Page last updated: 2024-08-05 15:01:20

antimetabolite

A substance which is structurally similar to a metabolite but which competes with it or replaces it, and so prevents or reduces its normal utilization.

ChEBI ID: 35221

Members (60)

MemberDefinitionClass
10-propargyl-10-deazaaminopterinA pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.pralatrexate
2-aminopurineThe parent compound of the 2-aminopurines, comprising a purine core carrying an amino substituent at the 2-position.2-aminopurine
3'-deoxyadenosine 5'-triphosphatecordycepin triphosphate
5-iodouracilAn organoiodine compound consisting of uracil having an iodo substituent at the 5-position.5-iodouracil
6-aminonicotinamideA monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 6-aminonicotinic acid with ammonia. An inhibitor of the NADP(+)-dependent enzyme, 6-phosphogluconate dehydrogenase, it interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as cisplatin, in killing cancer cells.6-aminonicotinamide
acivicinAn L-alpha-amino acid that is L-alanine in which the methyl group is replaced by a (5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl group. A glutamine analogue antimetabolite, it interferes with glutamate metabolism and several glutamate-dependent synthetic enzymes. It is obtained as a fermentation product of Streptomyces sviceus bacteria.acivicin
acyclovirAn oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.acyclovir
allopurinolA bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.allopurinol
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
anticapsinAn L-alpha-amino acid zwitterion obtained by transfer of a proton from the carboxy to the amino group of anticapsin; major species at pH 7.3.anticapsin zwitterion; anticapsin
anticapsinAn alanine derivative that is L-alanine bearing a 5-oxo-7-oxabicyclo[4.1.0]hept-2-yl substituent at position 3.anticapsin zwitterion; anticapsin
azaguanineA triazolopyrimidine that consists of 3,6-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidine bearing amino and oxo substituents at positions 5 and 7 respectively.8-azaguanine
azaserineA carboxylic ester resulting from the formal condensation of the carboxy group of diazoacetic acid with the alcoholic hydroxy group of L-serine. An antibiotic produced by a Streptomyces species.azaserine
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
azauracilA 1,2,4-triazine compound having oxo-substituents at the 3- and 5-positions.6-azauracil
azauridine6-azauridine
brequinarA quinolinemonocarboxylic acid that is quinoline substituted by 2'-fluoro[1,1'-biphenyl]-4-yl, methyl, carboxy and fluoro groups at positions 2, 3, 4, and 6, respectively. It is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis. The compound exhibits antineoplastic and antiviral properties.brequinar
brequinar sodiumAn organic sodium salt of brequinar.brequinar sodium
bromodeoxyuridineA pyrimidine 2'-deoxyribonucleoside compound having 5-bromouracil as the nucleobase.5-bromo-2'-deoxyuridine
canalineA non-proteinogenic L-alpha-amino acid that is L-homoserine in which the hydroxy group at position 4 is substituted by an aminooxy group. It has been isolated from legumes and plays an essential role in lugume chemical defense against insects.L-canaline zwitterion; L-canaline
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
ceruleninAn epoxydodecadienamide isolated from several species, including Acremonium, Acrocylindrum and Helicoceras. It inhibits the biosynthesis of several lipids by interfering with enzyme function.cerulenin
clofarabineA purine nucleoside analogue consisting of a 6-amino-2-chloropurin-9-yl group attached to the 1beta position of 2'-deoxy-2'-fluoro-D-arabinofuranose. It is metabolized intracellularly to the active 5'-triphosphate metabolite, which inhibits DNA synthesisis and so stops the growth of cancer cells. Clofarabine is used as an antimetabolite antineoplastic agent in the treatment of relapsed or refractory acute lymphoblastic leukaemia.clofarabine
cordycepincordycepin
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
cycloserineA 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).D-cycloserine zwitterion; D-cycloserine
cytarabineA pyrimidine nucleoside in which cytosine is attached to D-arabinofuranose via a beta-N(1)-glycosidic bond. Used mainly in the treatment of leukaemia, especially acute non-lymphoblastic leukaemia, cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It also has antiviral and immunosuppressant properties.cytarabine
diazooxonorleucineA non-proteinogenic L-alpha-amino acid that is L-norleucine which is substituted at position 5 by an oxo group and at position 6 by a diazo group. It is as inhibitor of various glutamine-utilising enzymes.6-diazo-5-oxo-L-norleucine zwitterion; 6-diazo-5-oxo-L-norleucine
didanosineA purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.didanosine
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
ethionineAn S-ethylhomocysteine that has S-configuration at the chiral centre.L-ethionine
ezetimibeA beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).ezetimibe
floxuridineA pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.floxuridine
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
fluorouracilA nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.5-fluorouracil
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
gemcitabine hydrochlorideA 2'-deoxycytidine hydrochloriode having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine hydrochloride is used in the treatment of various carcinomas, including non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.gemcitabine hydrochloride
hydroxyureaA member of the class of ureas that is urea in which one of the hydrogens is replaced by a hydroxy group. An antineoplastic used in the treatment of chronic myeloid leukaemia as well as for sickle-cell disease.hydroxyurea
i-677An L-alpha-amino acid that is L-serine in which the hydroxy group at position 3 is converted to the corresponding 2-aminoethyl ether. An antimetabolic antibiotic obtained from Streptomyces reseoviridofuscus.O-(2-aminoethyl)-L-serine
meglutolA dicarboxylic acid that is glutaric acid in which one of the two hydrogens at position 3 is substituted by a hydroxy group, while the other is substituted by a methyl group. It has been found to accumulate in urine of patients suffering from HMG-CoA lyase (3-hydroxy-3-methylglutaryl-CoA lyase, EC 4.1.3.4) deficiency. It occurs as a plant metabolite in Crotalaria dura.3-hydroxy-3-methylglutaric acid
mercaptopurineA thiol that is the tautomer of mercaptopurine.3,7-dihydropurine-6-thione; mercaptopurine; purine-6-thiol
mercaptopurineA member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.3,7-dihydropurine-6-thione; mercaptopurine; purine-6-thiol
methotrexatemethotrexate
metyraponeAn aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency.metyrapone
nsc-145,668A hydrochloride salt resulting from the reaction of equimolar amounts of ancitabine and hydrogen chloride.ancitabine hydrochloride
oxythiamineA 1,3-thiazolium cation that is 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole alkylated at the N3 position by a (2-methyl-4-oxo-1,4-dihydropyrimidin-5-yl)methyl group.oxythiamine(1+)
pemetrexedAn N-acylglutamic acid in which the N-acyl group is specified as 4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).pemetrexed
pentostatinA member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.pentostatin
propylthiouracilA pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.6-propyl-2-thiouracil
pyrazofurinA C-glycosyl compound that is 4-hydroxy-1H-pyrazole-5-carboxamide in which the hydrogen at position 3 has been replaced by a beta-D-ribofuranosyl group.pirazofurin
ribavirinA 1-ribosyltriazole that is the 1-ribofuranosyl derivative of 1,2,4-triazole-3-carboxamide. A synthetic guanosine analogue, it is an inhibitor of HCV polymerase and possesses a broad spectrum of activity against DNA and RNA viruses.ribavirin
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
stavudineA nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptasestavudine
thioguanine anhydrousA 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.tioguanine
thiouridineA thiouridine in which the oxygen replaced by sulfur is that at C-4.4-thiouridine
toyocamycinAn N-glycosylpyrrolopyrimidine that is tubercidin in which the hydrogen at position 5 of the pyrrolopyrimidine moiety has been replaced by a cyano group.toyocamycin
trifluridineA pyrimidine 2'-deoxyribonucleoside compound having 5-trifluoromethyluracil as the nucleobase. An antiviral drug used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis.trifluridine
tubercidinAn N-glycosylpyrrolopyrimidine that is adenosine in which the in the 5-membered ring that is not attached to the ribose moiety is replaced by a carbon. Tubercidin is produced in the culture broth of Streptomyces tubericidus.tubercidin
zalcitabineA pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.zalcitabine
zidovudineA pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.zidovudine

Research

Studies (210,180)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199055,232 (26.28)18.7374
1990's38,744 (18.43)18.2507
2000's48,195 (22.93)29.6817
2010's52,877 (25.16)24.3611
2020's15,132 (7.20)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials34,291 (13.62%)5.53%
Reviews23,373 (9.28%)6.00%
Case Studies29,065 (11.54%)4.05%
Observational1,234 (0.49%)0.25%
Other163,879 (65.07%)84.16%

Protein Targets (469)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency31.066314
15-lipoxygenase, partialHomo sapiens (human)Potency5.001612
67.9K proteinVaccinia virusPotency6.7437225
acetylcholinesteraseHomo sapiens (human)Potency35.052028
acid sphingomyelinaseHomo sapiens (human)Potency31.622811
activating transcription factor 6Homo sapiens (human)Potency0.088628
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency32.0662113
alpha-galactosidaseHomo sapiens (human)Potency29.787713
Alpha-synucleinHomo sapiens (human)Potency5.623411
Amyloid-beta precursor proteinHomo sapiens (human)Potency18.356411
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency29.716414
AR proteinHomo sapiens (human)Potency18.56381286
aryl hydrocarbon receptorHomo sapiens (human)Potency31.6899215
arylsulfatase AHomo sapiens (human)Potency19.587915
ATAD5 protein, partialHomo sapiens (human)Potency9.366238
Ataxin-2Homo sapiens (human)Potency10.9872213
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency17.953349
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency7.8254214
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency8.492111
Bloom syndrome protein isoform 1Homo sapiens (human)Potency40.2011216
BRCA1Homo sapiens (human)Potency11.220211
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency28.214112
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency70.547311
caspase-1 isoform alpha precursorHomo sapiens (human)Potency15.848911
caspase-3Cricetulus griseus (Chinese hamster)Potency15.793611
caspase-3Homo sapiens (human)Potency70.547311
Caspase-7Cricetulus griseus (Chinese hamster)Potency15.793611
Caspase-7Homo sapiens (human)Potency15.848911
Cellular tumor antigen p53Homo sapiens (human)Potency10.2984360
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency7.6613211
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency26.586413
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency0.794311
Chain A, Beta-lactamaseEscherichia coli K-12Potency22.740612
Chain A, Ferritin light chainEquus caballus (horse)Potency20.789525
Chain A, HADH2 proteinHomo sapiens (human)Potency29.094123
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency14.518613
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.2240212
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency13.700526
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency48.451626
Chain B, HADH2 proteinHomo sapiens (human)Potency29.094123
chromobox protein homolog 1Homo sapiens (human)Potency65.6444216
ClpPBacillus subtilisPotency23.735812
cytochrome P450 2C19 precursorHomo sapiens (human)Potency21.486512
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810713
cytochrome P450 2C9, partialHomo sapiens (human)Potency16.729917
cytochrome P450 2D6Homo sapiens (human)Potency20.195515
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency16.4600216
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.6015213
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency9.8287116
D(1A) dopamine receptorSus scrofa (pig)Potency0.926811
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency12.589311
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency5.799724
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency6.447135
DNA polymerase betaHomo sapiens (human)Potency59.621812
DNA polymerase eta isoform 1Homo sapiens (human)Potency31.622811
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency86.163218
DNA polymerase kappa isoform 1Homo sapiens (human)Potency46.779112
dopamine D1 receptorHomo sapiens (human)Potency4.610911
endonuclease IVEscherichia coliPotency5.618623
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.884610122
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency21.8332210
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency13.100710141
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.8066123
EWS/FLI fusion proteinHomo sapiens (human)Potency8.4676442
eyes absent homolog 2 isoform aHomo sapiens (human)Potency100.000011
farnesoid X nuclear receptorHomo sapiens (human)Potency16.9101422
flap endonuclease 1Homo sapiens (human)Potency16.992213
Fumarate hydrataseHomo sapiens (human)Potency14.754019
GVesicular stomatitis virusPotency16.729917
GABA theta subunitRattus norvegicus (Norway rat)Potency16.460018
GALC proteinHomo sapiens (human)Potency0.707912
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency16.460018
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency16.460018
gemininHomo sapiens (human)Potency5.6817339
GLI family zinc finger 3Homo sapiens (human)Potency13.4714224
glp-1 receptor, partialHomo sapiens (human)Potency7.169217
GLS proteinHomo sapiens (human)Potency18.318625
glucocerebrosidaseHomo sapiens (human)Potency20.082712
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.6603320
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.6764116
Glycoprotein hormones alpha chainHomo sapiens (human)Potency2.818411
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency0.819911
Guanine nucleotide-binding protein GHomo sapiens (human)Potency15.446423
heat shock protein beta-1Homo sapiens (human)Potency40.871012
hemoglobin subunit betaHomo sapiens (human)Potency7.7872519
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.810719
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency20.515117
Histone H2A.xCricetulus griseus (Chinese hamster)Potency40.6081232
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency14.125411
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency16.729917
huntingtin isoform 2Homo sapiens (human)Potency1.995311
hypothetical protein, conservedTrypanosoma bruceiPotency14.125411
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency32.463812
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency4.764124
IDH1Homo sapiens (human)Potency3.4122113
importin subunit beta-1 isoform 1Homo sapiens (human)Potency56.511022
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency16.7299114
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency19.702012
Integrin alpha-IIbHomo sapiens (human)Potency7.334115
Integrin beta-3Homo sapiens (human)Potency7.334115
Interferon betaHomo sapiens (human)Potency17.2780210
interleukin 8Homo sapiens (human)Potency68.355317
lamin isoform A-delta10Homo sapiens (human)Potency3.9398228
LuciferasePhotinus pyralis (common eastern firefly)Potency56.362323
M-phase phosphoprotein 8Homo sapiens (human)Potency41.176614
Microtubule-associated protein tauHomo sapiens (human)Potency22.7570214
mitogen-activated protein kinase 1Homo sapiens (human)Potency16.694523
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.035525
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency61.852713
neuropeptide S receptor isoform AHomo sapiens (human)Potency5.011911
NFKB1 protein, partialHomo sapiens (human)Potency1.978324
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency2.224713
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency19.4886342
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency6.5597216
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency0.087111
Nuclear receptor ROR-gammaHomo sapiens (human)Potency15.980314
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency7.196324
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency19.974012
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency7.1933360
P53Homo sapiens (human)Potency56.234111
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency35.481311
ParkinHomo sapiens (human)Potency44.668411
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency35.529324
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.1442213
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency33.356115
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency15.9072418
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency30.698547
phosphopantetheinyl transferaseBacillus subtilisPotency58.189118
PINK1Homo sapiens (human)Potency44.668411
plasminogen precursorMus musculus (house mouse)Potency3.4720111
polyproteinZika virusPotency14.754019
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency25.515412
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency22.387211
PPM1D proteinHomo sapiens (human)Potency18.556912
pregnane X nuclear receptorHomo sapiens (human)Potency30.6993317
pregnane X receptorRattus norvegicus (Norway rat)Potency48.022412
progesterone receptorHomo sapiens (human)Potency17.795029
pyruvate kinase PKM isoform aHomo sapiens (human)Potency39.810722
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency89.125111
RAR-related orphan receptor gammaMus musculus (house mouse)Potency15.4853233
ras-related protein Rab-9AHomo sapiens (human)Potency1.000011
regulator of G-protein signaling 4Homo sapiens (human)Potency25.325512
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency22.3393341
retinoid X nuclear receptor alphaHomo sapiens (human)Potency19.4781328
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency8.845348
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.934911
SMAD family member 2Homo sapiens (human)Potency49.942022
SMAD family member 3Homo sapiens (human)Potency49.942022
Smad3Homo sapiens (human)Potency6.147549
snurportin-1Homo sapiens (human)Potency56.511022
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency6.6578215
survival motor neuron protein isoform dHomo sapiens (human)Potency10.6204122
TAR DNA-binding protein 43Homo sapiens (human)Potency20.543614
TDP1 proteinHomo sapiens (human)Potency7.98872110
thioredoxin glutathione reductaseSchistosoma mansoniPotency20.443413
thioredoxin reductaseRattus norvegicus (Norway rat)Potency21.6172422
ThrombopoietinHomo sapiens (human)Potency6.301024
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency9.2085346
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency395.363446
thyroid stimulating hormone receptorHomo sapiens (human)Potency15.6167418
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency22.909014
tyrosine-protein kinase YesHomo sapiens (human)Potency41.070412
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.589311
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency3.4720111
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency3.4720111
USP1 protein, partialHomo sapiens (human)Potency28.258022
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency27.201713
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency18.070437
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency52.876914
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.6764116
VprHuman immunodeficiency virus 1Potency10.000011

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC504.000011
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)Ki0.023511
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.110622
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.014622
6-phosphogluconate dehydrogenase, decarboxylatingHomo sapiens (human)Ki136.700011
Adenosine deaminaseHomo sapiens (human)Ki0.000188
Adenosine deaminase Bos taurus (cattle)Ki0.000023
Adenosine deaminase Plasmodium falciparum (malaria parasite P. falciparum)Ki0.004122
Adenosine kinaseHomo sapiens (human)IC501,292,888.124045
Adenosine receptor A1Rattus norvegicus (Norway rat)IC503,235,940.000011
Adenosine receptor A1Homo sapiens (human)Ki7.410022
Adenosine receptor A1Mus musculus (house mouse)Ki4.430011
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki9.813333
Adenosine receptor A2aRattus norvegicus (Norway rat)IC503,235,940.000011
Adenosine receptor A2aHomo sapiens (human)Ki7.410011
Adenosine receptor A2bRattus norvegicus (Norway rat)IC503,235,940.000011
Adenosine receptor A3Homo sapiens (human)IC5021.687011
Adenosine receptor A3Rattus norvegicus (Norway rat)IC503,235,940.000011
Adenosine receptor A3Homo sapiens (human)Ki9.834022
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC5021.687011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki12.258011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC5021.687011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki12.258011
Apoptosis regulator Bcl-2Homo sapiens (human)GI50147.000011
AromataseHomo sapiens (human)IC502.815022
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.0000117
ATP-binding cassette sub-family C member 3Rattus norvegicus (Norway rat)Ki90.000011
Bcl-2-like protein 1Homo sapiens (human)GI50183.000011
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K1IC500.084011
Bifunctional dihydrofolate reductase-thymidylate synthaseToxoplasma gondiiIC504.84933254
Bifunctional dihydrofolate reductase-thymidylate synthaseTrypanosoma cruziIC500.110011
Bifunctional dihydrofolate reductase-thymidylate synthaseLeishmania majorKi0.000111
Bifunctional purine biosynthesis protein ATICHomo sapiens (human)IC506.693323
Bifunctional purine biosynthesis protein ATICHomo sapiens (human)Ki100.440012
Bile salt export pumpHomo sapiens (human)IC50380.5429535
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000014
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.0000117
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Ki341.333333
Carbonic anhydrase 1Homo sapiens (human)Ki10.000011
Carbonic anhydrase 2Homo sapiens (human)Ki19.000022
Carbonic anhydrase 4Homo sapiens (human)Ki113.000011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki15.565422
Carbonic anhydrase 9Homo sapiens (human)Ki23.000011
Carnitine O-palmitoyltransferase 1, muscle isoformHomo sapiens (human)IC50100.000011
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC503.120011
Chain A, DEOXYNUCLEOSIDE KINASEDrosophila melanogaster (fruit fly)IC500.760011
Chain A, N-methyl-D-aspartate Receptor Subunit 1Rattus norvegicus (Norway rat)Ki241.000013
Chain A, Purine nucleoside phosphorylaseEscherichia coliKi120.000011
Chain A, Purine nucleoside phosphorylase DeoD-typeEscherichia coli O157:H7Ki120.000011
Chain A, Thymidylate SynthaseEscherichia coliKi0.109012
Chain A, Thymidylate SynthaseHomo sapiens (human)Ki0.109011
Chain A, Uracil PhosphoribosyltransferaseToxoplasma gondiiKi25.000011
Chain E, Purine nucleoside phosphorylaseHomo sapiens (human)Ki90.000011
Cytidine deaminaseHomo sapiens (human)Ki190.000011
Cytochrome P450 11B1, mitochondrialHomo sapiens (human)IC500.01811010
Cytochrome P450 11B1, mitochondrialRattus norvegicus (Norway rat)IC504.735733
Cytochrome P450 11B1, mitochondrial Bos taurus (cattle)IC501.306036
Cytochrome P450 11B2, mitochondrialHomo sapiens (human)IC500.083899
Cytochrome P450 1A2Homo sapiens (human)IC504.800022
Cytochrome P450 2C19Homo sapiens (human)IC505.000011
Cytochrome P450 2C8Homo sapiens (human)IC505.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC504.600011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC502.865922
Cytochrome P450 3A4Homo sapiens (human)Ki190.000011
D-alanine--D-alanine ligaseEnterococcus faecalis V583IC50262.000011
Delta-type opioid receptorRattus norvegicus (Norway rat)IC500.003011
Deoxycytidine kinaseHomo sapiens (human)Ki680.000022
Deoxynucleoside kinaseDrosophila melanogaster (fruit fly)IC505,319.000022
Dihydrofolate reductaseEnterococcus faeciumIC500.001411
Dihydrofolate reductaseEscherichia coli K-12IC50103.13132446
Dihydrofolate reductaseGallus gallus (chicken)IC500.054522
Dihydrofolate reductaseHomo sapiens (human)IC502.430782112
Dihydrofolate reductaseLacticaseibacillus caseiIC5020.37402934
Dihydrofolate reductaseMus musculus (house mouse)IC500.03311111
Dihydrofolate reductaseMycobacterium tuberculosis H37RvIC500.017433
Dihydrofolate reductasePneumocystis cariniiIC5016.49521214
Dihydrofolate reductaseRattus norvegicus (Norway rat)IC500.00471011
Dihydrofolate reductaseEscherichia coli K-12Ki34.546055
Dihydrofolate reductaseHomo sapiens (human)Ki0.29611515
Dihydrofolate reductaseLacticaseibacillus caseiKi0.000011
Dihydrofolate reductaseMus musculus (house mouse)Ki0.23471819
Dihydrofolate reductasePneumocystis cariniiKi0.000011
Dihydrofolate reductaseStaphylococcus aureusKi0.000522
Dihydrofolate reductase Bacillus anthracisIC500.013612
Dihydrofolate reductase Bos taurus (cattle)IC50722.14801111
Dihydroorotate dehydrogenase Schistosoma mansoniIC5020.000022
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC500.01152626
Dihydroorotate dehydrogenase (quinone), mitochondrialRattus norvegicus (Norway rat)IC500.204245
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)Ki0.012022
Dihydropyrimidine dehydrogenase [NADP(+)]Homo sapiens (human)IC500.220011
DNA polymerase betaHomo sapiens (human)IC5020.000011
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)IC500.020011
Enoyl-[acyl-carrier-protein] reductase [NADH] Francisella tularensis subsp. tularensis SCHU S4IC5059.000011
Epidermal growth factor receptorHomo sapiens (human)IC500.320011
Equilibrative nucleoside transporter 1Homo sapiens (human)IC500.190011
exodeoxyribonuclease V subunit RecBEscherichia coli str. K-12 substr. MG1655IC5077.489824
exodeoxyribonuclease V subunit RecCEscherichia coli str. K-12 substr. MG1655IC5077.489724
exodeoxyribonuclease V subunit RecDEscherichia coli str. K-12 substr. MG1655IC5077.489824
Fatty acid synthaseGallus gallus (chicken)IC5013.000011
Fatty acid synthaseHomo sapiens (human)IC5013.553333
Fatty-acid amide hydrolase 1Mus musculus (house mouse)IC500.080011
Folate receptor alphaHomo sapiens (human)IC500.2936612
Folate receptor betaHomo sapiens (human)IC500.2185610
Folylpolyglutamate synthase, mitochondrialHomo sapiens (human)IC503.200011
Folylpolyglutamate synthase, mitochondrialMus musculus (house mouse)Ki166.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki113.000012
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki113.000012
Genome polyprotein Human rhinovirus sp.IC502,500.000011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki91.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC504.835022
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC502.300011
Histamine H3 receptorCavia porcellus (domestic guinea pig)IC508.690011
Histidine decarboxylaseRattus norvegicus (Norway rat)IC500.001411
Histone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)IC5044.000011
Janus kinase 2 (a protein tyrosine kinase)Homo sapiens (human)IC506.798011
Kappa-type opioid receptorRattus norvegicus (Norway rat)IC500.003011
Mitogen-activated protein kinase 3 Homo sapiens (human)IC505.516011
Mu-type opioid receptorRattus norvegicus (Norway rat)IC500.003011
Multidrug resistance associated proteinHomo sapiens (human)Ki1,200.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.0000117
MyeloperoxidaseHomo sapiens (human)IC502.810011
NADH-cytochrome b5 reductase 3 Homo sapiens (human)IC50279.400011
Nicotinamide N-methyltransferaseHomo sapiens (human)IC503.620011
NPC1-like intracellular cholesterol transporter 1Homo sapiens (human)IC500.370011
NPC1-like intracellular cholesterol transporter 1Rattus norvegicus (Norway rat)Ki0.200011
nuclear receptor coactivator 1 isoform 1 [Homo sapiens]Homo sapiens (human)IC5032.448323
nuclear receptor coactivator 3 isoform aHomo sapiens (human)IC5014.541023
Nuclear receptor ROR-gammaMus musculus (house mouse)IC5011.100011
Orotidine 5'-phosphate decarboxylaseMethanothermobacter thermautotrophicus str. Delta HKi8.600012
Orotidine 5'-phosphate decarboxylaseSaccharomyces cerevisiae S288CKi0.064011
Phosphatidylinositol 4-kinase alphaHomo sapiens (human)IC50341.600011
Phosphatidylinositol 4-kinase alphaHomo sapiens (human)Ki235.400011
Phosphatidylinositol 4-kinase betaHomo sapiens (human)IC50341.600011
Phosphatidylinositol 4-kinase betaHomo sapiens (human)Ki235.400011
Phosphatidylinositol 4-kinase type 2-alphaHomo sapiens (human)IC50341.600011
Phosphatidylinositol 4-kinase type 2-alphaHomo sapiens (human)Ki235.400011
Phosphatidylinositol 4-kinase type 2-betaHomo sapiens (human)IC50341.600011
Phosphatidylinositol 4-kinase type 2-betaHomo sapiens (human)Ki235.400011
Polyphenol oxidase 2Agaricus bisporusIC501,000.000011
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC5016.159011
Programmed cell death protein 4Homo sapiens (human)IC500.880011
Prostaglandin G/H synthase 1Homo sapiens (human)IC508.421512
Protease Human immunodeficiency virus 1IC5010.509045
Protein kinase C beta typeHomo sapiens (human)IC50150.000011
Protein kinase C epsilon typeHomo sapiens (human)IC50150.000011
Protein-arginine deiminase type-4Homo sapiens (human)IC509,050.000012
Proton-coupled amino acid transporter 1Homo sapiens (human)Ki4,400.000011
Proton-coupled folate transporterHomo sapiens (human)IC500.051658
Proton-coupled folate transporterHomo sapiens (human)Ki0.677677
Pteridine reductase 1Leishmania majorKi0.109522
Purine nucleoside phosphorylaseHomo sapiens (human)Ki135.500022
Reduced folate transporterHomo sapiens (human)IC500.061158
Reduced folate transporterHomo sapiens (human)Ki3.500011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5018.400044
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5015.86312526
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Ki0.051011
Ribonucleoside-diphosphate reductase large subunitHomo sapiens (human)IC50997.000011
RNA-directed RNA polymerase IC5015.400022
Serine hydroxymethyltransferase, cytosolicHomo sapiens (human)Ki79.233333
Shiga toxin subunit AShigella dysenteriaeIC5023.900011
Sodium/bile acid cotransporterHomo sapiens (human)Ki25.000011
Sodium/nucleoside cotransporter 2Homo sapiens (human)IC501,000.000011
Solute carrier family 15 member 1Homo sapiens (human)IC5012,210.000011
Solute carrier family 22 member 20Mus musculus (house mouse)Ki599.780012
Solute carrier family 22 member 6Mus musculus (house mouse)Ki896.125512
Steroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)IC5010.000011
Sterol 14-alpha demethylaseTrypanosoma cruzi strain CL BrenerIC50100.000011
Thymidine kinaseHuman alphaherpesvirus 1 (Herpes simplex virus type 1)IC50561.000022
Thymidine kinaseHuman alphaherpesvirus 1 strain SC16IC501,000.000011
Thymidine kinaseHuman herpesvirus 3 strain DumasIC501,000.000022
Thymidine kinaseUreaplasma parvum serovar 3 str. ATCC 700970IC5012.500011
Thymidine kinase Human alphaherpesvirus 2IC50200.000011
Thymidine kinase Macacine alphaherpesvirus 1IC50501.000012
Thymidine kinase Staphylococcus aureusKi944.000011
Thymidine kinase 2 Rattus norvegicus (Norway rat)Ki3,250.000011
Thymidine kinase 2, mitochondrialHomo sapiens (human)IC501,000.000022
Thymidine kinase, cytosolicHomo sapiens (human)IC50667.666733
Thymidine kinase, cytosolicHomo sapiens (human)Ki205.826746
Thymidine kinase, cytosolic Rattus norvegicus (Norway rat)Ki1,700.000011
Thymidylate kinaseHomo sapiens (human)Ki214.000011
Thymidylate kinaseMycobacterium tuberculosis H37RvKi124.333346
Thymidylate synthaseEscherichia coli K-12IC5011.4303312
Thymidylate synthaseHomo sapiens (human)IC5024.50312843
Thymidylate synthaseLacticaseibacillus caseiIC50121.21431414
Thymidylate synthaseMus musculus (house mouse)IC506.40611622
Thymidylate synthaseHomo sapiens (human)Ki0.235644
Thymidylate synthaseLacticaseibacillus caseiKi0.550011
Thymidylate synthaseMus musculus (house mouse)Ki22.670022
Thymidylate synthase Escherichia coliIC50110.68121316
Thymidylate synthase Escherichia coli LF82IC5047.000012
Thymidylate synthase Rattus norvegicus (Norway rat)IC5020.000011
Thyroid peroxidaseHomo sapiens (human)IC503.380011
Toll-like receptor 4Homo sapiens (human)IC501.040011
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC5014.000011
transactivating tegument protein VP16 [Human herpesvirus 1]Human alphaherpesvirus 1 (Herpes simplex virus type 1)IC5029.335023
Transcriptional activator protein LasRPseudomonas aeruginosa PAO1IC500.640011
Trifunctional purine biosynthetic protein adenosine-3Homo sapiens (human)IC506.272678
Trifunctional purine biosynthetic protein adenosine-3Mus musculus (house mouse)IC5020.000055
Trifunctional purine biosynthetic protein adenosine-3Homo sapiens (human)Ki0.611344
UDP-glucose 6-dehydrogenaseRattus norvegicus (Norway rat)Ki288.000011
UDP-glucose 6-dehydrogenaseStreptococcus pyogenesKi199.500022
UDP-glucuronosyltransferase 1A1 Rattus norvegicus (Norway rat)Ki100.000011
UDP-N-acetylmuramoyl-tripeptide--D-alanyl-D-alanine ligase Staphylococcus epidermidis RP62AIC50300.000011
Urease subunit alphaHelicobacter pylori 26695IC50100.000011
Urease subunit betaHelicobacter pylori 26695IC50100.000011
Uridine 5'-monophosphate synthaseHomo sapiens (human)Ki0.017011
Voltage-dependent calcium channel subunit alpha-2/delta-1Mus musculus (house mouse)Ki0.102412
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50622.500011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50622.500011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50622.500011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50622.500011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC5013.75204242
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC5017.43564042
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Ki1.800022
Xanthine dehydrogenase/oxidaseHomo sapiens (human)Ki2.891766
Xanthine dehydrogenase/oxidase [Includes: Xanthine dehydrogenase Rattus norvegicus (Norway rat)IC509.317733

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinaseEscherichia coli K-12Kd18.000011
Adenosine receptor A2aHomo sapiens (human)Kd77.000011
AlbuminHomo sapiens (human)Kd44.000014
Angiotensin-converting enzyme 2 Homo sapiens (human)EC5038.553313
C-X-C chemokine receptor type 4Homo sapiens (human)EC500.088011
Carbonic anhydrase 2Homo sapiens (human)EC500.001011
Chain A, Calmodulin-sensitive adenylate cyclaseBacillus anthracisKd130.000011
Chain A, RIO-type serine/threonine-protein kinase Rio1Archaeoglobus fulgidusKd0.040011
Chain B, DIHYDROFOLATE REDUCTASEEscherichia coliKd0.134415
Cyclin-dependent kinase 2Homo sapiens (human)EC500.001011
Dihydrofolate reductaseEscherichia coli K-12EC500.001011
Dihydrofolate reductaseEscherichia coli K-12Kd0.30621010
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)EC500.055011
Estrogen receptorRattus norvegicus (Norway rat)EC50150.000012
Estrogen receptor betaRattus norvegicus (Norway rat)EC50150.000012
Genome polyproteinHuman enterovirus 71 (strain BRCR)EC50100.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)EC5010.525022
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)EC502.950011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50300.000012
Heat shock cognate 71 kDa proteinHomo sapiens (human)Kd59.346214
heat shock protein 90Candida albicansEC50150.000011
High mobility group protein B1Homo sapiens (human)Kd0.262022
Histamine H1 receptorCavia porcellus (domestic guinea pig)EC5046.000011
Hsf1 proteinMus musculus (house mouse)EC503.057011
NS5 Zika virusEC505.200055
Nuclear hormone receptor family member daf-12Caenorhabditis elegansEC5067.526011
oxysterols receptor LXR-beta isoform 1Homo sapiens (human)EC5067.526011
Polymerase acidic proteinInfluenza A virus (A/Puerto Rico/8/1934(H1N1))EC5021.266733
Polymerase basic protein 2Influenza A virus (A/Puerto Rico/8/1934(H1N1))EC5020.000022
Procathepsin LHomo sapiens (human)EC5038.553313
Protease Human immunodeficiency virus 1EC500.126011
Purine nucleoside phosphorylaseMycobacterium tuberculosis H37RvKd364.007313
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC5038.553313
Replicase polyprotein 1abBetacoronavirus England 1EC5038.553313
Replicase polyprotein 1abHuman coronavirus 229EEC5038.553313
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC5038.553313
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC5038.553313
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC500.96652527
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Kd0.005411
RNA-directed RNA polymerase EC5046.000011
RNA-directed RNA polymerase catalytic subunitInfluenza A virus (A/Puerto Rico/8/1934(H1N1))EC5021.266733
Serine hydroxymethyltransferase, cytosolicHomo sapiens (human)Kd16.900011
Spike glycoproteinBetacoronavirus England 1EC5038.553313
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC5038.553313
streptokinase A precursorStreptococcus pyogenes M1 GASEC5051.859023
Stromelysin-1Homo sapiens (human)Kd25,000.000011
SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, isoform CRA_aHomo sapiens (human)EC5091.170011
Taste receptor type 2 member 38Homo sapiens (human)EC502.000011
Transmembrane protease serine 2Homo sapiens (human)EC5038.553313
Tyrosine-protein kinase ABL1Homo sapiens (human)EC500.001011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Kd0.000511

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)ID500.050011
AAA family ATPase Staphylococcus aureusKm192.000011
AdenosylhomocysteinaseHomo sapiens (human)Kinact266.000011
AdenosylhomocysteinaseHomo sapiens (human)KR407.000011
ATP-binding cassette sub-family C member 11Homo sapiens (human)Km957.000011
ATP-binding cassette sub-family C member 3Rattus norvegicus (Norway rat)Km8.100022
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)Km2,560.000033
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Km296.000011
Carbonic anhydrase 2Homo sapiens (human)Kinact28.000011
Carbonic anhydrase 9Homo sapiens (human)Kinact23.000011
Cytidine deaminaseHomo sapiens (human)Km359.333366
Deoxycytidine kinaseHomo sapiens (human)Km2.196733
Dihydrofolate reductaseHomo sapiens (human)IC801.440011
Dihydrofolate reductaseLacticaseibacillus caseiID500.013055
Dihydrofolate reductaseMus musculus (house mouse)ID500.017166
Ectonucleoside triphosphate diphosphohydrolase 1Bos taurus (cattle)Km2.900011
Folylpolyglutamate synthase, mitochondrialMus musculus (house mouse)Concentration47.000012
Folylpolyglutamate synthase, mitochondrialHomo sapiens (human)Km71.333333
Folylpolyglutamate synthase, mitochondrialMus musculus (house mouse)Km165.000011
Folylpolyglutamate synthase, mitochondrialHomo sapiens (human)Vmax0.820011
Hsf1 proteinMus musculus (house mouse)AC506.831022
HSP40, subfamily A [Plasmodium falciparum 3D7]Plasmodium falciparum 3D7AbsAC1000_uM6.281012
Hypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)Km38.092927
interferon gamma precursorHomo sapiens (human)AC500.346011
Liver carboxylesterase 1Homo sapiens (human)Km1,300.000011
LMP1 [Human herpesvirus 4]human gammaherpesvirus 4 (Epstein-Barr virus)AbsAC35_uM7.240011
LMP1 [Human herpesvirus 4]human gammaherpesvirus 4 (Epstein-Barr virus)AC501.118024
Microphthalmia-associated transcription factorHomo sapiens (human)AC500.875033
MSHDrosophila melanogaster (fruit fly)AC503.980011
Multidrug resistance associated proteinHomo sapiens (human)Km768.666733
Multidrug resistance-associated protein 1 Homo sapiens (human)Km1,540.000022
Multidrug resistance-associated protein 4Homo sapiens (human)Km1,300.000011
PAX8Homo sapiens (human)AC500.566733
POU domain, class 2, transcription factor 2Homo sapiens (human)Km94.000011
Probable deoxycytidylate deaminaseCaenorhabditis elegansKm160.000011
Proton-coupled folate transporterHomo sapiens (human)K0.157022
Reverse transcriptase/RNaseH Human immunodeficiency virus 1CC5067.000012
Reverse transcriptase/RNaseH Human immunodeficiency virus 1CD5070.000011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED500.026733
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC900.100011
Skn7pSaccharomyces cerevisiae (brewer's yeast)AbsAC40_uM5.101012
Solute carrier family 22 member 1 Homo sapiens (human)Km151.200011
Solute carrier family 22 member 11Homo sapiens (human)Km84.800022
Solute carrier family 22 member 6Homo sapiens (human)Km445.250034
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Km155.000012
Solute carrier family 22 member 7Homo sapiens (human)Km26.800011
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Km1,513.000012
Solute carrier family 22 member 8Homo sapiens (human)Km237.275044
Solute carrier family 22 member 8Mus musculus (house mouse)Km2.031912
Solute carrier organic anion transporter family member 1A3Rattus norvegicus (Norway rat)Km29.100045
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km24.700011
Taste receptor type 2 member 38Homo sapiens (human)Activity0.300011
Thymidine kinaseUreaplasma parvum serovar 3 str. ATCC 700970Km2.700011
Thymidine kinaseVaccinia virus WRKm71.500012
Thymidine kinase Staphylococcus aureusKm11.600011
Thymidine kinase, cytosolicHomo sapiens (human)Km24.350066
Thymidine kinase, cytosolic Rattus norvegicus (Norway rat)Phosphorylation rate4.000011
Thymidine phosphorylaseHomo sapiens (human)Km516.666713
Thymidylate synthaseMus musculus (house mouse)ED500.030011
Thymidylate synthaseMus musculus (house mouse)ID500.035011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km64.000011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km42.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km395.500012
Uridine phosphorylase 1Homo sapiens (human)Km6,000.000011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Km58.375044