Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)glutamic acid | 16fold selectivity for Leishmania major enzyme over human enzyme | Leishmania major | |
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)leucine | 84fold selectivity for Leishmania major enzyme over human enzyme | Leishmania major | |
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)phenylalanine | 87fold selectivity for Leishmania major enzyme over human enzyme | Leishmania major | |
(2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)tryptophan | 10fold selectivity for Leishmania major enzyme over human enzyme | Leishmania major | |
additional information | development of antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motifs | Leishmania major | |
trimethoprim | - |
Leishmania major |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Leishmania major | P07382 | bifunctional dihydrofolate reductase-thymidylate synthase, cf. EC 2.1.1.45 | - |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0001 | - |
pH 7, temperature not specified in the publication | Leishmania major | (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)glutamic acid | |
0.00013 | - |
pH 7, temperature not specified in the publication | Leishmania major | (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)leucine | |
0.00014 | - |
pH 7, temperature not specified in the publication | Leishmania major | (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)phenylalanine | |
0.00018 | - |
pH 7, temperature not specified in the publication | Leishmania major | (2-(4-((2,4-diaminopyrimidine-5-yl)methyl)-2,6-dimethoxyphenoxy)-2-oxoethyl)tryptophan | |
0.02 | - |
pH 7, temperature not specified in the publication | Leishmania major | trimethoprim |