
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5017.864522
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki10.500011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Ki2.535422
Amine oxidase [flavin-containing] BHomo sapiens (human)IC501.184024
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki2.617644
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki3.367644
Aminopeptidase NHomo sapiens (human)IC50100.000011
Amyloid-beta precursor proteinHomo sapiens (human)IC509.914377
Angiopoietin-1 receptorHomo sapiens (human)IC505.000011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50243,576.910033
Angiotensin-converting enzyme Homo sapiens (human)IC5011.000011
Angiotensin-converting enzyme 2 Homo sapiens (human)IC5010.000011
Anthrax toxin receptor 2Homo sapiens (human)IC50300.000011
Arginase Leishmania amazonensisIC502.100011
Arginase Leishmania amazonensisKi1.200011
Arginase-1Bos taurus (cattle)IC5047.000011
Arginase-1Homo sapiens (human)IC50622.500022
Arginase-1Bos taurus (cattle)Ki136.000033
AromataseHomo sapiens (human)IC5010.000011
ATP synthase subunit beta, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit delta, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit epsilon, mitochondrialBos taurus (cattle)IC50100.000011
ATP synthase subunit gamma, mitochondrialBos taurus (cattle)IC50100.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50116.1667112
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC500.644622
ATP-binding cassette sub-family C member 9Homo sapiens (human)IC500.220011
ATP-citrate synthase Rattus norvegicus (Norway rat)Ki11.666733
ATP-dependent translocase ABCB1Homo sapiens (human)IC5042.000011
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC500.503133
Aurora kinase BHomo sapiens (human)IC503.980011
Beta-glucosidaseAgrobacterium tumefaciensKi12.000022
Beta-glucosidase Prunus avium (sweet cherry)IC5081.000011
Beta-glucosidase ACaldicellulosiruptor saccharolyticusIC50218.333333
Beta-glucuronidaseHomo sapiens (human)IC5038.000011
Beta-hydroxyacyl-ACP dehydratase precursor (Fatty acid synthesis protein)Plasmodium falciparum (malaria parasite P. falciparum)IC502.000011
Beta-lactamaseEscherichia coli K-12IC50300.000011
Beta-secretase 1Homo sapiens (human)IC503.116733
Bile salt export pumpHomo sapiens (human)IC50239.1300949
Bile salt export pumpRattus norvegicus (Norway rat)IC50338.177839
Bile salt export pumpHomo sapiens (human)Ki27.500011
Bile salt export pumpRattus norvegicus (Norway rat)Ki6.100011
Breakpoint cluster region proteinHomo sapiens (human)IC5010.000011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50150.000022
Calcium dependent protein kinaseTriticum aestivum (bread wheat)IC5019.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50121.9000210
Carbonic anhydrase 1Homo sapiens (human)Ki21.620033
Carbonic anhydrase 12Homo sapiens (human)Ki28.850022
Carbonic anhydrase 13Homo sapiens (human)Ki9.730011
Carbonic anhydrase 2Homo sapiens (human)IC500.542012
Carbonic anhydrase 2Homo sapiens (human)Ki51.433333
Carbonic anhydrase 4Homo sapiens (human)Ki10.000011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki10.000011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki10.000011
Carbonic anhydrase 7Homo sapiens (human)Ki4.320011
Carbonic anhydrase 9Homo sapiens (human)Ki20.203333
Carnitine O-palmitoyltransferase 1, liver isoformHomo sapiens (human)IC5010.000011
Carnitine O-palmitoyltransferase 2, mitochondrialHomo sapiens (human)IC50100.000011
Carnitine O-palmitoyltransferase 2, mitochondrialRattus norvegicus (Norway rat)IC50100.000011
Casein kinase I isoform epsilonHomo sapiens (human)IC505.000011
Casein kinase II subunit alphaHomo sapiens (human)IC500.940033
Casein kinase II subunit alpha 3Homo sapiens (human)IC500.900011
Casein kinase II subunit alpha'Homo sapiens (human)IC500.940033
Casein kinase II subunit betaHomo sapiens (human)IC500.940033
Catechol O-methyltransferaseHomo sapiens (human)IC50147.100011
Catechol O-methyltransferaseRattus norvegicus (Norway rat)IC50147.100011
Cationic trypsinBos taurus (cattle)IC5010.200011
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)IC5023.875012
CDGSH iron-sulfur domain-containing protein 1Rattus norvegicus (Norway rat)IC501.000011
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)Ki1.020512
CDGSH iron-sulfur domain-containing protein 2Homo sapiens (human)IC504.800011
Cell division protein FtsZEscherichia coli K-12IC506.335022
Ceramide glucosyltransferaseHomo sapiens (human)IC50100.000011
Chain A [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 1Homo sapiens (human)IC500.087011
Chain A [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 3Homo sapiens (human)IC500.087011
Chain A, Dipeptidyl peptidase IVHomo sapiens (human)IC500.018011
Chain A, Pancreatic alpha-amylaseHomo sapiens (human)Ki110.000012
Chain A, Proto-oncogene serine/threonine-protein kinase Pim-1Homo sapiens (human)IC500.780014
Cholesteryl ester transfer proteinOryctolagus cuniculus (rabbit)IC50238.600011
CholinesteraseEquus caballus (horse)IC5015.266733
CholinesteraseHomo sapiens (human)IC5015.895022
Chymotrypsinogen ABos taurus (cattle)IC50360.000011
Cyclin-dependent kinase 1Homo sapiens (human)IC504.000011
Cyclin-dependent-like kinase 5 Homo sapiens (human)IC500.700011
Cystathionine beta-synthaseHomo sapiens (human)IC5018.800011
Cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC5015.000011
Cytochrome P450 1A1Homo sapiens (human)Ki0.503323
Cytochrome P450 1A2Homo sapiens (human)IC505.150022
Cytochrome P450 1B1Homo sapiens (human)IC500.974733
Cytochrome P450 1B1Homo sapiens (human)Ki0.252044
Cytochrome P450 2C19Homo sapiens (human)IC5010.000011
Cytochrome P450 2C9 Homo sapiens (human)IC503.277245
Cytochrome P450 2C9 Homo sapiens (human)Ki70.000011
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC5045.400011
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC501,927.000011
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC50833.000011
Cytochrome P450 2D6Homo sapiens (human)IC5056.480045
Cytochrome P450 3A4Homo sapiens (human)IC5057.907956
Cytosolic beta-glucosidaseHomo sapiens (human)IC50160.000022
D(3) dopamine receptorRattus norvegicus (Norway rat)IC502.000011
Death-associated protein kinase 1Homo sapiens (human)IC5023.000011
Delta-type opioid receptorHomo sapiens (human)Ki26.000011
Dihydrofolate reductaseHomo sapiens (human)Ki9,070.000012
Dihydroorotate dehydrogenase Leishmania majorIC5030.766412
Dipeptidyl peptidase 2Homo sapiens (human)IC5093.32251930
Dipeptidyl peptidase 4Homo sapiens (human)IC505.332480101
Dipeptidyl peptidase 4Mus musculus (house mouse)IC5050.023022
Dipeptidyl peptidase 4Rattus norvegicus (Norway rat)IC5012.683733
Dipeptidyl peptidase 4Homo sapiens (human)Ki0.000666
Dipeptidyl peptidase 8Homo sapiens (human)IC5050.75383347
Dipeptidyl peptidase 8Homo sapiens (human)Ki0.130011
Dipeptidyl peptidase 9Bos taurus (cattle)IC50100.000012
Dipeptidyl peptidase 9Homo sapiens (human)IC5071.88662635
Dipeptidyl peptidase 9Homo sapiens (human)Ki0.071011
Dipeptidyl peptidase IVPorphyromonas gingivalisIC5014.000012
DNA dC->dU-editing enzyme APOBEC-3A isoform aHomo sapiens (human)IC5017.500011
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)IC502.390011
DNA primase TraCEscherichia coliIC50700.000011
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)IC500.320022
ELAV-like protein 3Homo sapiens (human)IC501.000011
Enoyl-[acyl-carrier-protein] reductase [NADH] Francisella tularensis subsp. tularensis SCHU S4IC5079.000011
Enoyl-[acyl-carrier-protein] reductase [NADH] FabIEscherichia coli K-12IC5030.000011
Enoyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)IC506.450022
Enoyl-acyl-carrier protein reductase Plasmodium falciparum (malaria parasite P. falciparum)Ki2.828033
Epidermal growth factor receptorHomo sapiens (human)IC5012.000022
Estrogen receptorHomo sapiens (human)IC508.740011
Fibroblast growth factor receptor 1Homo sapiens (human)IC501.000011
Forkhead box protein M1Homo sapiens (human)IC50122.400011
Forkhead box protein M1Homo sapiens (human)Ki0.052011
Forkhead box protein O1Homo sapiens (human)IC500.033011
G-protein coupled receptor 35Homo sapiens (human)IC502.120011
GABA theta subunitRattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.800011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.800011
Genome polyprotein Zika virusIC5011.650022
Genome polyprotein Zika virusKi0.800011
Glyceraldehyde-3-phosphate dehydrogenase, glycosomalTrypanosoma cruziIC50149.000011
Glycogen debranching enzymeHomo sapiens (human)IC5010.000011
Glycogen debranching enzymeOryctolagus cuniculus (rabbit)IC500.190011
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC500.007011
Glycogen synthase kinase-3 betaHomo sapiens (human)IC500.003123
Heat shock protein HSP 90-betaHomo sapiens (human)IC5013.500011
Indoleamine 2,3-dioxygenase 1Mus musculus (house mouse)IC5061.000011
Indoleamine 2,3-dioxygenase 2Mus musculus (house mouse)IC504.500011
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)IC5032.100011
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)Ki5.510011
Inositol hexakisphosphate kinase 2Homo sapiens (human)IC500.700011
Inositol polyphosphate multikinaseHomo sapiens (human)IC501.100011
Insulin receptorHomo sapiens (human)IC502.000011
Insulin receptorHomo sapiens (human)Ki2.600011
Insulin-degrading enzymeHomo sapiens (human)IC50100.000011
Insulin-like growth factor 1 receptorHomo sapiens (human)IC502.000011
Integrase Human immunodeficiency virus 1IC508.775466
integrase, partialHuman immunodeficiency virus 1IC500.948922
Interstitial collagenaseHomo sapiens (human)IC502.920011
intestinal alkaline phosphatase precursorMus musculus (house mouse)IC5012.500011
Kynurenine 3-monooxygenaseRattus norvegicus (Norway rat)IC50100.000011
Lactase-phlorizin hydrolaseHomo sapiens (human)IC5062.000011
Lactase-phlorizin hydrolase Rattus norvegicus (Norway rat)IC5036.333333
Lactoylglutathione lyaseHomo sapiens (human)IC501.315044
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50200.000012
large T antigenBetapolyomavirus macacaeIC5016.350011
lens epithelium-derived growth factor p75Homo sapiens (human)IC500.948922
LIM domain kinase 1Homo sapiens (human)IC5010.000044
LIM domain kinase 2Homo sapiens (human)IC5010.000044
Lysine-specific demethylase 4EHomo sapiens (human)IC503.000011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC502.396733
Lysosomal acid glucosylceramidaseBos taurus (cattle)IC50210.000011
Lysosomal acid glucosylceramidaseHomo sapiens (human)IC50280.333366
Lysosomal acid glucosylceramidaseHomo sapiens (human)Ki68.333333
Lysosomal alpha-glucosidaseHomo sapiens (human)IC50358.85291617
Lysosomal alpha-glucosidaseMus musculus (house mouse)IC50144.470012
Lysosomal alpha-glucosidaseRattus norvegicus (Norway rat)IC500.312544
Lysosomal alpha-glucosidaseHomo sapiens (human)Ki12.529522
Malate dehydrogenase, cytoplasmicHomo sapiens (human)IC50400.000011
Maltase-glucoamylase, intestinalHomo sapiens (human)IC50280.55211819
Mannosyl-oligosaccharide glucosidaseSaccharomyces cerevisiae S288CIC5013.340011
Matrix metalloproteinase-9Homo sapiens (human)IC500.250011
Microtubule-associated protein tauHomo sapiens (human)IC502.100022
Mitogen-activated protein kinase 1Homo sapiens (human)IC505.619022
Mitogen-activated protein kinase 10Homo sapiens (human)IC501.940012
Mitogen-activated protein kinase 14Homo sapiens (human)IC501.940012
MO15-related protein kinase Pfmrk Plasmodium falciparum (malaria parasite P. falciparum)IC50157.000011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC5016.000011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50250.000011
Multidrug resistance-associated protein 1 Homo sapiens (human)IC5020.000011
Multidrug resistance-associated protein 1 Homo sapiens (human)Ki7.850022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50109.8333112
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.296733
Myosin light chain kinase, smooth muscleHomo sapiens (human)IC5012.000022
Myosin light chain kinase, smooth muscleHomo sapiens (human)Ki1.700011
NACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)IC5012.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC5010.000022
NeprilysinHomo sapiens (human)IC50100.000011
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC5035.350022
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki14.300011
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC5042.346055
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.820011
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.820011
Neutral alpha-glucosidase ABHomo sapiens (human)IC50472.825034
Neutral alpha-glucosidase ABHomo sapiens (human)Ki410.000011
Non-lysosomal glucosylceramidaseHomo sapiens (human)IC5024.950044
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC5038.000011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC5038.000011
Oligo-1,6-glucosidase IMA1Saccharomyces cerevisiae S288CIC50408.15451011
Oxysterols receptor LXR-alphaHomo sapiens (human)IC50137.500034
Oxysterols receptor LXR-betaHomo sapiens (human)IC50150.000023
P2Y purinoceptor 12Homo sapiens (human)Ki36.400011
Pancreatic alpha-amylaseSus scrofa (pig)IC508.708655
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC5010.000011
Peroxisome proliferator-activated receptor alphaMus musculus (house mouse)IC501.150011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC503.53181114
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)IC500.700011
Peroxisome proliferator-activated receptor gammaRattus norvegicus (Norway rat)IC500.700011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.48951114
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC506.400011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)IC503.260022
Polyphenol oxidase 2Agaricus bisporusIC50376.666733
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC508.350046
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC500.004611
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC505.106011
Potassium voltage-gated channel subfamily D member 3Homo sapiens (human)IC50100,000.000011
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC50316.228011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50228.000889
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC50316.228011
POU domain, class 2, transcription factor 1Homo sapiens (human)IC5043.000022
POU domain, class 2, transcription factor 2Homo sapiens (human)IC5080.000011
Probable maltase-glucoamylase 2Homo sapiens (human)IC50439.92171112
Prolyl endopeptidaseHomo sapiens (human)IC50114.500066
Prolyl endopeptidase FAPHomo sapiens (human)IC50196.55951321
Prolyl endopeptidase FAPMus musculus (house mouse)IC5033.580033
Prostaglandin G/H synthase 1Homo sapiens (human)IC50262.350022
Prostaglandin G/H synthase 1Ovis aries (sheep)IC506.750012
Prostaglandin G/H synthase 2Homo sapiens (human)IC5064.830034
Proteasome subunit beta type-5Homo sapiens (human)IC5011.000022
Protein E6Human papillomavirus 16IC500.850011
Protein-lysine 6-oxidaseHomo sapiens (human)IC501.000011
Protein-lysine 6-oxidaseHomo sapiens (human)Ki79.000011
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC5065.000022
Proton-coupled amino acid transporter 1Homo sapiens (human)Ki23,650.000012
Putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)IC500.040022
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)IC505.000011
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC500.777544
Replicase polyprotein 1abBetacoronavirus England 1IC5010.000012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC505.586723
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5016.140011
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC505.100011
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC506.750012
Serine/threonine-protein kinase B-rafHomo sapiens (human)IC501.562011
Serine/threonine-protein kinase Chk1Homo sapiens (human)IC5010.000011
Serine/threonine-protein kinase pim-1Homo sapiens (human)IC500.780022
Short transient receptor potential channel 5Homo sapiens (human)IC5010.000011
SialidaseClostridium perfringensIC5016.200011
Sialidase-2Homo sapiens (human)IC50150.000011
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50712.642522
Sodium/glucose cotransporter 1Homo sapiens (human)IC501.74861518
Sodium/glucose cotransporter 2Homo sapiens (human)IC500.00243035
Sodium/myo-inositol cotransporter 2Homo sapiens (human)IC500.380011
Solute carrier family 15 member 1Rattus norvegicus (Norway rat)Ki25.000011
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki7.800011
Solute carrier family 2, facilitated glucose transporter member 2Homo sapiens (human)IC5012.000022
Solute carrier family 2, facilitated glucose transporter member 4 Rattus norvegicus (Norway rat)Ki33.500011
Solute carrier family 22 member 1 Homo sapiens (human)IC501,083.333323
Solute carrier family 22 member 2Homo sapiens (human)IC50882.500012
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki38.320025
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Ki12.300011
Solute carrier family 22 member 8Homo sapiens (human)IC50100.000011
Solute carrier family 5 member 4Homo sapiens (human)IC500.001411
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC5031.150044
Squalene monooxygenase Rattus norvegicus (Norway rat)IC500.480022
Steryl-sulfataseHomo sapiens (human)IC500.800011
Substance-K receptorCavia porcellus (domestic guinea pig)IC5082.600011
Substance-P receptorCavia porcellus (domestic guinea pig)IC5082.600011
Sucrase-isomaltase, intestinalHomo sapiens (human)IC50406.23541213
Sucrase-isomaltase, intestinalRattus norvegicus (Norway rat)IC501.67131515
Telomerase reverse transcriptaseHomo sapiens (human)IC5037.000011
Testosterone 17-beta-dehydrogenase 3Homo sapiens (human)IC50100.500011
Thromboxane-A synthase Homo sapiens (human)IC501.492722
Transcription factor p65Homo sapiens (human)IC5038.000011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC5023.000011
Transient receptor potential cation channel subfamily A member 1Rattus norvegicus (Norway rat)IC5026.000022
Transient receptor potential cation channel subfamily M member 8Rattus norvegicus (Norway rat)IC50147.000022
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC5010.000011
TrehalaseHomo sapiens (human)IC5040.000011
Trehalase Rattus norvegicus (Norway rat)IC5041.666733
Trehalase Sus scrofa (pig)IC5041.000022
Trehalose synthase/amylase TreSMycobacterium tuberculosis CDC1551Ki0.250011
Tyrosine-protein kinase ABL1Homo sapiens (human)IC5010.000011
Tyrosine-protein kinase LckHomo sapiens (human)IC5051.000033
Tyrosine-protein kinase SYKHomo sapiens (human)IC5018.133333
Tyrosine-protein kinase transforming protein FpsFujinami sarcoma virusKi1.800011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5089.875034
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50296.200015
UDP-glucuronosyltransferase 1-6Homo sapiens (human)Ki20.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50296.200015
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50296.200015
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50296.200015
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50296.200015
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC505.000011
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC502.000011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5050,073.550022
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC50100,000.000011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50147.100011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50147.100011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50147.100011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC501.300011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC502.380011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrialHomo sapiens (human)EC500.080011
5'-AMP-activated protein kinase catalytic subunit alpha-2Homo sapiens (human)EC500.016811
5'-AMP-activated protein kinase subunit beta-1Homo sapiens (human)EC500.016811
5'-AMP-activated protein kinase subunit gamma-1Homo sapiens (human)EC500.016811
AlbuminHomo sapiens (human)Kd6.025611
AlbuminRattus norvegicus (Norway rat)Kd7.970011
alkaline phosphatase, germ cell type preproproteinHomo sapiens (human)EC5032.300011
alkaline phosphatase, intestinalHomo sapiens (human)EC50100.000011
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)Kd101.385314
Beta-adrenergic receptor kinase 1Homo sapiens (human)Kd7.400011
CholinesteraseHomo sapiens (human)EC500.002411
Cyclin-dependent kinase 2Homo sapiens (human)Kd100.000011
Dipeptidyl peptidase 4Homo sapiens (human)Kd0.0097410
endoribonuclease toxin MazFEscherichia coli str. K-12 substr. MG1655EC5099.000022
Estrogen receptorRattus norvegicus (Norway rat)EC50150.000012
Estrogen receptor betaRattus norvegicus (Norway rat)EC50150.000012
Free fatty acid receptor 1Homo sapiens (human)EC50812.831011
G-protein coupled receptor 35Homo sapiens (human)EC508.860022
Genome polyprotein Kd4.000011
Mitogen-activated protein kinase 14Homo sapiens (human)EC501.000011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)EC500.665014
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)EC500.665014
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)EC500.665014
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)EC500.665014
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)EC500.665014
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5015.800033
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC506.686733
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC500.90545155
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC500.755034
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Kd0.871011
Potassium channel subfamily K member 2Homo sapiens (human)EC50424.000012
Pyruvate kinase PKMHomo sapiens (human)EC500.000511
serine/threonine-protein kinase 33 isoform aHomo sapiens (human)EC5015.380012
Sodium/glucose cotransporter 1Homo sapiens (human)EC501.697069
Sodium/glucose cotransporter 2Homo sapiens (human)EC500.1407710
Sodium/glucose cotransporter 2Rattus norvegicus (Norway rat)EC500.003022
streptokinase A precursorStreptococcus pyogenes M1 GASEC5077.824522
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC5018.882345
Transient receptor potential cation channel subfamily A member 1Mus musculus (house mouse)EC5061.000011
Transient receptor potential cation channel subfamily A member 1Rattus norvegicus (Norway rat)EC503.600011
Tyrosine-protein kinase SYKHomo sapiens (human)EC5028.000033

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
2-5A-dependent ribonucleaseHomo sapiens (human)Activity30.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)AC5085.000011
ATP-dependent translocase ABCB1Homo sapiens (human)AC5085.000011
Beta-2 adrenergic receptor Bos taurus (cattle)Concentration1,000,000.000011
Beta-2 adrenergic receptor Bos taurus (cattle)KD app4.480011
Breakpoint cluster region proteinHomo sapiens (human)AC5045.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)AC5045.000011
Caspase 6, apoptosis-related cysteine peptidaseHomo sapiens (human)AC500.461011
Caspase-7Homo sapiens (human)AC505.400011
Cell division protein FtsZEscherichia coli K-12INH6.310022
Cell division protein FtsZEscherichia coli K-12Ka1.000011
Cytochrome P450 3A4Homo sapiens (human)Km81.700011
Cytochrome P450 3A5Homo sapiens (human)Km252.000011
dual specificity tyrosine-phosphorylation-regulated kinase 1ARattus norvegicus (Norway rat)AC507.534011
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.733512
fibroblast growth factor 22 isoform 1 precursorHomo sapiens (human)AbsAC1_uM4.370011
glycogen synthase kinase-3 alphaHomo sapiens (human)AC5021.456512
Pancreatic alpha-amylaseSus scrofa (pig)Kii5.870011
Pancreatic alpha-amylaseSus scrofa (pig)Kis31.600011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Fold activation1.120011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Activity3.140022
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Fold activation3.160011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Activity30.000011
Serine/threonine-protein kinase pim-1Homo sapiens (human)-Log IC500.110011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Km147.133313
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Km6.260011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)Activity10.000011
Tyrosine-protein kinase ABL1Homo sapiens (human)AC5045.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km58.000011
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Km11.000011