Page last updated: 2024-08-05 15:31:24

antifolate

An antimetabolite that impairs the action of folic acids

ChEBI ID: 73913

Members (2)

MemberDefinitionClass
cycloguanilA triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.cycloguanil
o 129A member of the class of pteridines that is pteridine in which the hydrogens at positions 2 and 4 are replaced by amino groups, whilst those at positions 6 and 7 are replaced by isopropyl groups.2,4-diamino-6,7-diisopropylpteridine

Research

Studies (245)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199045 (18.37)18.7374
1990's81 (33.06)18.2507
2000's74 (30.20)29.6817
2010's40 (16.33)24.3611
2020's5 (2.04)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials16 (6.13%)5.53%
Reviews4 (1.53%)6.00%
Case Studies3 (1.15%)4.05%
Observational0 (0.00%)0.25%
Other238 (91.19%)84.16%

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K1IC5024.973366
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K1Ki0.43621719
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC505.800011
Dihydrofolate reductaseEscherichia coli K-12IC5020.910011
Dihydrofolate reductasePneumocystis cariniiIC500.450011
Dihydrofolate reductaseRattus norvegicus (Norway rat)IC500.110011
Dihydrofolate reductaseEscherichia coli K-12Ki1.020011
Dihydrofolate reductaseGallus gallus (chicken)Ki0.112211
Dihydrofolate reductaseHomo sapiens (human)Ki14.488533
Dihydrofolate reductaseLacticaseibacillus caseiKi17.378011
Dihydrofolate reductasePneumocystis cariniiKi36.377633
Pteridine reductase 1Leishmania majorKi0.240011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Dihydrofolate reductaseEscherichia coli K-12Kd11.770011
Trace amine-associated receptor 5Mus musculus (house mouse)EC5010.000011