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prodrug

A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.

ChEBI ID: 50266

Members (140)

MemberDefinitionClass
1,4-butanediolA butanediol that is butane in which one hydrogen of each of the methyl groups is substituted by a hydroxy group. A colourless, water-miscible, viscous liquid at room temperature (m.p. 16degreeC) with a high boiling point (230degreeC), it is mainly used for the production of other organic chemicals, particularly the solvent oxolane (also known as tetrahydrofuran or THF).butane-1,4-diol
2-hydroxyestradiolA 2-hydroxy steroid that consists of 17beta-estradiol having an additional hydroxy group at position 2.2-hydroxy-17beta-estradiol
4-phenylbutyric acidA monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation.4-phenylbutyric acid
4-phenylbutyric acid, sodium saltThe organic sodium salt of 4-phenylbutyric acid. A prodrug for phenylacetate, it is used to treat urea cycle disorders.sodium phenylbutyrate
abiraterone acetateA sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo into abiraterone. Used for treatment of metastatic castrate-resistant prostate cancer.abiraterone acetate
acemetacinA carboxylic ester that is the carboxymethyl ester of indometacin. A non-steroidal anti-inflammatory drug, it is used in the treatment of rheumatoid arthritis, osteoarthritis, and low back pain, as well as for postoperative pain and inflammation. Its activity is due to both acemetacin and its major metabolite, indometacin.acemetacin
adefovir dipivoxilAn organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.adefovir pivoxil
amdinocillin pivoxilA penicillanic acid ester that is the [(2,2-dimethylpropanoyl)oxy]methyl ester and prodrug of mecillinam.pivmecillinam
amifostine anhydrousAn organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy.amifostine
aminolevulinic acidThe simplest delta-amino acid in which the hydrogens at the gamma position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp.5-aminolevulinic acid; 5-ammoniolevulinate
aminolevulinic acid hydrochlorideA hydrochloride that is the monohydrochloride of 5-aminolevulinic acid. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp.5-aminolevulinic acid hydrochloride
amodiaquineA quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.amodiaquine
ampiroxicamA benzothiazine that is the 1-[(ethoxycarbonyl)oxy]ethyl ether of piroxicam. A prodrug for piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.ampiroxicam
amrubicinA synthetic anthracycline antibiotic with molecular formula C25H25NO9. A specific inhibitor of topoisomerase II, it is used (particularly as the hydrochloride salt) in the treatment of cancer, especially lung cancer, where it is a prodrug for the active metabolite, ambrucinol.amrubicin
ancitabineAn organic heterotricyclic compound resulting from the formal condensation of the oxo group of cytidine to the 2' position with loss of water to give the corresponding cyclic ether. A prodrug, it is metabolised to the antineoplastic agent cytarabine, so is used to maintain a more constant antineoplastic action.ancitabine
aripiprazole lauroxilA dodecanoate ester obtained by formal condensation of the carboxy group of dodecanoic acid with the hydroxy group of 7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-3,4-dihydroquinolin-1(2H)-yl]methanol. A prodrug for aripiprazole, it is used for treatment of schizophrenia.aripiprazole lauroxil
azaribineA N-glycosyl-1,2,4-triazine that is 6-azauridine acetylated at positions 2', 3' and 5' on the sugar ring. It is a prodrug for 6-azauridine and is used for treatment of psoriasis.azaribine
azathioprineA thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.azathioprine
azd 1152A dihydrogen phosphate prodrug of a pyrazoloquinazoline aurora kinase inhibitor AZD1152-hydroxyquinazoline pyrazol anilide(HQPA) and is converted rapidly to the active AZD1152-HQPA in plasma.AZT-1152
bacampicillinA penicillanic acid ester that is the 1-ethoxycarbonyloxyethyl ester of ampicillin. It is a semi-synthetic, microbiologically inactive prodrug of ampicillin.bacampicillin
baicalinThe glycosyloxyflavone which is the 7-O-glucuronide of baicalein. It is an active ingredient of Chinese herbal medicine Scutellaria baicalensis.baicalin
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
beclomethasone dipropionateA steroid ester comprising beclomethasone having propionyl groups at the 17- and 21-positions.beclomethasone dipropionate
benazeprilA benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.benazepril
benzoylmetronidazoleA benzoate ester resulting from the formal condensation of benzoic acid with the hydroxy group of metronidazole.metronidazole benzoate
bitolterolThe di-4-toluate ester of (+-)-N-tert-butylnoradrenaline (colterol). A pro-drug for colterol, a beta2-adrenergic receptor agonist, bitolterol is used as its methanesulfonate salt for relief of bronchospasm in conditions such as asthma, chronic bronchitis and emphysema.bitolterol
brl 15572A hydrochloride that is the monohydrochloride salt of 3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol. A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol hydrochloride
brl 428102-Amino-9H-purine in which the hydrogen at position 9 is substituted by a 4-acetoxy-3-(acetoxymethyl)but-1-yl group. A prodrug of the antiviral penciclovir, it is used for the treatment of acute herpes zoster (shingles), for the treatment or suppression of recurrent genital herpes in immunocompetent patients and for the treatment of recurrent mucocutaneous herpes simplex infections in HIV infected patients.famciclovir
capecitabineA carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.capecitabine
carbimazoleA member of the class of imidazoles that is methimazole in which the nitrogen bearing a hydrogen is converted into its ethoxycarbonyl derivative. A prodrug for methimazol, carbimazole is used for the treatment of hyperthyroidism.carbimazole
cefamandole nafateA cephalosporin prodrug having (R)-O-formylmandelamido and N-methylthiotetrazole side-groups.cefamandole nafate
cefditoren pivoxilThe pivaloyloxymethyl ester prodrug of cefditoren.cefditoren pivoxil
cefotiam hexetilThe 1-(cyclohexyloxycarbonyloxy)ethyl ester of cefotiam. It is used as its dihydrochloride salt as a prodrug for cefotiam.cefotiam hexetil ester
cefpodoxime proxetilThe 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.cefpodoxime proxetil
cgs 12066bA maleate salt that is the dimaleate salt of 4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline dimaleate
chlorazepateA 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.clorazepic acid
cilazapril, anhydrousA pyridazinodiazepine resulting from the formal condensation of the carboxy group of cilazaprilat with ethanol. It is a drug used in the treatment of hypertension and heart failure.cilazapril
clorazepate dipotassiumThe compound of monopotassium clorazepate with potassium hydroxide. It is used for the management of anxiety disorders, for the short-term relief of anxiety, as adjunctive therapy in the management of epilepsy, and for the symptomatic relief of acute alcohol withdrawal.dipotassium clorazepate
codeineA morphinane alkaloid found in the opium poppy, Papaver somniferum var. album; has analgesic, anti-tussive and anti-diarrhoeal properties.codeine
cyc 682A nucleoside analogue resulting from the formal condensation of the carboxy group of hexadecanoic acid with the amino group of CNDAC. It is the prodrug of CNDAC and is currently in clinical development for the treatment of acute myeloid leukemia (AML).sapacitabine
dabigatran etexilateAn aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.dabigatran etexilate
dabigatran etexilateAn aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.dabigatran etexilate
dacarbazineA monocarboxylic acid amide that is 1H-imidazole-4-carboxamide which is substituted at position 5 by a 3,3-dimethyltriaz-1-en-1-yl group. It is used for the treatment of metastatic malignant melanoma, and in combination with other drugs for the treatment of Hodgkin's disease and soft-tissue sarcoma.dacarbazine
dextromethorphanA 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.dextromethorphan
diloxanide furoateA carboxylic ester resulting from the formal condensation of the carboxy group of furan-2-carboxylic acid with the hydroxy group of 2,2-dichloro-N-(4-hydroxyphenyl)-N-methylacetamide. It is a drug used for the treatment of asymptomatic amebiasis.diloxanide furoate
dipivefrinThe dipivalate ester of (+-)-epinephrine (racepinephrine). A pro-drug of epinephrine, the hydrochloride is used topically as eye drops to reduce intra-ocular pressure in the treatment of open-angle glaucoma or ocular hypertension.dipivefrin
dipyroneA pyrazole that is antiipyrine substituted at C-4 by a methyl(sulfomethyl)amino group, the sodium salt of which, metamizole sodium, was widely used as a powerful analgesic and antipyretic, but withdrawn from many markets from the 1970s due to a risk of causing risk of causing agranulocytosis.metamizole
dipyroneAn organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic.metamizole sodium
dirithromycinThe hemi-aminal resulting from the condensation of the erythromycin derivative (9S)-erythromycyclamine with 2-(2-methoxyethoxy)acetaldehyde. As the oxazine ring containing the hemi-aminal group is unstable under both acidic and alkaline conditions, dirithromycin functions as a more lipid-soluble prodrug for (9S)-erythromycyclamine. Administered as enteric coated tablets to protect it from acid catalysed hydrolysis in the stomach, it is used to treat respiratory tract, skin, and soft tissue infections caused by susceptible organisms.dirithromycin
doxifluridineA pyrimidine 5'-deoxyribonucleoside that is 5-fluorouridine in which the hydroxy group at the 5' position is replaced by a hydrogen. It is an oral prodrug of the antineoplastic agent 5-fluorouracil. Designed to circumvent the rapid degradation of 5-fluorouracil by dihydropyrimidine dehydrogenase in the gut wall, it is converted into 5-fluorouracil in the presence of pyrimidine nucleoside phosphorylase.doxifluridine
droxicamAn organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.droxicam
droxidopaA serine derivative that is L-serine substituted at the beta-position by a 3,4-dihydroxyphenyl group. A prodrug for noradrenalone, it is used for treatment of neurogenic orthostatic hypotensiondroxidopa
enalaprilA dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).enalapril
enalapril maleateThe maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.enalapril maleate
etanidazoleA monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitro-1H-imidazol-1-yl)acetic acid with the amino group of ethanolamine. Used as a radiosensitising agent for hypoxic tumour cells.etanidazole
etc-1002An alpha,omega-dicarboxylic acid that is pentadecanedioic acid which is substituted by methyl groups groups at positions 2 and 14, and by a hydroxy group at position 8. It is a drug used for the treatment of high LDL cholesterol, which is sometimes referred to as 'bad cholesterol'.bempedoic acid
ethionamideA thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.ethionamide
fingolimodAn aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.fingolimod
fingolimod hydrochlorideThe hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod).fingolimod hydrochloride
flucytosineAn organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.flucytosine
fludarabine phosphateA purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas.fludarabine phosphate
fluphenazine depotThe prodrug of fluphenazine, an antipsychotic drug used for the symptomatic management of psychosis in patients with schizophrenia.fluphenazine decanoate
fluticasone furoateA trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a 2-furoyl substituent at position 17. Used in combination with vilanterol trifenate for treatment of bronchospasm associated with chronic obstructive pulmonary disease.fluticasone furoate
fosamprenavirA sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir.fosamprenavir
fosaprepitantA morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid.fosaprepitant
fosfluconazoleFosfluconazole
gemcitabineA 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.gemcitabine
gs-7340An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection.tenofovir alafenamide
heroinA morphinane alkaloid that is morphine bearing two acetyl substituents on the O-3 and O-6 positions. As with other opioids, heroin is used as both an analgesic and a recreational drug. Frequent and regular administration is associated with tolerance and physical dependence, which may develop into addiction. Its use includes treatment for acute pain, such as in severe physical trauma, myocardial infarction, post-surgical pain, and chronic pain, including end-stage cancer and other terminal illnesses.heroin
imidaprilA member of the class of imidazolidines that is (4S)-1-methyl-2-oxoimidazolidine-4-carboxylic acid in which the hydrogen of the imidazolidine nitrogen has been substituted by (1S)-1-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}ethyl group. It is the prodrug for imidaprilat, an ACE inhibitor used for the treatment of chronic heart failure.imidapril
irinotecanA member of the class of pyranoindolizinoquinolines that is the carbamate ester obtained by formal condensation of the carboxy group of [1,4'-bipiperidine]-1'-carboxylic acid with the phenolic hydroxy group of (4S)-4,11-diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2- hydrochloride]quinoline-3,14-dione. Used (in the form of its hydrochloride salt trihydrate) in combination with fluorouracil and leucovorin, for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy. It is converted via hydrolysis of the carbamate linkage to its active metabolite, SN-38, which is ~1000 times more active.irinotecan
irinotecan hydrochlorideA hydrochloride obtained by combining irinotecan with one molar equivalent of hydrochloric acid. Used (in the form of its trihydrate) in combination with fluorouracil and leucovorin, for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy. It is converted via hydrolysis of the carbamate linkage to its active metabolite, SN-38, which is ~1000 times more active.irinotecan hydrochloride (anhydrous)
jte 607The dihydrochloride salt of JTE-607. It is a cytokine inhibitor which suppresses the production of proinflammatory cytokines such as interleukin (IL-1beta), IL-6, IL-8, granulocyte macrophage colony stimulating factor (GM-CSF), and tumor necrosis factor (TNF-alpha). It acts as a pro-drug which is cleaved by carboxylesterase 1 (CES1) to its active free acid form, which then binds to cleavage and polyadenylation specificity factor 3 (CPSF3).JTE-607 dihydrochloride
lamivudineA monothioacetal that consists of cytosine having a (2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl moiety attached at position 1. An inhibitor of HIV-1 reverse transcriptase, it is used as an antiviral in the treatment of AIDS and hepatitis B.lamivudine
latanoprostA prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.latanoprost
leflunomideA monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.leflunomide
lenampicillinA penicillanic acid ester that is the (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester of ampicillin. It is a prodrug of ampicillin.lenampicillin
levodopaAn optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's diseaseL-dopa zwitterion; L-dopa
lovastatinA fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).lovastatin
loxoprofenA monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration.loxoprofen
lucanthoneA thioxanthen-9-one compound having a methyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. Formerly used for the treatment of schistosomiasis. It is a prodrug, being metabolised to hycanthone.lucanthone
mestranolA terminal acetylenic compound that is (17alpha)-17-ethynylestra-1(10),2,4-triene substituted by a methoxy group at position 3 and a hydroxy group at position 17.mestranol
methyl 5-aminolevulinateThe methyl ester of 5-aminolevulinic acid. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells.methyl 5-aminolevulinate
methyl 5-aminolevulinate hydrochlorideThe hydrochloride salt of methyl 5-aminolevulinate. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells.methyl 5-aminolevulinate hydrochloride
methylprednisolone suleptanateAn organic sodium salt that is the monosodium salt of methylprednisolone 21-suleptanic acid ester. It is a prodrug of methylprednisolone developed by Pharmacia Corp for the treatment of asthma.methylprednisolone suleptanate
metronidazoleA member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.metronidazole
midodrineAn aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.midodrine
ML-210An N-acylpiperazine that is piperazine substituted by 5-methyl-4-nitro-1,2-oxazole-3-carbonyl and bis(4-chlorophenyl)methyl groups at positions 1 and 4, respectively. It is a glutathione peroxidase 4 (GPX4) inhibitor which induces ferroptosis in cancer cells expressing the RAS oncogene.ML-210
molnupiravirA nucleoside analogue that is N(4)-hydroxycytidine in which the 5'-hydroxy group is replaced by a (2-methylpropanoyl)oxy group. It is the prodrug of the active antiviral ribonucleoside analog N(4)-hydroxycytidine (EIDD-1931), has activity against a number of RNA viruses including SARS-CoV-2, MERS-CoV, and seasonal and pandemic influenza viruses. It is currently in phase III trials for the treatment of patients with COVID-19.molnupiravir
mycophenolate mofetilA carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.mycophenolate mofetil
N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromideA hydrobromide salt prepared from N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonising the behavioral effects of cocaine.N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide
nabumetoneA methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.nabumetone
naproxen-n-butyl nitrateA carboxylic ester obtained by formal condensation of the carboxy group of naproxen with the hydroxy group of 4-(nitrooxy)butanol. A cyclooxygenase-inhibiting nitric oxide donator that is metabolised to naproxen and a nitric oxide donating moiety, effective in treatment of osteoarthritis.naproxcinod
nelarabineA purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G).nelarabine
nepafenacA monocarboxylic acid amide that is amfenac in which the carboxylic acid group has been converted into the corresponding carboxamide. It is a prodrug for amfenac, used in eye drops to treat pain and inflammation following cataract surgery.nepafenac
nitroglycerinA nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.nitroglycerin
olsalazineAn azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease.olsalazine
oseltamivirA cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.oseltamivir
parecoxibAn N-acylsulfonamide resulting from the formal condensation of valdecoxib with propionic acid. It is a prodrug for valdecoxib.parecoxib
penamecillinA penicillanic acid ester that is the acetoxymethyl ester of benzylpenicillin. It is a prodrug for benzylpenicillin.penamecillin
PF-07304814An indolecarboxamide resulting from the formal condensation of the carboxy group of 4-methoxy-1H-indole-2-carboxylic acid with the primary amino group of N-[(2S)-3-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]-4-(phosphonooxy)butan-2-yl]-L-leucinamide. It is the phosphate prodrug of PF-00835231, an anticoronaviral agent.PF-07304814
pivampicillinA penicillanic acid ester that is the pivaloyloxymethyl ester of ampicillin. It is a prodrug of ampicillin.pivampicillin
pn 401An acetate ester that is uracil in which the three hydroxy hydrogens are replaced by acetate group. A prodrug for uridine, it is used for the treatment of hereditary orotic aciduria and for management of fluorouracil toxicity.uridine triacetate
ppi-0903A cephalosporin having [4-(1-methylpyridinium-4-yl)-1,3-thiazol-2-yl]sulfanyl and {(2Z)-2-(ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl}amino side groups located at positions 3 and 7 respectively. The N-phospho prodrug of ceftaroline, a broad-spectrum antibiotic active against methicillin-resistant Staphylococcus aureus (MRSA). It is used for the treatment of adults with acute bacterial skin and skin structure infections.ceftaroline fosamil
prednisolone phosphateA synthetic glucocorticoid resulting from the formal condensation of the 21-hydroxy group of prednisolone with one of the hydroxy groups of phosphoric acid. It is a prodrug for prednisolone that is activated in vivo by phosphatases.prednisolone phosphate
prednisoneA synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.prednisone
proglumetacinA carboxylic ester obtained by formal condensation of the carboxy group of indometacin with the hydroxy group of 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl N(2)-benzoyl-N,N-dipropyl-alpha-glutaminate. Used (as its dimaleate salt) to control pain and inflammation associated with musculoskeletal and joint disorders. Following oral administration, it is metabolised to indometacin and proglumide, a drug with antisecretory effects that helps prevent injury to the stomach lining.proglumetacin
psilocybinA tryptamine alkaloid that is N,N-dimethyltryptamine carrying an additional phosphoryloxy substituent at position 4. The major hallucinogenic alkaloid isolated from Psilocybe mushrooms (also known as Teonanacatl or "magic mushrooms").psilocybin
pyrazinamideA monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.pyrazinecarboxamide
quinaprilA member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.quinapril
ramiprilA dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.ramipril
rubitecanA pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.rubitecan
rx-3117A triol that is (1S,2R)-4-fluoro-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol which is substituted by a 4-amino-2-oxopyrimidin-1(2H)-yl group at position 5. It is a cytidine analog which exhibits anticancer activity in several cancers, including gemcitabine-resistant tumours.roducitabine
s 8932A carboxylic ester resulting from the formal condensation of the carboxy group of N-[(S)-{[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl]methoxy}(phenoxy)phosphoryl]-L-alanine with the hydroxy group of 2-ethylbutan-1-ol. A broad-spectrum antiviral prodrug with potent in vitro antiviral activity against a diverse panel of RNA viruses such as Ebola virus, MERS-CoV and SARS-CoV. It is currently in Phase III clinical trials for the treatment of Covid-19 in adults.remdesivir
salicinAn aryl beta-D-glucoside that is salicyl alcohol in which the phenolic hydrogen has been replaced by a beta-D-glucosyl residue.salicin
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
selexipagA member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid).selexipag
simvastatinA member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.simvastatin
sk&f 77434A hydrobromide salt prepared from N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide
sofosbuvirA nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.sofosbuvir
spiraprilspirapril
sulindacA monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.sulindac
suxibuzoneA pyrazolidine that is phenylbutazone which is substituted by a 3-carboxypropanoylmethyl group at the 4-position. Suxibuzone is a prodrug for phenylbutazone and is commonly used as an anti-inflammatory drug in horses.suxibuzone
tak 491A carboxylic ester obtained by formal condensation of the carboxy group of azilsartan with the hydroxy group of 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one. A prodrug for azilsartan, it is used for treatment of hypertension.azilsartan medoxomil
talampicillinA penicillanic acid ester that is the 1-phthalidyl ester of ampicillin. It is a prodrug of ampicillin.talampicillin
tazaroteneThe ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.tazarotene
tedizolid phosphateA phosphate monoester resulting from the formal condensation of equimolar amounts of phosphoric acid with the hydroxy group of tedizolid . It is a prodrug of tedizolid, used for the treatment of acute bacterial skin infections caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species, and Enterococcus faecalis.tedizolid phosphate
temozolomideAn imidazotetrazine that is 3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine which is substituted at positions 3, 4, and 8 by methyl, oxo, and carboxamide groups, respectively. A prodrug for MTIC (5-(3-methyltriaz-1-en-1-yl)-1H-imidazole-4-carboxamide, formed by spontaneous hydrolysis of temozolomide in the body), it is used as an oral alkylating agent for the treatment of newly diagnosed malignant glioblastoma multiforme (concomitantly with radiotherapy) and malignant melanoma.temozolomide
tenofovir disoproxil fumarateA fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.tenofovir disoproxil fumarate
tiazofurinA C-glycosyl compound that is 1,3-thiazole-4-carboxamide in which the hydrogen at position 2 has been replaced by a beta-D-ribofuranosyl group. It is metabolised to thiazole-4-carboxamide adenine dinucleotide (TAD), a selective inhibitor of inosine monophosphate dehydrogenase (IMP dehydrogenase).tiazofurine
trandolaprilA heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.trandolapril
travoprostThe isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.travoprost
tributyrinA triglyceride obtained by formal acylation of the three hydroxy groups of glycerol by butyric acid.tributyrin
uf 021The isopropyl ester of unoprostone.isopropyl unoprostone
uracilA common and naturally occurring pyrimidine nucleobase in which the pyrimidine ring is substituted with two oxo groups at positions 2 and 4. Found in RNA, it base pairs with adenine and replaces thymine during DNA transcription.uracil
valganciclovirThe L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine.valganciclovir
varespladib methylA methyl ester resulting from the formal condensation of the carboxy group of varespladib with methanol. It is a potential therapy for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s.varespladib methyl
ximelagatranA member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.ximelagatran (hydroxylamine form); ximelagatran
zofenoprilA proline derivative that is 4-(phenylsulfanyl)-L-proline in which the amine proton is replaced by a (2S)-3-(benzoylsulfanyl)-2-methylpropanoyl group. A prodrug for zofenoprilat.zofenopril

Research

Studies (219,463)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199054,926 (25.03)18.7374
1990's33,250 (15.15)18.2507
2000's51,479 (23.46)29.6817
2010's59,491 (27.11)24.3611
2020's20,317 (9.26)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials38,123 (15.50%)5.53%
Reviews22,549 (9.17%)6.00%
Case Studies34,632 (14.08%)4.05%
Observational1,447 (0.59%)0.25%
Other149,206 (60.66%)84.16%

Protein Targets (816)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency22.784613
15-lipoxygenase, partialHomo sapiens (human)Potency27.285414
67.9K proteinVaccinia virusPotency19.995025
acetylcholinesteraseHomo sapiens (human)Potency31.9855421
activating transcription factor 6Homo sapiens (human)Potency27.931529
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.295819
alpha-galactosidaseHomo sapiens (human)Potency39.074323
Alpha-synucleinHomo sapiens (human)Potency31.622811
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency13.157013
AR proteinHomo sapiens (human)Potency14.475512164
aryl hydrocarbon receptorHomo sapiens (human)Potency16.3346220
arylsulfatase AHomo sapiens (human)Potency15.059518
ATAD5 protein, partialHomo sapiens (human)Potency12.176348
Ataxin-2Homo sapiens (human)Potency7.9476210
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency10.796458
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency7.1297214
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency23.934111
beta-2 adrenergic receptorHomo sapiens (human)Potency25.920712
Bloom syndrome protein isoform 1Homo sapiens (human)Potency44.9789313
BRCA1Homo sapiens (human)Potency10.000011
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency65.380216
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency26.629716
caspase-3Cricetulus griseus (Chinese hamster)Potency33.491511
caspase-3Homo sapiens (human)Potency26.629716
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency21.3866341
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency9.379227
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency23.0837117
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency12.589311
Chain A, Beta-lactamaseEscherichia coli K-12Potency19.6744217
Chain A, CruzipainTrypanosoma cruziPotency24.349315
Chain A, Ferritin light chainEquus caballus (horse)Potency25.009414
Chain A, HADH2 proteinHomo sapiens (human)Potency18.365826
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency31.909414
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.3187111
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency12.853824
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency21.924316
Chain B, HADH2 proteinHomo sapiens (human)Potency18.365826
chromobox protein homolog 1Homo sapiens (human)Potency71.9751216
cytochrome P450 2C19 precursorHomo sapiens (human)Potency13.910016
cytochrome P450 2C9 precursorHomo sapiens (human)Potency22.106012
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.8416120
cytochrome P450 2D6Homo sapiens (human)Potency19.0476116
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency2.511911
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.5948218
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.3936230
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency9.6133122
D(3) dopamine receptor isoform eHomo sapiens (human)Potency35.481311
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency5.313812
DNA polymerase betaHomo sapiens (human)Potency32.667212
DNA polymerase eta isoform 1Homo sapiens (human)Potency19.595722
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency58.853029
DNA polymerase kappa isoform 1Homo sapiens (human)Potency12.639715
dopamine D1 receptorHomo sapiens (human)Potency4.104412
endonuclease IVEscherichia coliPotency20.362024
Endothelin receptor type BRattus norvegicus (Norway rat)Potency9.172612
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency9.172612
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.687910168
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency16.7617323
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency17.602810131
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.1382121
EWS/FLI fusion proteinHomo sapiens (human)Potency12.7445450
farnesoid X nuclear receptorHomo sapiens (human)Potency24.2020320
flap endonuclease 1Homo sapiens (human)Potency30.813736
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency63.095711
Fumarate hydrataseHomo sapiens (human)Potency20.7327110
GVesicular stomatitis virusPotency15.8416120
GABA theta subunitRattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.594819
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.594819
gemininHomo sapiens (human)Potency7.4931449
GLI family zinc finger 3Homo sapiens (human)Potency18.4408347
glp-1 receptor, partialHomo sapiens (human)Potency16.025416
GLS proteinHomo sapiens (human)Potency21.039128
glucocerebrosidaseHomo sapiens (human)Potency11.841913
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency17.1820545
glucokinase regulatory proteinHomo sapiens (human)Potency5.011911
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency15.6139113
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency8.590012
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.464212
heat shock protein beta-1Homo sapiens (human)Potency39.9816214
hemoglobin subunit betaHomo sapiens (human)Potency1.937758
hexokinase-4 isoform 1Homo sapiens (human)Potency5.011911
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency20.8053210
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.446618
histone deacetylase 9 isoform 3Homo sapiens (human)Potency7.511027
Histone H2A.xCricetulus griseus (Chinese hamster)Potency35.3863216
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency35.481515
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.8416120
huntingtin isoform 2Homo sapiens (human)Potency10.435334
hypothetical protein, conservedTrypanosoma bruceiPotency12.086934
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency45.217729
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency13.2258314
IDH1Homo sapiens (human)Potency14.934219
importin subunit beta-1 isoform 1Homo sapiens (human)Potency24.471423
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.8416140
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency11.220211
Integrin alpha-IIbHomo sapiens (human)Potency12.924412
Integrin beta-3Homo sapiens (human)Potency12.924412
Interferon betaHomo sapiens (human)Potency18.6599340
interleukin 8Homo sapiens (human)Potency66.824211
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency42.800012
lamin isoform A-delta10Homo sapiens (human)Potency6.7904229
LuciferasePhotinus pyralis (common eastern firefly)Potency21.8797313
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency18.800723
M-phase phosphoprotein 8Homo sapiens (human)Potency26.287016
Microtubule-associated protein tauHomo sapiens (human)Potency23.1845214
mitogen-activated protein kinase 1Homo sapiens (human)Potency14.352326
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency9.411027
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency30.465317
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.592413
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency14.705914
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency1.738813
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency25.7719354
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency11.9530110
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency29.8139210
Nuclear receptor ROR-gammaHomo sapiens (human)Potency12.748714
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.7854211
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency10.576818
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.3849351
P53Homo sapiens (human)Potency56.234112
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency119.047012
ParkinHomo sapiens (human)Potency16.112523
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency68.830323
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency8.3783223
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency55.806217
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency25.9819424
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency19.6287522
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency12.173933
phosphopantetheinyl transferaseBacillus subtilisPotency62.1753316
PINK1Homo sapiens (human)Potency23.350712
plasminogen precursorMus musculus (house mouse)Potency4.9206110
polyproteinZika virusPotency20.7327110
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency12.589311
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency18.854112
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency12.084915
PPM1D proteinHomo sapiens (human)Potency20.6453110
pregnane X nuclear receptorHomo sapiens (human)Potency23.8803325
pregnane X receptorRattus norvegicus (Norway rat)Potency47.393612
progesterone receptorHomo sapiens (human)Potency21.7866318
pyruvate kinaseLeishmania mexicana mexicanaPotency13.731257
pyruvate kinase PKM isoform aHomo sapiens (human)Potency24.028325
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency125.892011
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency24.961813
RAR-related orphan receptor gammaMus musculus (house mouse)Potency12.6689251
ras-related protein Rab-9AHomo sapiens (human)Potency2.817814
regulator of G-protein signaling 4Homo sapiens (human)Potency26.160513
relaxin receptor 1 isoform 1Homo sapiens (human)Potency17.782811
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency22.5552348
retinoid X nuclear receptor alphaHomo sapiens (human)Potency15.1848331
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency1.558622
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency27.749214
SMAD family member 2Homo sapiens (human)Potency28.0900317
SMAD family member 3Homo sapiens (human)Potency28.0900317
Smad3Homo sapiens (human)Potency10.572218
snurportin-1Homo sapiens (human)Potency24.471423
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency14.5874228
survival motor neuron protein isoform dHomo sapiens (human)Potency10.1845216
TAR DNA-binding protein 43Homo sapiens (human)Potency24.060216
TDP1 proteinHomo sapiens (human)Potency13.1942272
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.059816
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.3211419
ThrombopoietinHomo sapiens (human)Potency7.943322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.0521355
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency90.267525
thyroid stimulating hormone receptorHomo sapiens (human)Potency18.1725622
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency41.377822
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency44.668411
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency31.622811
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency20.749111
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency4.9206110
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency4.9206110
USP1 protein, partialHomo sapiens (human)Potency37.0706214
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency28.7300220
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency17.8408418
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency65.074916
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency15.6139113
WRNHomo sapiens (human)Potency5.497922

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC502.57681618
3-hydroxy-3-methylglutaryl-coenzyme A reductaseSchizosaccharomyces pombe 972h-IC5095.200011
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)Ki34.001322
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)IC500.04591112
5-hydroxytryptamine receptor 7Homo sapiens (human)IC50200.000011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50100.000011
AcetylcholinesteraseHomo sapiens (human)IC5020.365455
AcetylcholinesteraseRattus norvegicus (Norway rat)IC5030.000011
AcetylcholinesteraseHomo sapiens (human)Ki0.050511
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.026411
Acyl-CoA desaturase 1Mus musculus (house mouse)IC500.008011
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC5016.800011
Adenosine receptor A1Homo sapiens (human)IC5026.720011
Adenosine receptor A1Homo sapiens (human)Ki15.586011
Adenylate cyclase type 10Homo sapiens (human)IC503.000011
AlbuminHomo sapiens (human)Ki26,302,700,000.000011
Alcohol dehydrogenase E chainEquus caballus (horse)Ki10,000.000011
Alcohol dehydrogenase S chainEquus caballus (horse)Ki10,000.000011
Aldo-keto reductase family 1 member B1Bos taurus (cattle)IC500.293011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC502.690011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC504.158314
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki4.123714
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC502.690011
Alpha-2C adrenergic receptorHomo sapiens (human)IC503.171011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.461011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5010.847012
Amyloid-beta precursor proteinHomo sapiens (human)IC504.700022
Androgen receptorRattus norvegicus (Norway rat)IC5012.809334
Androgen receptorRattus norvegicus (Norway rat)Ki13.615512
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC501.006149
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC500.069633
Angiotensin-converting enzyme Homo sapiens (human)IC500.6569920
Angiotensin-converting enzyme 2 Homo sapiens (human)IC500.074212
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50128.2769126
ATP-dependent translocase ABCB1Homo sapiens (human)IC50154.3636611
Aurora kinase AHomo sapiens (human)IC500.326835
Aurora kinase AHomo sapiens (human)Ki1.368011
Aurora kinase BHomo sapiens (human)IC501.775157
Aurora kinase BHomo sapiens (human)Ki0.000411
Aurora kinase CHomo sapiens (human)IC500.062724
bcl-2-related protein A1Mus musculus (house mouse)IC50100.000022
Bile salt export pumpHomo sapiens (human)IC50222.9898644
Bile salt export pumpRattus norvegicus (Norway rat)IC50399.700013
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50125.4792224
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Ki7.950011
Cannabinoid receptor 1Homo sapiens (human)IC5028.540011
Cannabinoid receptor 1Homo sapiens (human)Ki22.532011
Capsid protein Hepatitis B virusIC5050.050022
Carbonic anhydrase 1Homo sapiens (human)IC50375.500012
Carbonic anhydrase 1Homo sapiens (human)Ki30.000022
Carbonic anhydrase 12Homo sapiens (human)Ki50.000011
Carbonic anhydrase 2Homo sapiens (human)IC50375.500012
Carbonic anhydrase 2Homo sapiens (human)Ki30.000022
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.130911
Carbonic anhydrase 9Homo sapiens (human)Ki50.000011
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC500.003011
Cereblon isoform 4Magnetospirillum gryphiswaldenseKi24.500022
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.026411
Chain A, Antigen Cd11a (p180)Homo sapiens (human)IC502.400011
Chain A, DEOXYNUCLEOSIDE KINASEDrosophila melanogaster (fruit fly)IC500.760011
Chain A, Histamine N-methyltransferaseHomo sapiens (human)Ki0.018614
Chain A, Uracil-DNA GlycosylaseThermus thermophilusKi0.088011
CholinesteraseEquus caballus (horse)IC500.119311
CholinesteraseHomo sapiens (human)IC500.003344
Cyclin-dependent kinase 1Homo sapiens (human)IC5014.360011
Cystathionine gamma-lyaseHomo sapiens (human)IC50200.000011
Cytochrome P450 1A2Homo sapiens (human)IC5035.166723
Cytochrome P450 2C9 Homo sapiens (human)IC5036.996723
Cytochrome P450 2D1Rattus norvegicus (Norway rat)IC50792.000012
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC50121.800012
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC502,053.800012
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC501,176.000012
Cytochrome P450 2D6Homo sapiens (human)IC5050.542679
Cytochrome P450 2J2Homo sapiens (human)IC5025.495012
Cytochrome P450 3A4Homo sapiens (human)IC508.400011
Cytochrome P450 3A4Homo sapiens (human)Ki24.000011
D(1A) dopamine receptorHomo sapiens (human)Ki0.001211
D(3) dopamine receptorHomo sapiens (human)IC501.929011
D(3) dopamine receptorHomo sapiens (human)Ki0.655011
Delta-type opioid receptorHomo sapiens (human)IC509.300011
Delta-type opioid receptorMus musculus (house mouse)IC5010.000013
Delta-type opioid receptorHomo sapiens (human)Ki52.207011
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC507.933333
Dihydroorotate dehydrogenase (quinone), mitochondrialMus musculus (house mouse)IC500.030011
Dihydroorotate dehydrogenase (quinone), mitochondrialRattus norvegicus (Norway rat)IC500.009011
Dipeptidyl peptidase 4Homo sapiens (human)IC50225.000011
Disabled homolog 2-interacting proteinHomo sapiens (human)Ki1.260011
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)IC505.000022
Epidermal growth factor receptorHomo sapiens (human)IC50304.293333
Equilibrative nucleoside transporter 1Homo sapiens (human)IC500.190011
Estrogen receptorHomo sapiens (human)IC502.509022
Estrogen receptorHomo sapiens (human)Ki0.005211
Estrogen receptor 1Homo sapiens (human)IC5050.000011
Estrogen receptor betaHomo sapiens (human)IC505.000011
G2/mitotic-specific cyclin-B1Homo sapiens (human)IC5014.360011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki77.624711
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)IC5012.900011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki77.624711
Glucocorticoid receptorHomo sapiens (human)IC500.382333
Glucocorticoid receptorHomo sapiens (human)Ki0.260822
glucose-6-phosphate 1-dehydrogenase isoform bHomo sapiens (human)IC5072.500011
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonasePlasmodium bergheiIC5027.966733
Glutamate dehydrogenase 1, mitochondrial Bos taurus (cattle)Ki10,000.000011
Glutamate receptor 1Homo sapiens (human)Ki790.000011
Glutamate receptor 2Homo sapiens (human)Ki790.000011
Glutamate receptor 3Homo sapiens (human)Ki790.000011
Glutamate receptor 4Homo sapiens (human)Ki790.000011
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki790.000011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki2.246011
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki1.680011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki2.246011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.146011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.521011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.146011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.521011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.146011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.521011
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC501.146011
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki0.521011
Histone deacetylase 1Homo sapiens (human)IC5079.303733
Histone deacetylase 1Homo sapiens (human)Ki4.570012
Histone deacetylase 11 Homo sapiens (human)Ki4.570012
Histone deacetylase 2Homo sapiens (human)IC5045.466522
Histone deacetylase 2Homo sapiens (human)Ki4.570012
Histone deacetylase 3Homo sapiens (human)IC50260.000011
Histone deacetylase 3Homo sapiens (human)Ki4.570012
Histone deacetylase 4Homo sapiens (human)IC502,000.000011
Histone deacetylase 4Homo sapiens (human)Ki4.570012
Histone deacetylase 5Homo sapiens (human)IC502,000.000011
Histone deacetylase 5Homo sapiens (human)Ki4.570012
Histone deacetylase 6Homo sapiens (human)IC50128.142522
Histone deacetylase 6Homo sapiens (human)Ki4.570012
Histone deacetylase 7Homo sapiens (human)IC502,000.000011
Histone deacetylase 7Homo sapiens (human)Ki4.570012
Histone deacetylase 8Homo sapiens (human)IC5093.000011
Histone deacetylase 8Homo sapiens (human)Ki4.570012
Histone deacetylase 9Homo sapiens (human)IC502,000.000011
Histone deacetylase 9Homo sapiens (human)Ki4.570012
Insulin receptor Rattus norvegicus (Norway rat)IC500.011712
integrase, partialHuman immunodeficiency virus 1IC500.593922
Integrin alpha-LHomo sapiens (human)IC503.090022
Integrin beta-2Homo sapiens (human)IC503.090022
Intercellular adhesion molecule 1Homo sapiens (human)IC503.780011
Interstitial collagenaseHomo sapiens (human)IC506.060011
Kappa-type opioid receptorHomo sapiens (human)IC5015.000011
Kappa-type opioid receptorMus musculus (house mouse)IC5010.000013
Kappa-type opioid receptorHomo sapiens (human)Ki25.411011
LactoperoxidaseHomo sapiens (human)IC5010.400011
Lactoylglutathione lyaseHomo sapiens (human)Ki69.700024
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50200.000012
Large neutral amino acids transporter small subunit 1Homo sapiens (human)IC50100.000011
large T antigenBetapolyomavirus macacaeIC50100.000011
lens epithelium-derived growth factor p75Homo sapiens (human)IC500.593922
Lysine-specific histone demethylase 1AHomo sapiens (human)IC503.190033
Metabotropic glutamate receptor 3Rattus norvegicus (Norway rat)Ki10,000.000012
Mineralocorticoid receptor Homo sapiens (human)IC500.166011
Mu-type opioid receptorHomo sapiens (human)IC500.105011
Mu-type opioid receptorMus musculus (house mouse)IC5010.000013
Mu-type opioid receptorHomo sapiens (human)Ki3.513522
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50128.575034
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5043.250022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50123.8885126
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki10.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC501.556011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.217011
NAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)IC50416.900011
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC50100.000011
NeuraminidaseInfluenza A virus (A/Aichi/2/1968(H3N2))IC500.001611
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))IC501.134466
NeuraminidaseInfluenza A virus (A/Singapore/1/1957(H2N2))IC500.003012
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC5027.176044
NeuraminidaseInfluenza B virus (B/Lee/1940)IC500.005011
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki12.100011
NeuraminidaseInfluenza B virus (B/Lee/1940)Ki0.001111
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))IC500.004322
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))IC502.031733
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))IC500.000222
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))IC500.110422
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))IC5013.00768283
Neuraminidase Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))Ki0.004911
Neuraminidase Influenza A virus (A/duck/Laos/25/2006(H5N1))Ki0.001111
Neuraminidase Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))Ki0.000111
Neuraminidase Influenza A virus (A/Turkey/651242/2006(H5N1))Ki0.007911
Neuraminidase Influenza A virus (A/Wilson-Smith/1933(H1N1))Ki0.000522
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC5011.050011
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC5011.050011
Neutrophil elastaseHomo sapiens (human)IC500.027011
NS5 Zika virusIC501.360011
Nuclear receptor subfamily 4 group A member 2Homo sapiens (human)IC5013.400011
photoreceptor-specific nuclear receptorHomo sapiens (human)IC501.164011
polyadenylate-binding protein 1Homo sapiens (human)IC5054.725022
Polyamine deacetylase HDAC10Homo sapiens (human)Ki4.570012
Polyphenol oxidase 2Agaricus bisporusIC504.000011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50100.000011
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.258011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50301.995011
Progesterone receptorHomo sapiens (human)IC500.021011
Prolyl endopeptidaseHomo sapiens (human)IC5012.150022
Prostacyclin receptorHomo sapiens (human)IC500.062011
Prostaglandin E synthaseHomo sapiens (human)IC5080.000011
Prostaglandin G/H synthase 1Homo sapiens (human)IC50100.000011
Prostaglandin G/H synthase 1Ovis aries (sheep)IC5016.000011
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50100.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC5021.765745
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50100.000011
Protein cereblonHomo sapiens (human)IC50707.500012
Protein cereblonHomo sapiens (human)Ki212.000011
Protein-arginine deiminase type-4Homo sapiens (human)IC505,250.000012
ProthrombinHomo sapiens (human)Ki0.002011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC505.7011811
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC506.410011
Retinoic acid receptor RXR-alphaHomo sapiens (human)IC5082.900011
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC503.610011
SialidaseClostridium perfringensIC5061.100011
Sialidase-1Homo sapiens (human)IC503,666.666733
Sialidase-2Homo sapiens (human)IC502,333.333333
Sialidase-3Homo sapiens (human)IC505,250.000044
Sialidase-4Homo sapiens (human)IC503,666.666733
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC500.098733
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.036522
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.348011
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki5.070011
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium-dependent dopamine transporter Homo sapiens (human)IC506.494012
Sodium-dependent dopamine transporter Homo sapiens (human)Ki5.159512
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC504.158214
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki4.123714
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.021912
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.011712
Solute carrier family 15 member 1Homo sapiens (human)IC5053,566.666723
Solute carrier family 15 member 1Homo sapiens (human)Ki790.000011
Solute carrier family 15 member 1Rattus norvegicus (Norway rat)Ki3,250.000022
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki230.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC5070.437534
Solute carrier family 22 member 2Homo sapiens (human)IC502.700011
Solute carrier family 22 member 3Homo sapiens (human)IC5074.600011
Solute carrier family 22 member 6Homo sapiens (human)IC5013.500011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC5011.820045
Solute carrier organic anion transporter family member 2A1Homo sapiens (human)Ki10.000011
Sphingosine 1-phosphate receptor 1Homo sapiens (human)IC500.721922
Sphingosine 1-phosphate receptor 2Homo sapiens (human)IC5010.000011
Sphingosine 1-phosphate receptor 3Homo sapiens (human)IC5010.000011
Sphingosine 1-phosphate receptor 4Homo sapiens (human)IC5010.000011
Sphingosine 1-phosphate receptor 5Homo sapiens (human)IC502.100011
Sphingosine-1-phosphate lyase 1Homo sapiens (human)IC5034.500022
Sphingosine-1-phosphate lyase 1Mus musculus (house mouse)IC5052.400011
Steroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)IC500.017522
Substance-K receptorHomo sapiens (human)IC5028.224011
Substance-K receptorHomo sapiens (human)Ki9.408011
Succinyl-diaminopimelate desuccinylaseHaemophilus influenzae Rd KW20IC501,000.000011
Thioredoxin reductase Entamoeba histolyticaKi3.300011
Thymidylate kinaseMycobacterium tuberculosis H37RvKi560.000011
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC5014.900011
transactivating tegument protein VP16 [Human herpesvirus 1]Human alphaherpesvirus 1 (Herpes simplex virus type 1)IC504.426011
Trypsin-1Homo sapiens (human)IC501,000.000011
Trypsin-2Homo sapiens (human)IC501,000.000011
Trypsin-3Homo sapiens (human)IC501,000.000011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC501.200011
TyrosinaseHomo sapiens (human)IC508,400.000011
Tyrosine-protein kinase ABL1Homo sapiens (human)IC50100.000011
Tyrosine-protein kinase ABL2Homo sapiens (human)IC50100.000011
Tyrosine-protein kinase FynHomo sapiens (human)IC502.146011
Tyrosine-protein kinase LckHomo sapiens (human)IC503.729011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50116.050022
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50116.050022
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50116.050022
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50116.050022
X-linked inhibitor of apoptosisHomo sapiens (human)IC50100.000022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
26S proteasome regulatory subunit 6BHomo sapiens (human)Kd30.000011
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC503.475011
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC502.319011
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC500.074011
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.506011
5'-AMP-activated protein kinase catalytic subunit alpha-1Homo sapiens (human)Kd30.000011
5'-AMP-activated protein kinase subunit gamma-1Homo sapiens (human)Kd30.000011
5'-AMP-activated protein kinase subunit gamma-2Homo sapiens (human)Kd30.000011
AarF domain-containing protein kinase 1Homo sapiens (human)Kd30.000011
Actin-related protein 2Homo sapiens (human)Kd30.000011
Actin-related protein 3Homo sapiens (human)Kd30.000011
Activated CDC42 kinase 1Homo sapiens (human)Kd30.000011
Activin receptor type-1Homo sapiens (human)Kd30.000011
Activin receptor type-1BHomo sapiens (human)Kd30.000011
Activin receptor type-2BHomo sapiens (human)Kd30.000011
Acyl-CoA dehydrogenase family member 10Homo sapiens (human)Kd30.000011
Acyl-CoA dehydrogenase family member 11Homo sapiens (human)Kd30.000011
Adenine phosphoribosyltransferaseHomo sapiens (human)Kd30.000011
Adenosine kinaseHomo sapiens (human)Kd30.000011
Adenylate kinase 2, mitochondrialHomo sapiens (human)Kd30.000012
ADP/ATP translocase 2Homo sapiens (human)Kd30.000011
ADP/ATP translocase 3Homo sapiens (human)Kd30.000011
AlbuminHomo sapiens (human)Kd44.000011
Androgen receptorHomo sapiens (human)EC5017.050011
Angiotensin-converting enzyme 2 Homo sapiens (human)EC502.380617
AP2-associated protein kinase 1Homo sapiens (human)Kd30.000011
ATP-dependent 6-phosphofructokinase, platelet typeHomo sapiens (human)Kd30.000011
ATP-dependent RNA helicase DDX1Homo sapiens (human)Kd30.000011
ATP-dependent RNA helicase DDX3XHomo sapiens (human)Kd30.000011
ATP-dependent RNA helicase DDX42Homo sapiens (human)Kd30.000011
Atypical kinase COQ8A, mitochondrialHomo sapiens (human)Kd30.000011
Aurora kinase AHomo sapiens (human)Kd0.049011
Beta-adrenergic receptor kinase 1Homo sapiens (human)Kd30.000011
BMP-2-inducible protein kinaseHomo sapiens (human)Kd30.000011
Bone morphogenetic protein receptor type-1AHomo sapiens (human)Kd30.000011
Bone morphogenetic protein receptor type-1BHomo sapiens (human)Kd30.000011
Bone morphogenetic protein receptor type-2Homo sapiens (human)Kd30.000011
Breakpoint cluster region proteinHomo sapiens (human)Kd30.000011
calcineurin A1, putativeCandida dubliniensis CD36EC50180.000011
Calcium/calmodulin-dependent protein kinase kinase 2Homo sapiens (human)Kd30.000011
Calcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)Kd30.000011
Calcium/calmodulin-dependent protein kinase type II subunit gammaHomo sapiens (human)Kd30.000011
Calcium/calmodulin-dependent protein kinase type IVHomo sapiens (human)Kd30.000011
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)Kd30.000011
cAMP-dependent protein kinase catalytic subunit betaHomo sapiens (human)Kd30.000011
cAMP-dependent protein kinase catalytic subunit gammaHomo sapiens (human)Kd30.000011
cAMP-dependent protein kinase type II-alpha regulatory subunitHomo sapiens (human)Kd30.000011
Capsid protein Hepatitis B virusEC505.185022
Casein kinase I isoform alphaHomo sapiens (human)Kd30.000011
Casein kinase I isoform deltaHomo sapiens (human)Kd30.000011
Casein kinase I isoform epsilonHomo sapiens (human)Kd30.000011
Casein kinase I isoform gamma-1Homo sapiens (human)Kd30.000011
Casein kinase I isoform gamma-2Homo sapiens (human)Kd30.000011
Casein kinase I isoform gamma-3Homo sapiens (human)Kd30.000011
Casein kinase II subunit alpha'Homo sapiens (human)Kd1.947011
cGMP-dependent protein kinase 1 Homo sapiens (human)Kd30.000011
Chain A, AROMATIC AMINO ACID AMINOTRANSFERASEParacoccus denitrificansKd5,000.000019
Chain B, AROMATIC AMINO ACID AMINOTRANSFERASEParacoccus denitrificansKd5,000.000019
Chromodomain-helicase-DNA-binding protein 4Homo sapiens (human)Kd30.000011
Citron Rho-interacting kinaseHomo sapiens (human)Kd30.000011
Complement C5Homo sapiens (human)Kd0.570011
Cyclin-dependent kinase 1Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 12Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 13Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 16Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 17Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 2Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 3Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 4Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 6Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 7Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase 9Homo sapiens (human)Kd30.000011
Cyclin-dependent kinase-like 5Homo sapiens (human)Kd30.000011
Cyclin-dependent-like kinase 5 Homo sapiens (human)Kd30.000011
Cyclin-G-associated kinaseHomo sapiens (human)Kd30.000011
Cysteine--tRNA ligase, cytoplasmicHomo sapiens (human)Kd30.000012
Cytochrome c1, heme protein, mitochondrialHomo sapiens (human)Kd30.000011
Cytochrome P450 2C9 Homo sapiens (human)EC500.230011
Cytochrome P450 3A4Homo sapiens (human)EC5017.050011
dCTP pyrophosphatase 1Homo sapiens (human)Kd30.000011
Delta(24)-sterol reductaseHomo sapiens (human)Kd30.000012
Deoxycytidine kinaseHomo sapiens (human)Kd30.000011
Discoidin domain-containing receptor 2Homo sapiens (human)Kd30.000011
DNA replication licensing factor MCM4Homo sapiens (human)Kd30.000011
DNA topoisomerase 2-alphaHomo sapiens (human)Kd30.000012
DNA topoisomerase 2-betaHomo sapiens (human)Kd30.000011
DNA-(apurinic or apyrimidinic site) endonucleaseHomo sapiens (human)Kd0.089011
DnaJ homolog subfamily A member 1Homo sapiens (human)Kd30.000011
Dual specificity mitogen-activated protein kinase kinase 1Homo sapiens (human)Kd30.000011
Dual specificity mitogen-activated protein kinase kinase 2Homo sapiens (human)Kd30.000011
Dual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)Kd30.000011
Dual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)Kd0.082011
Dual specificity mitogen-activated protein kinase kinase 6Homo sapiens (human)Kd30.000011
Dual specificity protein kinase CLK1Homo sapiens (human)Kd30.000011
Dual specificity protein kinase CLK2Homo sapiens (human)Kd30.000011
Dual specificity protein kinase CLK3Homo sapiens (human)Kd30.000011
Dual specificity testis-specific protein kinase 1Homo sapiens (human)Kd30.000011
Dual specificity testis-specific protein kinase 2Homo sapiens (human)Kd30.000011
Dual specificity tyrosine-phosphorylation-regulated kinase 1AHomo sapiens (human)Kd1.699011
Dynamin-like 120 kDa protein, mitochondrialHomo sapiens (human)Kd30.000011
EKC/KEOPS complex subunit TP53RKHomo sapiens (human)Kd30.000011
Electron transfer flavoprotein subunit betaHomo sapiens (human)Kd30.000011
Elongation factor Tu, mitochondrialHomo sapiens (human)Kd30.000011
Ephrin type-A receptor 1Homo sapiens (human)Kd30.000011
Ephrin type-A receptor 2Homo sapiens (human)Kd30.000011
Ephrin type-A receptor 4Homo sapiens (human)Kd30.000011
Ephrin type-A receptor 5Homo sapiens (human)Kd30.000011
Ephrin type-A receptor 7Homo sapiens (human)Kd30.000011
Ephrin type-B receptor 2Homo sapiens (human)Kd30.000011
Ephrin type-B receptor 3Homo sapiens (human)Kd30.000011
Ephrin type-B receptor 4Homo sapiens (human)Kd30.000011
Ephrin type-B receptor 6Homo sapiens (human)Kd30.000011
Epidermal growth factor receptorHomo sapiens (human)Kd1.734011
Epithelial discoidin domain-containing receptor 1Homo sapiens (human)Kd30.000012
Estrogen receptorHomo sapiens (human)EC501.082022
Estrogen receptor betaHomo sapiens (human)EC501.082022
Eukaryotic translation initiation factor 2-alpha kinase 1Homo sapiens (human)Kd30.000011
Eukaryotic translation initiation factor 5BHomo sapiens (human)Kd30.000011
Exosome RNA helicase MTR4Homo sapiens (human)Kd30.000011
Ferrochelatase, mitochondrialHomo sapiens (human)Kd30.000011
Fibroblast growth factor receptor 1Homo sapiens (human)Kd30.000011
Flavin reductase (NADPH)Homo sapiens (human)Kd0.070412
Focal adhesion kinase 1Homo sapiens (human)Kd30.000011
General transcription and DNA repair factor IIH helicase subunit XPDHomo sapiens (human)Kd30.000011
Glucocorticoid receptorHomo sapiens (human)EC500.000422
Glucocorticoid receptorHomo sapiens (human)Kd0.029011
Glycine receptor subunit alpha-1Homo sapiens (human)EC500.380011
Glycine--tRNA ligaseHomo sapiens (human)Kd30.000011
Glycogen phosphorylase, brain formHomo sapiens (human)Kd30.000011
Glycogen phosphorylase, liver formHomo sapiens (human)Kd30.000011
Glycogen synthase kinase-3 alphaHomo sapiens (human)Kd30.000011
Glycogen synthase kinase-3 betaHomo sapiens (human)Kd30.000011
GTP-binding nuclear protein RanHomo sapiens (human)Kd30.000011
Guanine nucleotide-binding protein G(i) subunit alpha-2Homo sapiens (human)Kd30.000011
heat shock protein 90Candida albicansEC50106.903733
Heme oxygenase 2Homo sapiens (human)Kd30.000011
Hepatocyte growth factor receptorHomo sapiens (human)Kd30.000011
High affinity nerve growth factor receptorHomo sapiens (human)Kd30.000011
Hsf1 proteinMus musculus (house mouse)EC502.179022
Inhibitor of nuclear factor kappa-B kinase subunit epsilonHomo sapiens (human)Kd30.000011
Inosine-5'-monophosphate dehydrogenase 2Homo sapiens (human)Kd30.000011
Insulin receptorHomo sapiens (human)Kd30.000011
Insulin-like growth factor 1 receptorHomo sapiens (human)Kd30.000011
Integrin alpha-LHomo sapiens (human)Kd12.900011
Interleukin-1 receptor-associated kinase 1Homo sapiens (human)Kd30.000011
Interleukin-1 receptor-associated kinase 3Homo sapiens (human)Kd30.000011
Interleukin-1 receptor-associated kinase 4Homo sapiens (human)Kd30.000011
Isoleucine--tRNA ligase, mitochondrialHomo sapiens (human)Kd30.000011
LIM domain kinase 1Homo sapiens (human)Kd30.000011
LIM domain kinase 2Homo sapiens (human)Kd30.000011
Long-chain-fatty-acid--CoA ligase 5Homo sapiens (human)Kd30.000011
Macrophage-stimulating protein receptorHomo sapiens (human)Kd1.416011
MAP kinase-activated protein kinase 2Homo sapiens (human)Kd30.000011
MAP kinase-activated protein kinase 3Homo sapiens (human)Kd30.000012
MAP kinase-activated protein kinase 5Homo sapiens (human)Kd30.000011
MAP/microtubule affinity-regulating kinase 3Homo sapiens (human)Kd30.000011
Mas-related G-protein coupled receptor member X2Homo sapiens (human)EC508.400022
Mast/stem cell growth factor receptor KitHomo sapiens (human)Kd0.017011
Maternal embryonic leucine zipper kinaseHomo sapiens (human)Kd30.000011
matrix metalloproteinase 1, partialHomo sapiens (human)EC505.650011
Membrane-associated progesterone receptor component 1Homo sapiens (human)Kd30.000011
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinaseHomo sapiens (human)Kd30.000011
MidasinHomo sapiens (human)Kd30.000011
Mineralocorticoid receptor Homo sapiens (human)EC503.000011
Misshapen-like kinase 1Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 1Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 10Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 11Homo sapiens (human)Kd30.000012
Mitogen-activated protein kinase 14Homo sapiens (human)Kd30.000012
Mitogen-activated protein kinase 15Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 3 Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 7Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 8Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase 9Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 1Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 11Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 2Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 20Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 3Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 4Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 5Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase 6Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase kinase 1Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase kinase 2Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase kinase 3Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase kinase 4Homo sapiens (human)Kd30.000011
Mitogen-activated protein kinase kinase kinase kinase 5Homo sapiens (human)Kd2.236011
Mu-type opioid receptorHomo sapiens (human)EC506.100011
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.468011
Multifunctional protein ADE2Homo sapiens (human)Kd30.000011
Myosin light chain kinase 3Homo sapiens (human)Kd30.000011
Myosin light chain kinase, smooth muscleHomo sapiens (human)Kd30.000011
Myosin-14Homo sapiens (human)Kd30.000011
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13Homo sapiens (human)Kd30.000011
Non-receptor tyrosine-protein kinase TNK1Homo sapiens (human)Kd30.000011
Non-receptor tyrosine-protein kinase TYK2Homo sapiens (human)Kd30.000011
NS5 Zika virusEC5015.510022
NUAK family SNF1-like kinase 2Homo sapiens (human)Kd30.000012
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC501.602022
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC5063.100011
Nuclear receptor subfamily 4 group A member 2Homo sapiens (human)EC5036.820055
Nucleolar GTP-binding protein 1Homo sapiens (human)Kd30.000011
Obg-like ATPase 1Homo sapiens (human)Kd30.000011
Peroxisomal acyl-coenzyme A oxidase 1Homo sapiens (human)Kd30.000011
Peroxisomal acyl-coenzyme A oxidase 3Homo sapiens (human)Kd30.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC5022.650011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Kd100.000011
Phenylalanine--tRNA ligase beta subunitHomo sapiens (human)Kd30.000011
Phosphatidylethanolamine-binding protein 1Homo sapiens (human)Kd30.000011
Phosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)Kd30.000011
Phosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)Kd30.000011
Phospholipid hydroperoxide glutathione peroxidaseHomo sapiens (human)EC5016.522022
Phosphorylase b kinase gamma catalytic chain, liver/testis isoformHomo sapiens (human)Kd30.000011
Platelet-derived growth factor receptor alphaHomo sapiens (human)Kd0.038011
Platelet-derived growth factor receptor betaHomo sapiens (human)Kd1.366522
Probable ATP-dependent RNA helicase DDX6Homo sapiens (human)Kd30.000011
Procathepsin LHomo sapiens (human)EC502.380617
Prostacyclin receptorHomo sapiens (human)EC500.006011
Prostacyclin receptorRattus norvegicus (Norway rat)EC500.200011
Prostaglandin D2 receptorHomo sapiens (human)EC500.100011
Protein kinase C alpha typeHomo sapiens (human)Kd30.000011
Protein kinase C beta typeHomo sapiens (human)Kd30.000011
Protein kinase C delta typeHomo sapiens (human)Kd30.000011
Protein kinase C iota typeHomo sapiens (human)Kd30.000011
Protein kinase C theta typeHomo sapiens (human)Kd30.000011
Protein-tyrosine kinase 2-betaHomo sapiens (human)Kd30.000011
Protein-tyrosine kinase 6Homo sapiens (human)Kd30.000011
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)Kd0.144522
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)Kd30.000011
Putative heat shock protein HSP 90-beta 2Homo sapiens (human)Kd30.000011
Pyridoxal kinaseHomo sapiens (human)Kd30.000011
Rab-like protein 3Homo sapiens (human)Kd30.000011
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)Kd30.000011
RAC-beta serine/threonine-protein kinaseHomo sapiens (human)Kd30.000011
RAC-gamma serine/threonine-protein kinaseHomo sapiens (human)Kd30.000011
Ras-related protein Rab-10Homo sapiens (human)Kd30.000011
Ras-related protein Rab-6AHomo sapiens (human)Kd0.033011
Receptor-interacting serine/threonine-protein kinase 2Homo sapiens (human)Kd1.850011
Receptor-interacting serine/threonine-protein kinase 3Homo sapiens (human)Kd30.000011
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)Kd0.132522
recombinase AMycobacterium tuberculosis H37RvEC50195.150022
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC502.380617
Replicase polyprotein 1abBetacoronavirus England 1EC502.380617
Replicase polyprotein 1abHuman coronavirus 229EEC502.380617
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC502.8294410
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC502.380617
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Kd11.950022
Retinoic acid receptor alphaHomo sapiens (human)EC500.063011
Retinoic acid receptor betaHomo sapiens (human)EC500.000811
Retinoic acid receptor gamma Homo sapiens (human)EC500.040011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC5025.021022
Rho-associated protein kinase 1Homo sapiens (human)Kd30.000011
Rho-associated protein kinase 2Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase alpha-1Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase alpha-3Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase alpha-4Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase alpha-5Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase alpha-6Homo sapiens (human)Kd30.000011
Ribosomal protein S6 kinase beta-1Homo sapiens (human)Kd30.000011
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)Kd30.000011
RNA cytidine acetyltransferaseHomo sapiens (human)Kd30.000011
RNA-directed RNA polymerase EC500.14541212
S-adenosylmethionine synthase isoform type-2Homo sapiens (human)Kd30.000011
Septin-9Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 10Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 16Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 24Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 26Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 3Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase 4Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase ATRHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase B-rafHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase Chk1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase D2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase D3Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase ICKHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase LATS1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase MARK2Homo sapiens (human)Kd30.000012
Serine/threonine-protein kinase MRCK alphaHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase MRCK betaHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase MRCK gammaHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase N1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase N2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase Nek1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase Nek2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase Nek3Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase Nek9Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase NLKHomo sapiens (human)Kd30.000011
Serine/threonine-protein kinase PAK 2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase PAK 4Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase PAK 6Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase pim-1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase PLK4Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase SIK2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase SIK3Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase STK11Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase TAO1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase TAO2Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase TAO3Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase TBK1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase ULK1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase ULK3Homo sapiens (human)Kd30.000012
Serine/threonine-protein kinase/endoribonuclease IRE1Homo sapiens (human)Kd30.000011
Serine/threonine-protein kinase/endoribonuclease IRE2Homo sapiens (human)Kd30.000011
Sphingosine 1-phosphate receptor 1Homo sapiens (human)EC503.834966
Sphingosine 1-phosphate receptor 2Homo sapiens (human)EC5010.000011
Sphingosine 1-phosphate receptor 3Homo sapiens (human)EC505.628744
Sphingosine 1-phosphate receptor 4Homo sapiens (human)EC505.000222
Sphingosine 1-phosphate receptor 5Homo sapiens (human)EC504.387533
Spike glycoproteinBetacoronavirus England 1EC502.380617
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC502.380617
STE20-like serine/threonine-protein kinase Homo sapiens (human)Kd30.000011
STE20-related kinase adapter protein alphaHomo sapiens (human)Kd30.000011
streptokinase A precursorStreptococcus pyogenes M1 GASEC500.428512
Structural maintenance of chromosomes protein 1AHomo sapiens (human)Kd30.000011
Structural maintenance of chromosomes protein 2Homo sapiens (human)Kd30.000011
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrialHomo sapiens (human)Kd30.000011
Taste receptor type 2 member 16Homo sapiens (human)EC501,400.000022
Taste receptor type 2 member 46Homo sapiens (human)EC5031.000011
TGF-beta receptor type-1Homo sapiens (human)Kd30.000011
TGF-beta receptor type-2Homo sapiens (human)Kd30.000011
Thyroid hormone receptor-associated protein 3Homo sapiens (human)Kd30.000011
TRAF2 and NCK-interacting protein kinaseHomo sapiens (human)Kd30.000011
Transmembrane protease serine 2Homo sapiens (human)EC502.380617
Tyrosine--tRNA ligase, cytoplasmicHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase ABL1Homo sapiens (human)Kd30.000011
Tyrosine-protein kinase ABL2Homo sapiens (human)Kd30.000011
Tyrosine-protein kinase BTKHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase CSKHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase FerHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase Fes/FpsHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase FRKHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase FynHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase HCKHomo sapiens (human)Kd2.886011
Tyrosine-protein kinase JAK1Homo sapiens (human)Kd30.000011
Tyrosine-protein kinase LckHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase LynHomo sapiens (human)Kd3.633011
Tyrosine-protein kinase MerHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase SYKHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase TecHomo sapiens (human)Kd30.000011
Tyrosine-protein kinase YesHomo sapiens (human)Kd30.000011
U5 small nuclear ribonucleoprotein 200 kDa helicaseHomo sapiens (human)Kd30.000011
Uncharacterized protein FLJ45252Homo sapiens (human)Kd30.000011
Very long-chain specific acyl-CoA dehydrogenase, mitochondrialHomo sapiens (human)Kd30.000011
Wee1-like protein kinaseHomo sapiens (human)Kd30.000012

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AAA family ATPase Staphylococcus aureusKm192.000011
Adenosine receptor A1Rattus norvegicus (Norway rat)KA11.400011
Adenosine receptor A2aRattus norvegicus (Norway rat)KA11.400012
ATP-dependent translocase ABCB1Homo sapiens (human)Km4,200.000011
Carbonic anhydraseCandida albicans SC5314KA0.960011
Carbonic anhydraseMethanosarcina thermophilaKA39.000011
Carbonic anhydraseMethanothermobacter thermautotrophicus str. Delta HKa11.400011
Carbonic anhydraseSaccharomyces cerevisiae S288CKa90.000022
Carbonic anhydrase Cryptococcus neoformans var. grubiiKA43.300011
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ka23.300011
Carbonic anhydrase 1Homo sapiens (human)KA3.10001111
Carbonic anhydrase 12Homo sapiens (human)KA1.670011
Carbonic anhydrase 13Mus musculus (house mouse)KA43.000011
Carbonic anhydrase 14Homo sapiens (human)KA12.100011
Carbonic anhydrase 15Mus musculus (house mouse)KA6.500011
Carbonic anhydrase 2Homo sapiens (human)KA11.40001313
Carbonic anhydrase 3Homo sapiens (human)Ka13.500022
Carbonic anhydrase 4Homo sapiens (human)KA15.300022
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)KA0.036011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)KA0.063011
Carbonic anhydrase 6Homo sapiens (human)Ka18.000022
Carbonic anhydrase 7Homo sapiens (human)KA58.300011
Carbonic anhydrase 9Homo sapiens (human)KA51.300011
Carbonic anhydrase-like protein, putativeTrypanosoma cruzi strain CL BrenerKA0.830011
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC502.480011
Cytidine deaminaseHomo sapiens (human)Km600.666733
Cytochrome P450 2C8Homo sapiens (human)Km1.900011
Cytochrome P450 2D6Homo sapiens (human)Km1.400011
Deoxycytidine kinaseHomo sapiens (human)Km1.775022
DNA topoisomerase 1Homo sapiens (human)CC50100.000011
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvMIC25.340011
FlavodoxinHelicobacter pylori 26695MIC67.300033
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)KA58.300011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)KA58.300011
H3 histone acetyltransferaseCandida albicans SC5314AC509.630011
HRAS, partialHomo sapiens (human)AC5023.047033
Hsf1 proteinMus musculus (house mouse)AbsAC40_uM25.200011
HSP40, subfamily A [Plasmodium falciparum 3D7]Plasmodium falciparum 3D7AbsAC1000_uM1.512011
hypothetical protein CAALFM_CR05890CACandida albicans SC5314AC509.630011
interferon gamma precursorHomo sapiens (human)AC5022.855022
Liver carboxylesterase 1Homo sapiens (human)Km1,460.000018
Lysosomal protective proteinHomo sapiens (human)Km610.000011
Monocarboxylate transporter 10Rattus norvegicus (Norway rat)Km6,430.000011
PAX8Homo sapiens (human)AC505.340011
Plasma kallikreinHomo sapiens (human)KA0.063011
Polyphenol oxidase 2Agaricus bisporusKic1.900011
Polyphenol oxidase 2Agaricus bisporusKm860.000011
RCG53912, isoform CRA_a Rattus norvegicus (Norway rat)Km64.600011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC50196.940022
RNA-directed RNA polymerase EC900.834377
Skn7pSaccharomyces cerevisiae (brewer's yeast)AbsAC40_uM1.830011
SLC16A10 proteinHomo sapiens (human)Km1,212.500011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Km252.000011
Sphingosine kinase 1Homo sapiens (human)Km23.700011
Sphingosine kinase 1 Rattus norvegicus (Norway rat)Km64.600011
Sphingosine kinase 2Homo sapiens (human)Km23.700011
Taste receptor type 2 member 16Homo sapiens (human)Activity70.000022
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km1,100.000012
Uridine phosphorylase 1Homo sapiens (human)Km6,000.000011