Found 49 Enz. Inhib. hit(s) with Target = 'Bifunctional dihydrofolate reductase-thymidylate synthase' and Ligand = 'BDBM18512' TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 0.190nMAssay Description:Thermodynamic dissociation constant of compound for mutant T46S E. coli dihydrofolate reductaseMore data for this Ligand-Target Pair
3D Structure (crystal)TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 0.190nMAssay Description:Inhibitor constant of compound for plasmodium falciparum dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Mahidol University
Mahidol University
Affinity DataKi: 0.200nM ΔG°: -55.4kJ/mole IC50: 80nMpH: 7.0 T: 2°CAssay Description:The concentration of inhibitor that inhibited 50% of the parasite growth (IC50) was determined from the sigmoidal curve obtained by plotting the perc...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium vivax (malaria parasite P. vivax))
National Center For Genetic Engineering and Biotechnology At Thailand
National Center For Genetic Engineering and Biotechnology At Thailand
Affinity DataKi: 0.210nM ΔG°: -55.2kJ/mole IC50: 180nMpH: 7.0 T: 2°CAssay Description:Nineteen Pyr analogs were studied for their inhibition activity against cells expressing either WT or SP21 mutant PvDHFR-TS. The assays were conducte...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 0.600nMAssay Description:Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 0.600nMAssay Description:Inhibition of the wild-type dihydrofolate reductase (DHFR)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Mahidol University
Mahidol University
Affinity DataKi: 0.850nMAssay Description:Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3) by M...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 0.870nMAssay Description:Inhibition constant against Plasmodium falciparum dihydrofolate reductaseChecked by AuthorMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 1.40nMAssay Description:Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single S108T mutationMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 1.5nMAssay Description:Binding affinity was evaluated as inhibition of recombinant wild type (WT) Plasmodium falciparum DHFR-TS.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 1.5nMAssay Description:Inhibition constant against wild-type PfDHFR (Plasmodium falciparum dihydrofolate reductase)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 3.60nMAssay Description:Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with double (A16V + S108T) mutationsMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 6nMAssay Description:Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with single A16V mutationMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 9.80nM ΔG°: -45.7kJ/mole IC50: 3.09E+4nMpH: 7.0 T: 2°CAssay Description:The concentration of inhibitor that inhibited 50% of the parasite growth (IC50) was determined from the sigmoidal curve obtained by plotting the perc...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 28.6nMAssay Description:Inhibition of the S108N mutant of dihydrofolate reductase (DHFR)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 53.9nMAssay Description:Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 67.1nMAssay Description:Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparumMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 72nMAssay Description:Binding affinity was evaluated as inhibition of mutant (C59R + S108N) Plasmodium falciparum DHFR-TS.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 112nMAssay Description:Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparumMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 380nMAssay Description:Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with triple (C59R + S108N + I164L) mutationsMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 385nMAssay Description:Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparumMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataKi: 860nMAssay Description:Inhibition constant against PfDHFR (Plasmodium falciparum dihydrofolate reductase) with quadruple (N51I + C59R + S108N + I164L) mutationsMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 26nMAssay Description:Inhibition of Plasmodium falciparum DHFR using DHF as substrate preincubated for 15 mins followed DHF addition measured after 15 mins by spectrophoto...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 58nMAssay Description:Inhibition of Plasmodium falciparum DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 80nMAssay Description:Inhibition of Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 80nMAssay Description:Inhibition of Plasmodium falciparum DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 80nMAssay Description:In vitro anti-plasmodial activity against Plasmodium falciparum with wild type dihydrofolate reductase (TM4/8.2).More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 139nMAssay Description:Inhibition of Toxoplasma gondii DHFR-TS expressed in Escherichia coli BL21 competent cells using DHF as substrate preincubated for 15 mins followed b...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 200nMAssay Description:Inhibition of Toxoplasma gondii DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 230nMAssay Description:Inhibition of Toxoplasma gondii TS-DHFR expressed in Escherichia coli BL21 preincubated for 15 mins followed by addition of DHF as substrate and NADP...More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibition of Dihydrofolate reductase of Toxoplasma gondiiMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibitory activity against Toxoplasma gondii Dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibition of T. gondii Dihydrofolate ReductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibitory activity against Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Compound was tested for inhibition activity against toxoplasma gondii (T. gondii) Dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibitory activity against dihydrofolate reductase DHFR in Toxoplasma gondii.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:Inhibitory concentration against Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Duquesne University
Curated by ChEMBL
Duquesne University
Curated by ChEMBL
Affinity DataIC50: 390nMAssay Description:The ability of the compound to inhibit T. gondii Dihydrofolate reductase was testedMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals
US Patent
Vyera Pharmaceuticals
US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma cruzi)
Vyera Pharmaceuticals
US Patent
Vyera Pharmaceuticals
US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Mahidol University
Mahidol University
Affinity DataIC50: 2.48E+3nMAssay Description:Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Leishmania major)
Vyera Pharmaceuticals
US Patent
Vyera Pharmaceuticals
US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 3.09E+4nMAssay Description:Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with mutant enzyme C59R+S108N- pfDihydrofolate reductase (K1CB1)More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 4.17E+4nMAssay Description:In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N+I164L (Csl-2) dihydrofolate reductase.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: 7.35E+4nMAssay Description:In vitro anti-plasmodial activity against Plasmodium falciparum with mutant N51I+C59R+S108N (W2) dihydrofolate reductase.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Pennsylvania State University
Curated by ChEMBL
Pennsylvania State University
Curated by ChEMBL
Affinity DataIC50: >1.00E+5nMAssay Description:In vitro anti-plasmodial activity against Plasmodium falciparum with mutant CN51I+C59R+S108N+I164L (V1/S) dihydrofolate reductase.More data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
Dartmouth College
Curated by ChEMBL
Dartmouth College
Curated by ChEMBL
Affinity DataIC50: >1.00E+6nMAssay Description:Inhibition of Cryptosporidium hominis DHFRMore data for this Ligand-Target Pair
