Page last updated: 2024-08-05 15:23:02

EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor

An EC 1.3.98.* (oxidoreductase acting on CH-CH group of donors, with other, known, acceptors) inhibitor that interferes with the action of dihydroorotate oxidase (fumarate), EC 1.3.98.1 (formerly EC 1.3.3.1).

ChEBI ID: 68542

Members (2)

MemberDefinitionClass
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
teriflunomideAn enamide obtained by formal condensation of the carboxy group of (2Z)-2-cyano-3-hydroxybut-2-enoic acid with the anilino group of 4-(trifluoromethyl)aniline. Used for the treatment of relapsing forms of multiple sclerosis and rheumatoid arthritis.teriflunomide

Research

Studies (1,997)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19907 (0.35)18.7374
1990's234 (11.72)18.2507
2000's669 (33.50)29.6817
2010's768 (38.46)24.3611
2020's319 (15.97)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials223 (9.76%)5.53%
Reviews419 (18.33%)6.00%
Case Studies330 (14.44%)4.05%
Observational36 (1.57%)0.25%
Other1,278 (55.91%)84.16%

Protein Targets (123)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency48.508812
activating transcription factor 6Homo sapiens (human)Potency54.941022
AR proteinHomo sapiens (human)Potency13.1146916
aryl hydrocarbon receptorHomo sapiens (human)Potency7.609724
arylsulfatase AHomo sapiens (human)Potency37.933011
ATAD5 protein, partialHomo sapiens (human)Potency8.658844
Ataxin-2Homo sapiens (human)Potency3.902212
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency3.902224
Bloom syndrome protein isoform 1Homo sapiens (human)Potency28.183822
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency1.805812
caspase-3Homo sapiens (human)Potency1.805812
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.000023
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.848911
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.622811
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.802911
cytochrome P450 2D6Homo sapiens (human)Potency24.545411
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency2.821424
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.467111
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency2.745412
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency25.118911
Endothelin receptor type BRattus norvegicus (Norway rat)Potency17.782811
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency17.782811
estrogen nuclear receptor alphaHomo sapiens (human)Potency5.7544711
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency2.74601016
EWS/FLI fusion proteinHomo sapiens (human)Potency16.136244
farnesoid X nuclear receptorHomo sapiens (human)Potency54.941011
Fumarate hydrataseHomo sapiens (human)Potency11.770411
GVesicular stomatitis virusPotency13.802911
GABA theta subunitRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency2.821412
gemininHomo sapiens (human)Potency1.871422
GLI family zinc finger 3Homo sapiens (human)Potency12.695636
glp-1 receptor, partialHomo sapiens (human)Potency14.125411
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency4.896611
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency7.040312
heat shock protein beta-1Homo sapiens (human)Potency29.194522
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.622813
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
histone deacetylase 9 isoform 3Homo sapiens (human)Potency1.756124
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.802911
huntingtin isoform 2Homo sapiens (human)Potency2.969822
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency61.644811
IDH1Homo sapiens (human)Potency14.581011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.802912
Integrin alpha-IIbHomo sapiens (human)Potency10.000011
Integrin beta-3Homo sapiens (human)Potency10.000011
Interferon betaHomo sapiens (human)Potency18.268938
lamin isoform A-delta10Homo sapiens (human)Potency7.064312
LuciferasePhotinus pyralis (common eastern firefly)Potency22.367034
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency17.015722
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.079411
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency31.622811
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency1.199012
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency23.168624
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency2.059611
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency54.941011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.481311
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency3.981111
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency1.018636
P53Homo sapiens (human)Potency56.234111
ParkinHomo sapiens (human)Potency1.636011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency1.383922
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency37.933011
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency48.966211
phosphopantetheinyl transferaseBacillus subtilisPotency39.810711
plasminogen precursorMus musculus (house mouse)Potency8.912511
polyproteinZika virusPotency11.770411
PPM1D proteinHomo sapiens (human)Potency18.556914
pregnane X nuclear receptorHomo sapiens (human)Potency4.800423
progesterone receptorHomo sapiens (human)Potency61.130611
pyruvate kinaseLeishmania mexicana mexicanaPotency17.782822
RAR-related orphan receptor gammaMus musculus (house mouse)Potency1.394224
ras-related protein Rab-9AHomo sapiens (human)Potency1.071612
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency5.763337
retinoid X nuclear receptor alphaHomo sapiens (human)Potency39.153322
survival motor neuron protein isoform dHomo sapiens (human)Potency12.879526
TDP1 proteinHomo sapiens (human)Potency4.362926
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.631011
ThrombopoietinHomo sapiens (human)Potency7.943322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency4.422524
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency44.668411
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency8.912511
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency8.912511
USP1 protein, partialHomo sapiens (human)Potency31.622811
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency54.941022
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency20.683122
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency7.040312

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC504.630011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki4.591011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5020.696011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Bile salt export pumpHomo sapiens (human)IC50140.133333
Bile salt export pumpRattus norvegicus (Norway rat)IC50111.600011
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC504.300011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cytochrome P450 1A2Homo sapiens (human)IC500.500011
Cytochrome P450 3A4Homo sapiens (human)IC500.300012
Cytochrome P450 3A5Homo sapiens (human)IC500.300012
Dihydrofolate reductaseHomo sapiens (human)IC500.388011
Dihydroorotate dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)IC5098.872544
Dihydroorotate dehydrogenase Schistosoma mansoniIC5050.000022
Dihydroorotate dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)Ki22.675022
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC501.58222323
Dihydroorotate dehydrogenase (quinone), mitochondrialMus musculus (house mouse)IC500.103045
Dihydroorotate dehydrogenase (quinone), mitochondrialRattus norvegicus (Norway rat)IC500.016067
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)Ki0.920733
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Protein-arginine deiminase type-4Homo sapiens (human)IC502,400.000011
Sodium-dependent dopamine transporter Homo sapiens (human)IC502.884011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.291011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC504.630011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki4.591011
Stromal interaction molecule 1Homo sapiens (human)IC504.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)EC508.906312
matrix metalloproteinase 1, partialHomo sapiens (human)EC505.650011