EC Number   |
IC50 Value |
IC50 Value Maximum |
Inhibitor |
Reference |
|---|
    6.3.2.17 | -999 |
- |
2-[[[(4S)-4-carboxy-4-[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)amino]butyl](hydroxy)phosphoryl]methyl]pentanedioic acid |
45 nM for species of low mobility, 3.5 nm for species of high mobility |
701922 |
| 6.3.2.17 | -999 |
- |
2-[[[(4S)-4-[(4-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl)amino]-4-carboxybutyl](hydroxy)phosphoryl]methyl]pentanedioic acid |
51 nM for species of low mobility, 1.7 nM for species of high mobility |
701922 |
| 6.3.2.17 | -999 |
- |
2-[[[(4S)-4-[(4-[[(2-amino-4-oxo-3,4-dihydropteridin-6-yl)methyl]amino]benzoyl)amino]-4-carboxybutyl](hydroxy)phosphoryl]methyl]pentanedioic acid |
65 nM for species of low mobility, 6.5 nM for species of high mobility |
701922 |
| 6.3.2.17 | -999 |
- |
N-(4-[[(2-amino-4-oxo-3,4-dihydropteridin-6-yl)methyl]amino]benzoyl)-L-gamma-glutamyl-5-[(2,4-dicarboxybutyl)(hydroxy)phosphoryl]-L-norvaline |
576 nM for species of low mobility, 98 nM for species of high mobility |
701922 |
| 6.3.2.17 | 0.000001 |
- |
methotrexate-Glu |
IC50 of 0.0000014 mM in the wild type cell line, IC50 of 0.000001 mM to 0.00095 mM in the antifolates-resistant sublines |
651536 |
| 6.3.2.17 | 0.0000012 |
- |
(S)-2(5-(((1,2-dihydro-3-methyl-1-oxobenzo-(f)quinazolin-9-yl)methyl)-1-oxo-2-isoindolinyl))-glutaric acid |
IC50 of 0.0000009 mM in the wild type cell line, IC50 of 0.0000012 mM to 0.000539 mM in the antifolates-resistant sublines |
651536 |
| 6.3.2.17 | 0.000006 |
- |
Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl-L-ornithine |
IC50 of 0.000001 mM in the wild type cell line, IC50 of 0.000006 mM to 0.0017 mM in the antifolates-resistant sublines |
651536 |
| 6.3.2.17 | 0.000008 |
- |
(2S)-2-(o-fluoro-p-(N-(2,7-dimethyl-4-oxo-3,4-dihydroquinazolin-6-yl)methyl)-N-(prop-2-ynyl-amino)benzamido)-4-(tetrazol-5-yl)butyric acid |
IC50 of 0.0000153 mM in the wild type cell line, IC50 of 0.000008 mM to 0.0016 mM in the antifolates-resistant sublines |
651536 |
| 6.3.2.17 | 0.000008 |
- |
methotrexate-phosphinate |
competitive inhibition, IC50 of 0.000008 mM, at fixed substrate and recombinant enzyme concentrations. The most potent FPGS inhibitor based on methotrexate heterocycle. CCRF-CEM R2 subline does not respond to inhibition by this compound at 0.001 mM |
649799 |
| 6.3.2.17 | 0.0000095 |
- |
methotrexate |
wild type enzyme from cytosol |
672921 |
