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Found 2783 Enz. Inhib. hit(s) with Target = 'Bifunctional dihydrofolate reductase-thymidylate synthase'
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50016325(2-{4-[(2,4-Diamino-pyrido[2,3-d]pyrimidin-6-ylmeth...)
Affinity DataIC50:  0.00210nMAssay Description:Inhibition against Toxoplasma gondii Dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM50035483(5-Chloro-N*6*-(2,5-dimethoxy-benzyl)-quinazoline-2...)
Affinity DataIC50:  0.390nMAssay Description:Inhibition of Plasmodium falciparum DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18229(5-[3-({2,4-diamino-5-methylpyrido[2,3-d]pyrimidin-...)
Affinity DataIC50:  0.460nMAssay Description:Dihydrofolate reductase was assayed with no inhibitor and with a series of concentrations of inhibitors to allow for a range of inhibition from 10 to...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
Mahidol University

LigandPNGBDBM18793(6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]...)
Affinity DataKi:  0.0110nM ΔG°:  -62.5kJ/mole IC50:  0.570nMpH: 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))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM18793(6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]...)
Affinity DataIC50:  0.570nMAssay Description:Inhibition of Plasmodium falciparum DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.580nMAssay Description:Inhibition of Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.580nMAssay Description:Inhibition of Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM50531784(Fanotaprim | TRC-2533 | TRC-2533-NX | US11530198, ...)
Affinity DataIC50:  0.708nMAssay Description:TBDMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50049611(6-[(Methyl-phenyl-amino)-methyl]-pyrido[3,2-d]pyri...)
Affinity DataIC50:  0.840nMAssay Description:Inhibition of Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.850nMAssay Description:Concentration inhibiting T. gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.850nMAssay Description:Inhibition of dihydrofolate reductase (DHFR) from Toxoplasma gondii(tg)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.850nMAssay Description:Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondiiMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.850nMAssay Description:Inhibitory concentration against Dihydrofolate reductase from Toxoplasma gondii (tg)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50029766(2,4-DIAMINO-5-METHYL-6-[(3,4,5-TRIMETHOXY-N-METHYL...)
Affinity DataIC50:  0.850nMAssay Description:Inhibitory concentration against Toxoplasma gondii Dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50067865(CHEMBL337603 | N*6*-(3,4-Dimethoxy-phenyl)-N*6*-me...)
Affinity DataIC50:  0.880nMAssay Description:Inhibitory activity against dihydrofolate reductase (DHFR) from Toxoplasma gondiiMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM66082((2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methy...)
Affinity DataIC50:  0.891nMAssay Description:TBDMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM585342(5-(4-(3-(2-ethylpyrimidin-5- yl)phenyl)piperidin-1...)
Affinity DataIC50:  0.891nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma cruzi)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM66082((2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methy...)
Affinity DataIC50:  1.10nMAssay Description:TBDMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25826(5-[(3R)-3-(3-methoxy-5-phenylphenyl)but-1-yn-1-yl]...)
Affinity DataIC50:  1.10nMpH: 7.0 T: 2°CAssay Description:Enzyme activity assays were performed by monitoring the change in UV absorbance at 340 nm. Enzyme assays were performed at least four times. IC50 val...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25826(5-[(3R)-3-(3-methoxy-5-phenylphenyl)but-1-yn-1-yl]...)
Affinity DataIC50:  1.10nMAssay Description:Compounds were evaluated in spectrophotometric enzyme assays using ChDHFR-TS and hDHFR. Inhibition constants (IC50) were measured (see Table 4). The ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM585318(5-(4-(3-(tetrahydro-2H-pyran-4- yl)phenyl)piperazi...)
Affinity DataIC50:  1.10nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM66082((2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methy...)
Affinity DataIC50:  1.29nMAssay Description:TBDMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18268(5-methyl-6-{[(3,4,5-trimethoxyphenyl)amino]methyl}...)
Affinity DataIC50:  1.35nMAssay Description:TBDMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18268(5-methyl-6-{[(3,4,5-trimethoxyphenyl)amino]methyl}...)
Affinity DataIC50:  1.40nMAssay 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
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18050(2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)a...)
Affinity DataIC50:  1.40nMAssay Description:Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii was evaluated using 90 microM dihydrofolic acid as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18497(6-methyl-5-[(3R)-3-(3,4,5-trimethoxyphenyl)but-1-y...)
Affinity DataIC50:  1.40nMpH: 7.0 T: 2°CAssay Description:Enzyme activity assays were performed by monitoring the rate of enzyme-dependent NADPH consumption at an absorbance of 340 nm over a period of severa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM18792(1-(4-chlorophenyl)-6,6-dimethyl-1,6-dihydro-1,3,5-...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of Plasmodium falciparum DHFRMore data for this Ligand-Target Pair
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50531784(Fanotaprim | TRC-2533 | TRC-2533-NX | US11530198, ...)
Affinity DataIC50:  1.60nMAssay 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(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25818(5-[3-(3-methoxy-5-phenylphenyl)but-1-yn-1-yl]-6-me...)
Affinity DataIC50:  1.80nMAssay Description:Compounds were evaluated in spectrophotometric enzyme assays using ChDHFR-TS and hDHFR. Inhibition constants (IC50) were measured (see Table 4). The ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25818(5-[3-(3-methoxy-5-phenylphenyl)but-1-yn-1-yl]-6-me...)
Affinity DataIC50:  1.80nMpH: 7.0 T: 2°CAssay Description:Enzyme activity assays were performed by monitoring the change in UV absorbance at 340 nm. Enzyme assays were performed at least four times. IC50 val...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50059944(4-{[4-(2,4-Diamino-6-ethyl-pyrimidin-5-yl)-2-nitro...)
Affinity DataIC50:  1.80nMAssay Description:Inhibitory activity against Dihydrofolate reductase from Toxoplasma gondii was evaluated using 90 microM dihydrofolic acid as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18225(2,4-diamino-5-deazapteridine, 4 | 4-[3-({2,4-diami...)
Affinity DataIC50:  1.90nMAssay Description:Dihydrofolate reductase was assayed with no inhibitor and with a series of concentrations of inhibitors to allow for a range of inhibition from 10 to...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM50531779(CHEMBL4553229 | US11530198, Example 4)
Affinity DataIC50:  1.91nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18227(2,4-diamino-5-deazapteridine, 6 | 6-[3-({2,4-diami...)
Affinity DataIC50:  2nMAssay Description:Dihydrofolate reductase was assayed with no inhibitor and with a series of concentrations of inhibitors to allow for a range of inhibition from 10 to...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM50531785(CHEMBL4543226 | US11530198, Example 69)
Affinity DataIC50:  2nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM585298(5-(4-([1,1'-biphenyl]-3-yl)-3- methylpiperazin-1- ...)
Affinity DataIC50:  2nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM50531784(Fanotaprim | TRC-2533 | TRC-2533-NX | US11530198, ...)
Affinity DataIC50:  2.09nMAssay Description:TBDMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25820(5-{3-[3-(2,6-dimethylphenyl)-5-methoxyphenyl]but-1...)
Affinity DataIC50:  2.10nMpH: 7.0 T: 2°CAssay Description:Enzyme activity assays were performed by monitoring the change in UV absorbance at 340 nm. Enzyme assays were performed at least four times. IC50 val...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM31777(thieno[2,3-d]pyrimidine deriv., 2)
Affinity DataIC50:  2.10nMAssay Description:DHFRs were assayed spectrophotometrically in the reaction buffer solution containing dihydrofolate. The reaction was initiated with an amount of enzy...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25819(5-{3-[3-methoxy-5-(2-methylphenyl)phenyl]but-1-yn-...)
Affinity DataIC50:  2.10nMpH: 7.0 T: 2°CAssay Description:Enzyme activity assays were performed by monitoring the change in UV absorbance at 340 nm. Enzyme assays were performed at least four times. IC50 val...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25820(5-{3-[3-(2,6-dimethylphenyl)-5-methoxyphenyl]but-1...)
Affinity DataIC50:  2.10nMAssay Description:Compounds were evaluated in spectrophotometric enzyme assays using ChDHFR-TS and hDHFR. Inhibition constants (IC50) were measured (see Table 4). The ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Cryptosporidium hominis)
University Of Connecticut At Storrs

LigandPNGBDBM25819(5-{3-[3-methoxy-5-(2-methylphenyl)phenyl]but-1-yn-...)
Affinity DataIC50:  2.10nMAssay Description:Compounds were evaluated in spectrophotometric enzyme assays using ChDHFR-TS and hDHFR. Inhibition constants (IC50) were measured (see Table 4). The ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50067861(CHEMBL140940 | N*6*-Methyl-N*6*-phenyl-pyrido[3,2-...)
Affinity DataIC50:  2.20nMAssay Description:Inhibitory activity against dihydrofolate reductase (DHFR) from Toxoplasma gondiiMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Leishmania major)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM66082((2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methy...)
Affinity DataIC50:  2.29nMAssay Description:TBDMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Plasmodium falciparum (isolate K1 / Thailand))
East China University Of Science And Technology

Curated by ChEMBL
LigandPNGBDBM18793(6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]...)
Affinity DataKi:  0.0200nM ΔG°:  -61.1kJ/mole IC50:  2.30nMpH: 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(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18228(4-[2-({2,4-diamino-5-methylpyrido[2,3-d]pyrimidin-...)
Affinity DataIC50:  2.30nMAssay Description:Dihydrofolate reductase was assayed with no inhibitor and with a series of concentrations of inhibitors to allow for a range of inhibition from 10 to...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18226(2,4-diamino-5-deazapteridine, 5 | 5-[3-({2,4-diami...)
Affinity DataIC50:  2.30nMAssay Description:Dihydrofolate reductase was assayed with no inhibitor and with a series of concentrations of inhibitors to allow for a range of inhibition from 10 to...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM50531797(CHEMBL4550110 | US11530198, Example 86)
Affinity DataIC50:  2.51nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Trypanosoma brucei brucei)
Vyera Pharmaceuticals

US Patent
LigandPNGBDBM585326(5-(4-(3-(2-chloropyrimidin-5- yl)phenyl)piperazin-...)
Affinity DataIC50:  2.51nMAssay Description:TBDMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBifunctional dihydrofolate reductase-thymidylate synthase(Toxoplasma gondii)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50034942(6-{[Ethyl-(3,4,5-trimethoxy-phenyl)-amino]-methyl}...)
Affinity DataIC50:  2.70nMAssay Description:Inhibition of Toxoplasma gondii dihydrofolate reductaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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