Page last updated: 2024-08-05 14:42:33

alkylating agent

Highly reactive chemical that introduces alkyl radicals into biologically active molecules and thereby prevents their proper functioning. It could be used as an antineoplastic agent, but it might be very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. It could also be used as a component of poison gases.

ChEBI ID: 22333

Members (52)

MemberDefinitionClass
1,2-dimethylhydrazineA member of the class of hydrazines that is hydrazine in which one of the hydrogens attached to each nitrogen is replaced by a methyl group. A powerful DNA alkylating agent and carcinogen, it is used to induce colon cancer in laboratory rats and mice.1,2-dimethylhydrazine
4-hydroxycyclophosphamideA phosphorodiamide that consists of 2-amino-1,3,2-oxazaphosphinan-4-ol 2-oxide having two 2-chloroethyl groups attached to the exocyclic nitrogen.4-hydroxycyclophosphamide
5-(3-methyl-1-triazeno)imidazole-4-carboxamideA monocarboxylic acid amide that is dacarbazine in which one of the methyl groups is replaced by a hydrogen. It is the active metabolite of dacarbazine, and is also produced by spontaneous hydrolysis of temozolomide in the body.MTIC
acrylamideA member of the class of acrylamides that results from the formal condensation of acrylic acid with ammonia.acrylamide
aziridineaziridine
bis(chloromethyl) etherAn ether that is dimethyl ether in which one of the hydrogens attached to each of the methyl group has replaced by a chlorine.bis(chloromethyl) ether
bromoethaneA bromoalkane that is ethane carrying a bromo substituent. It is an alkylating agent used as a chemical intermediate in various organic syntheses.bromoethane
bromopyruvateA 2-oxo monocarboxylic acid that is pyruvic acid in which one of the methyl hydrogens is replaced by bromine. Synthetic brominated derivative and structural analog of pyruvic acid. Highly reactive alkylating agent. Anti-cancer drug3-bromo-2-oxopropanoic acid; 3-bromopyruvic acid
busulfanA methanesulfonate ester that is butane-1,4-diol in which the hydrogens of the hydroxy groups are replaced by methanesulfonyl groups. An alkylating antineoplastic agent, it is used for the treatment of chronic myeloid leukemia (although it has been largely replaced by newer drugs). It is also used as an insect sterilant.busulfan
carmustineA member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.carmustine
chlorambucilA monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.chlorambucil
chloroacetic acidA chlorocarboxylic acid that is acetic acid carrying a 2-chloro substituent.chloroacetic acid
colibactinA member of the class of 1,3-thiazoles that comprises of two units of 2-[(2-{6-[(2S)-2-methyl-3,4-dihydro-2H-pyrrol-5-yl]-5-oxo-4-azaspiro[2.4]hept-6-en-7-yl}acetamido)methyl]-1,3-thiazole-4-carboxylic acid linked together via the formal condensation of the carboxy groups. It is a secondary metabolite produced by certain strains of bacteria found in the human gut such as Escherichia coli. It has the ability to bind covalently to DNA and is strongly associated with colorectal cancer.colibactin
cyclophosphamideThe monohydrate of cyclophosphamide.cyclophosphamide hydrate
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
dehydroalanineA 2,3-dehydroamino acid that is alanine which has been dehydrogenated to introduce a double bond between positions 2 and 3.2-aminoacrylic acid; 2-ammonioprop-2-enoate
diaziquoneA 1,4-benzoquinone that is substituted at positions 2 and 5 have been replaced by aziridin-1-yl groups and at positions 3 and 6 by (ethoxycarbonyl)amino groups.diaziquone
diazomethaneThe simplest diazo compound, in which a diazo group is attached to a methylene group.diazomethane
diethyl sulfateThe diethyl ester of sulfuric acid.diethyl sulfate
dimethyl sulfateThe dimethyl ester of sulfuric acid.dimethyl sulfate
dimethyl sulfoxideA 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.dimethyl sulfoxide
dimethylmyleranA methanesulfonate ester that is hexane-2,5-diol in which the hydrogens of the hydroxy groups are replaced by methanesulfonyl groups.dimethylmyleran
ecteinascidin 743A tetrahydroisoquinoline alkaloid obtained from a Caribbean tunicate Ecteinascidia turbinata. Used for the treatment of soft tissue sarcoma and relapsed ovarian cancer.trabectedin
estramustineA carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.estramustine
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
ethyl methanesulfonateA methanesulfonate ester resulting from the formal condensation of methanesulfonic acid with ethanol.ethyl methanesulfonate
ethylenimine quinoneA member of the class of 1,4-benzoquinones that is p-benzoquinone in which the hydrogens at positions 2 and 5 are replaced by aziridin-1-yl groups.2,5-bis(aziridin-1-yl)-1,4-benzoquinone
ethylnitrosoureaA member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by ethyl and nitroso groups.N-ethyl-N-nitrosourea
hycanthone methanesulfonateA methanesulfonate salt resulting from the reaction of equimolar amounts of hycanthone and methanesulfonic acid. It was formerly used as a schistosomicide for individual or mass treatement of infection with Schistosoma haematobium and S. mansoni, but due to its toxicity and concern about possible carcinogenicity, it has been replaced by other drugs such as praziquantel.hycanthone mesylate
ifosfamideThe simplest member of the class of ifosfamides that is 1,3,2-oxazaphosphinan-2-amine 2-oxide substituted by 2-chloroethyl groups on both the nitrogen atoms respectively. It is a nitrogen mustard alkylating agent used in the treatment of advanced breast cancer.ifosfamide
iodoacetic acidA haloacetic acid that is acetic acid in which one of the hydrogens of the methyl group is replaced by an iodine atom.iodoacetic acid
lomustineAn N-nitrosourea that is urea in which one of the nitrogens is substituted by a 2-chloroethyl group and by a nitroso group, while the other nitrogen is substituted by a cyclohexyl group. An alkylating antineoplastic agent, it is used in the treatment of brain tumours, lung cancer, malignant melanoma and other solid tumours.lomustine
mechlorethaminemechlorethamine
melphalanA phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.melphalan
methyl methanesulfonateA methanesulfonate ester resulting from the formal condensation of methanesulfonic acid with methanol.methyl methanesulfonate
methylnitronitrosoguanidineAn N-nitroguanidine compound having nitroso and methyl substituents at the N'-positionN-methyl-N'-nitro-N-nitrosoguanidine
methylnitrosoureaA member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.N-methyl-N-nitrosourea
mitomycinmitomycin C
mitomycin aA member of the family of mitomycins that exhibits antibiotic and antitumour properties as well as a high level of toxicity.mitomycin A
mustard gasAn ethyl sulfide that is diethyl sulfide in which a hydrogen from each of the terminal methyl groups is replaced by a chlorine. It is a powerful vesicant regulated under the Chemical Weapons Convention.bis(2-chloroethyl) sulfide
nimustineAn organochlorine compound that is urea in which the two hydrogens on one of the amino groups are replaced by nitroso and 2-chloroethyl groups and one hydrogen from the other amino group is replaced by a 4-amino-2-methylpyrimidin-5-ylmethyl] group. An antineoplastic agent especially effective against malignant brain tumors.nimustine
nsc 224070A member of the class of 1,4-benzoquinones that is 1,4-benzoquinone in which the hydrogens at positions 2 and 5 have been replaced by aziridin-1-yl groups while the hydrogens at positions 3 and 6 have been replaced by (2-hydroxyethyl)amino groups.2,5-bis(2-hydroxyethylamino)-3,6-diaziridinylbenzoquinone
perfosfamideA phosphorodiamide that is the active metabolite of the nitrogen mustard cyclophosphamide. It has potent antineoplastic and immunosuppressive properties.4-hydroperoxycyclophosphamide
pipobromanAn N-acylpiperazine that is piperazine in which each of the nitrogens has been acylated by a 3-bromopropionoyl group. An anti-cancer drug.pipobroman
s-chloromethylglutathioneAn S-substituted glutathione that is glutathione in which the mercapto hydrogen has been replaced by a chloromethyl group.S-(chloromethyl)glutathione
semustineAn organochlorine compound that is urea in which the two hydrogens on one of the amino groups are replaced by nitroso and 2-chloroethyl groups and one hydrogen from the other amino group is replaced by a 4-methylcyclohexyl group.semustine
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
tilimycinA pyrrolobenzodiazepine that is (11aS)-2,3,5,10,11,11a-hexahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine which is substituted by an oxo group at position 5 and by hydroxy groups at positions 9 and 11. It is an enterotoxic natural product synthesized via a non-ribosomal peptide synthase in Klebsiella oxytoca.tilimycin
tosylphenylalanyl chloromethyl ketoneThe N-tosyl derivative of L-phenylalanyl chloromethyl ketone.N-tosyl-L-phenylalanyl chloromethyl ketone
triaziquoneA member of the class of 1,4-benzoquinones that is 1,4-benzoquinone in which three of the ring hydrogens are replaced by aziridin-1-yl groups.triaziquone
triethylenemelaminetretamine
trimethyl phosphiteAn organophosphorus compound that is phosphane in which the three hydrogens are replaced by methoxy groups. It is an alkylating agent used primarily in the synthesis of organophosphate compounds.trimethyl phosphite

Research

Studies (86,633)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199029,611 (34.18)18.7374
1990's16,430 (18.97)18.2507
2000's17,048 (19.68)29.6817
2010's17,616 (20.33)24.3611
2020's5,928 (6.84)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials9,000 (9.15%)5.53%
Reviews5,705 (5.80%)6.00%
Case Studies6,628 (6.74%)4.05%
Observational161 (0.16%)0.25%
Other76,878 (78.15%)84.16%

Protein Targets (216)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency25.848713
15-lipoxygenase, partialHomo sapiens (human)Potency34.352113
67.9K proteinVaccinia virusPotency6.596723
acetylcholinesteraseHomo sapiens (human)Potency18.282423
activating transcription factor 6Homo sapiens (human)Potency26.773727
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency13.6311215
Alpha-synucleinHomo sapiens (human)Potency17.358212
Amyloid-beta precursor proteinHomo sapiens (human)Potency16.360111
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency17.406913
AR proteinHomo sapiens (human)Potency21.18411242
aryl hydrocarbon receptorHomo sapiens (human)Potency24.5239212
arylsulfatase AHomo sapiens (human)Potency0.132412
ATAD5 protein, partialHomo sapiens (human)Potency19.992234
Ataxin-2Homo sapiens (human)Potency34.139826
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency13.334034
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency42.296328
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency11.995511
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency5.847911
Bloom syndrome protein isoform 1Homo sapiens (human)Potency17.3040310
BRCA1Homo sapiens (human)Potency5.011911
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency56.234111
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.848015
caspase-3Cricetulus griseus (Chinese hamster)Potency33.491511
caspase-3Homo sapiens (human)Potency33.848015
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency23.3970332
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency13.698223
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency21.964013
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency8.134911
Chain A, Beta-lactamaseEscherichia coli K-12Potency8.764912
Chain A, CruzipainTrypanosoma cruziPotency10.113437
Chain A, HADH2 proteinHomo sapiens (human)Potency39.810711
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.125111
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.832612
Chain A, PAPAINCarica papaya (papaya)Potency15.848911
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency23.809223
Chain B, HADH2 proteinHomo sapiens (human)Potency39.810711
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency52.508524
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.506012
cytochrome P450 2C9 precursorHomo sapiens (human)Potency19.952611
cytochrome P450 2C9, partialHomo sapiens (human)Potency29.108613
cytochrome P450 2D6Homo sapiens (human)Potency13.960416
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency1.834127
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.7491211
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.006019
D(1A) dopamine receptorHomo sapiens (human)Potency10.000011
D(1A) dopamine receptorSus scrofa (pig)Potency20.749111
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency13.899313
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency19.952611
DNA polymerase eta isoform 1Homo sapiens (human)Potency100.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency68.324713
DNA polymerase kappa isoform 1Homo sapiens (human)Potency15.052412
endonuclease IVEscherichia coliPotency8.539812
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.50431271
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency22.442536
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency30.0005737
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.7677115
EWS/FLI fusion proteinHomo sapiens (human)Potency14.5366430
farnesoid X nuclear receptorHomo sapiens (human)Potency30.690447
flap endonuclease 1Homo sapiens (human)Potency8.436811
Fumarate hydrataseHomo sapiens (human)Potency23.069417
GVesicular stomatitis virusPotency29.108613
GABA theta subunitRattus norvegicus (Norway rat)Potency1.612714
GALC proteinHomo sapiens (human)Potency0.707912
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency1.612714
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency1.612714
gemininHomo sapiens (human)Potency10.3370319
GLI family zinc finger 3Homo sapiens (human)Potency30.0425216
glp-1 receptor, partialHomo sapiens (human)Potency7.811712
GLS proteinHomo sapiens (human)Potency27.397913
glucocerebrosidaseHomo sapiens (human)Potency39.810711
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency22.4075411
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency13.529013
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.481311
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency47.990412
heat shock protein beta-1Homo sapiens (human)Potency57.265722
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.952613
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency5.546213
Histone H2A.xCricetulus griseus (Chinese hamster)Potency44.1226214
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency29.108613
huntingtin isoform 2Homo sapiens (human)Potency35.481312
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency20.394412
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency18.008739
IDH1Homo sapiens (human)Potency13.278012
importin subunit beta-1 isoform 1Homo sapiens (human)Potency125.892011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency29.108616
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.589311
Integrin alpha-IIbHomo sapiens (human)Potency6.309611
Integrin beta-3Homo sapiens (human)Potency6.309611
Interferon betaHomo sapiens (human)Potency24.3372313
interleukin 8Homo sapiens (human)Potency63.589614
lamin isoform A-delta10Homo sapiens (human)Potency8.6593212
lethal factor (plasmid)Bacillus anthracis str. A2012Potency17.538415
LuciferasePhotinus pyralis (common eastern firefly)Potency36.064235
Microtubule-associated protein tauHomo sapiens (human)Potency18.787028
mitogen-activated protein kinase 1Homo sapiens (human)Potency10.055612
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency30.383424
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency64.091912
neuropeptide S receptor isoform AHomo sapiens (human)Potency16.271012
NFKB1 protein, partialHomo sapiens (human)Potency4.038226
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency11.397412
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency46.5626425
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency11.009512
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency27.299512
Nuclear receptor ROR-gammaHomo sapiens (human)Potency66.084414
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency23.543324
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency14.168414
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency16.3445317
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency19.952611
ParkinHomo sapiens (human)Potency20.596211
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency12.114024
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency58.445514
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.8321516
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency34.630337
phosphopantetheinyl transferaseBacillus subtilisPotency5.623411
plasminogen precursorMus musculus (house mouse)Potency4.978815
polyproteinZika virusPotency23.069417
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency23.049915
PPM1D proteinHomo sapiens (human)Potency21.751516
pregnane X nuclear receptorHomo sapiens (human)Potency47.3277310
pregnane X receptorRattus norvegicus (Norway rat)Potency35.481311
progesterone receptorHomo sapiens (human)Potency16.606825
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency89.125111
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.2324222
ras-related protein Rab-9AHomo sapiens (human)Potency73.078011
regulator of G-protein signaling 4Homo sapiens (human)Potency12.651112
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency43.0062330
retinoid X nuclear receptor alphaHomo sapiens (human)Potency1,131.7935318
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.751144
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency11.917311
Smad3Homo sapiens (human)Potency17.520313
snurportin-1Homo sapiens (human)Potency125.892011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency19.270325
survival motor neuron protein isoform dHomo sapiens (human)Potency15.605716
TAR DNA-binding protein 43Homo sapiens (human)Potency23.422113
TDP1 proteinHomo sapiens (human)Potency9.0749234
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.154813
thioredoxin reductaseRattus norvegicus (Norway rat)Potency38.1053313
ThrombopoietinHomo sapiens (human)Potency10.000024
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency20.0554323
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency17.126333
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.7412418
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency13.899313
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency4.978815
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency4.978815
USP1 protein, partialHomo sapiens (human)Potency49.341235
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency35.473629
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency13.745038
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency22.314759
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency13.529013
WRNHomo sapiens (human)Potency50.118711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC501.884522
Alcohol dehydrogenase E chainEquus caballus (horse)Ki7,762.470011
Alcohol dehydrogenase S chainEquus caballus (horse)Ki7,762.470011
Alpha-2A adrenergic receptorHomo sapiens (human)IC504.809011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki1.803011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000017
Bile salt export pumpHomo sapiens (human)IC50260.9200413
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000017
Carbonic anhydrase 1Homo sapiens (human)Ki50.000012
Carbonic anhydrase 12Homo sapiens (human)Ki50.000012
Carbonic anhydrase 2Homo sapiens (human)Ki50.000012
Carbonic anhydrase 9Homo sapiens (human)Ki50.000012
Cathepsin GHomo sapiens (human)IC50110.000011
Cereblon isoform 4Magnetospirillum gryphiswaldenseIC5020.800011
Cereblon isoform 4Magnetospirillum gryphiswaldenseKi5,570.233333
Choline O-acetyltransferase Rattus norvegicus (Norway rat)Ki25,000.000011
ChymaseHomo sapiens (human)IC503.300011
Chymotrypsin-like elastase family member 2ASus scrofa (pig)IC5048.000011
Chymotrypsinogen ABos taurus (cattle)IC50140.000011
Cyclin-dependent kinase 8Homo sapiens (human)IC5012.500022
Cytochrome P450 2D6Homo sapiens (human)IC5065.100011
Fibroblast growth factor receptor 4Homo sapiens (human)IC500.938011
Glutathione reductaseSaccharomyces cerevisiae S288CIC50441.000011
Glutathione reductase, mitochondrialHomo sapiens (human)IC508.100011
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)Ki25.000011
Isocitrate lyase 1Mycobacterium tuberculosis CDC1551IC5017.500011
Large neutral amino acids transporter small subunit 1 Rattus norvegicus (Norway rat)Ki55.000011
Matrix metalloproteinase-9Homo sapiens (human)IC505.215011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000017
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC503.800011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC503.800011
perilipin-1Homo sapiens (human)IC501.868011
perilipin-5Homo sapiens (human)IC501.901011
polyadenylate-binding protein 1Homo sapiens (human)IC5054.725022
Protein cereblonHomo sapiens (human)IC50264.000011
Protein cereblonHomo sapiens (human)Ki68,568.500022
protein-arginine deiminase type-4Homo sapiens (human)IC5013.000011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC501.370011
Serum paraoxonase/arylesterase 1Homo sapiens (human)Ki8,973.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC5080.700011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki37.400011
TPA: protein transporter TIM10Saccharomyces cerevisiae S288CIC500.640011
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC502.180011
Transcription factor p65Homo sapiens (human)IC503.800011
TrypsinSus scrofa (pig)IC50200.000011
Tyrosine-protein kinase ABL1Homo sapiens (human)IC50100.000011
Tyrosine-protein kinase ABL2Homo sapiens (human)IC50100.000011
Tyrosine-protein phosphatase non-receptor type 11Homo sapiens (human)IC50300.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Insulin-like growth factor-binding protein 5Homo sapiens (human)Kd696,000.000077
recombinase AMycobacterium tuberculosis H37RvEC501.287522

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.005011
PAX8Homo sapiens (human)AC505.340011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC50162.666022