Roles > EC 2.1.1.45 (thymidylate synthase) inhibitor
Page last updated: 2024-08-05 15:29:10

EC 2.1.1.45 (thymidylate synthase) inhibitor

An EC 2.1.1.* (methyltransferases) inhibitor that interferes with the action of thymidylate synthase (EC 2.1.1.45).

ChEBI ID: 63720

Members (2)

MemberDefinitionClass
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
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

Research

Studies (3,122)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990221 (7.08)18.7374
1990's128 (4.10)18.2507
2000's578 (18.51)29.6817
2010's1,596 (51.12)24.3611
2020's599 (19.19)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials778 (24.20%)5.53%
Reviews445 (13.84%)6.00%
Case Studies352 (10.95%)4.05%
Observational42 (1.31%)0.25%
Other1,598 (49.70%)84.16%

Protein Targets (62)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
67.9K proteinVaccinia virusPotency0.696222
ATAD5 protein, partialHomo sapiens (human)Potency2.909311
Cellular tumor antigen p53Homo sapiens (human)Potency4.071222
chromobox protein homolog 1Homo sapiens (human)Potency79.432811
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.432811
estrogen nuclear receptor alphaHomo sapiens (human)Potency12.439033
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency13.333211
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.959133
EWS/FLI fusion proteinHomo sapiens (human)Potency0.390344
farnesoid X nuclear receptorHomo sapiens (human)Potency0.105911
Fumarate hydrataseHomo sapiens (human)Potency11.220211
gemininHomo sapiens (human)Potency1.636011
GLI family zinc finger 3Homo sapiens (human)Potency15.846511
glp-1 receptor, partialHomo sapiens (human)Potency2.238711
heat shock protein beta-1Homo sapiens (human)Potency33.488911
Histone H2A.xCricetulus griseus (Chinese hamster)Potency0.325722
IDH1Homo sapiens (human)Potency1.835611
lamin isoform A-delta10Homo sapiens (human)Potency1.995311
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency16.895622
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency10.322511
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency6.682422
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.867622
polyproteinZika virusPotency11.220211
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency11.220211
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency4.480322
survival motor neuron protein isoform dHomo sapiens (human)Potency12.589311
TDP1 proteinHomo sapiens (human)Potency0.199124
thioredoxin reductaseRattus norvegicus (Norway rat)Potency100.000011
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency8.767622
tyrosine-protein kinase YesHomo sapiens (human)Potency38.708811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bifunctional dihydrofolate reductase-thymidylate synthaseToxoplasma gondiiIC502.47801515
Bifunctional purine biosynthesis protein ATICHomo sapiens (human)IC500.070011
Bifunctional purine biosynthesis protein ATICHomo sapiens (human)Ki200.000011
Bile salt export pumpHomo sapiens (human)IC501,000.000011
Chain A, Thymidylate SynthaseEscherichia coliKi0.109012
Chain A, Thymidylate SynthaseHomo sapiens (human)Ki0.109011
Dihydrofolate reductaseEscherichia coli K-12IC50383.52501212
Dihydrofolate reductaseHomo sapiens (human)IC507.67621717
Dihydrofolate reductaseLacticaseibacillus caseiIC50173.075044
Dihydrofolate reductasePneumocystis cariniiIC50230.000011
Dihydrofolate reductaseHomo sapiens (human)Ki0.007133
Dihydrofolate reductaseMus musculus (house mouse)Ki0.560011
exodeoxyribonuclease V subunit RecBEscherichia coli str. K-12 substr. MG1655IC5092.268522
exodeoxyribonuclease V subunit RecCEscherichia coli str. K-12 substr. MG1655IC5092.268522
exodeoxyribonuclease V subunit RecDEscherichia coli str. K-12 substr. MG1655IC5092.268522
Folate receptor alphaHomo sapiens (human)IC500.241766
Folate receptor betaHomo sapiens (human)IC500.258566
Proton-coupled folate transporterHomo sapiens (human)IC500.022955
Proton-coupled folate transporterHomo sapiens (human)Ki0.677677
Reduced folate transporterHomo sapiens (human)IC500.092855
Serine hydroxymethyltransferase, cytosolicHomo sapiens (human)Ki79.233333
Thymidine kinase Macacine alphaherpesvirus 1IC502.000011
Thymidylate kinaseMycobacterium tuberculosis H37RvKi97.000011
Thymidylate synthaseHomo sapiens (human)IC5015.81182222
Thymidylate synthaseLacticaseibacillus caseiIC5029.000044
Thymidylate synthaseHomo sapiens (human)Ki0.114233
Thymidylate synthaseLacticaseibacillus caseiKi0.550011
Thymidylate synthaseMus musculus (house mouse)Ki0.340011
Thymidylate synthase Escherichia coliIC50122.23851313
Thymidylate synthase Escherichia coli LF82IC5076.000011
Thymidylate synthase Rattus norvegicus (Norway rat)IC5020.000011
Trifunctional purine biosynthetic protein adenosine-3Homo sapiens (human)IC505.028566
Trifunctional purine biosynthetic protein adenosine-3Mus musculus (house mouse)IC5020.000033
Trifunctional purine biosynthetic protein adenosine-3Homo sapiens (human)Ki0.611244

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Serine hydroxymethyltransferase, cytosolicHomo sapiens (human)Kd16.900011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
LMP1 [Human herpesvirus 4]human gammaherpesvirus 4 (Epstein-Barr virus)AC501.318022
Proton-coupled folate transporterHomo sapiens (human)K0.157022
Thymidine phosphorylaseHomo sapiens (human)Km798.000011
Thymidylate synthaseMus musculus (house mouse)ID500.035011