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GAR transformylase Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
LometrexolIC505.77 [1], 14.0 [2], 220.0 [3], 14000.0 [4]
LometrexolKi6.0 [1], 60.0 [2], 130.0 [3]
PemetrexedIC5030.0 [1], 30000.0 [2]
PemetrexedKi380.0 [1], 1000.0 [2]
N-(4-((3-(2,4-Diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl)amino)benzoyl)glutamic acidIC503000.0 [1]
N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic AcidIC505.6 [1], 6.8 [2], 6800.0 [3]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidIC502.0 [1], 3.5 [2]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidKi68.0 [1]
DdathfIC50220.0 [1]
2-[[4-[(2-Methyl-4-oxo-3H-quinazolin-6-yl)methyl-prop-2-ynylamino]benzoyl]amino]pentanedioic acidIC5017000.0 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acidIC503.46 [1], 630.0 [2]
Dideazaacyclotetrahydrofolic acidIC501600.0 [1]
Dideazaacyclotetrahydrofolic acidKi1700.0 [1]
N-{4-[4-(2-Amino-4-Oxo-1,4-Dihydrothieno[2,3-D]pyrimidin-6-Yl)butyl]benzoyl}-L-Glutamic AcidIC5013.3 [1], 13300.0 [2]
(2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidIC502.4 [1]
(2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidKi13.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acidIC502.6 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acidKi9.1 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl-formylamino]benzoyl]amino]pentanedioic acidIC507600.0 [1], 18000.0 [2]
2-[[4-(3-Amino-1-oxo-2,5,6,6a,7,8,10,10a-octahydropyrimido[4,5-h][2,6]naphthyridin-9-yl)benzoyl]amino]pentanedioic acidIC5020000.0 [1]
2-[[4-[3-(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pteridin-6-yl)propyl]benzoyl]amino]pentanedioic acidIC500.0 [1], 0.01 [2]
(S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acidIC5082.0 [1]
(S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acidKi5500.0 [1]
(S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acidIC50101.0 [1]
(S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acidKi6500.0 [1]
MethotrexateIC5020000.0 [1]
2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-formylamino]benzoyl]amino]pentanedioic acidKi4000.0 [1]
DideazafolateKi2000.0 [1]
2-{4-[(2-Amino-4-hydroxy-pyrido[3,2-d]pyrimidin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acidIC5020000.0 [1]
5,10-Dideazafolic acidIC5016.2 [1]
(2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]amino]pentanedioic acidIC5018.0 [1]
2-[[4-[(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)methyl-methyl-amino]benzoyl]amino]pentanedioic acidIC5030000.0 [1]
(2S)-2-[[4-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]amino]pentanedioic acidIC507.2 [1]
(2S)-2-[[4-[6-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]amino]pentanedioic acidIC508.6 [1]
2-[[4-[(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)methylamino]benzoyl]amino]pentanedioic acidIC5030000.0 [1]
1,5-Dihydroimidazo[4,5-C][1,2,6]thiadiazin-4(3h)-One 2,2-DioxideKi100000.0 [1]
2-[[4-[6-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]amino]-4-(2H-tetrazol-5-yl)butanoic acidKi130.0 [1]
DoptcgaIC502060.0 [1]
DoptzgaIC50140.0 [1]
5-Amino-2-[[4-[(2-amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[2,3-d]pyrimidin-6-yl)methylamino]benzoyl]amino]pentanoic acidIC504800.0 [1]
2-[[4-[Acetyl-[(2-amino-4-oxo-3H-quinazolin-6-yl)methyl]amino]benzoyl]amino]pentanedioic acidKi1300.0 [1]
7-[(2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2,2-dioxo-1H-imidazo[4,5-c][1,2,6]thiadiazin-4-oneKi100000.0 [1]
[(2R,3S,4R,5R)-3,4-Dihydroxy-5-(2,2,4-trioxo-1H-imidazo[4,5-c][1,2,6]thiadiazin-7-yl)oxolan-2-yl]methyl dihydrogen phosphateKi4800.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propoxy]benzoyl]amino]pentanedioic acidIC505300.0 [1]
(2S)-2-[[4-[6-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]amino]pentanedioic acidKi15.0 [1]
(2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]thiophene-2-carbonyl]amino]pentanedioic acidKi35.0 [1]
4-[6-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]-N-(2H-tetrazol-5-ylmethyl)benzamideKi5000.0 [1]
(2S)-2-[[4-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]benzoyl]amino]pentanedioic acidKi38.0 [1]
(2S)-2-[[6-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanylmethyl]-4,5,6,7-tetrahydro-1-benzothiophene-2-carbonyl]amino]pentanedioic acidKi30.0 [1]
(2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-3-ethylthiophene-2-carbonyl]amino]pentanedioic acidKi14.0 [1]
2-[[4-[6-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]amino]acetic acidKi21000.0 [1]
(2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-4-methylthiophene-2-carbonyl]amino]pentanedioic acidKi32.0 [1]
(2S)-2-[[5-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acidKi28.0 [1]
(2S)-2-[[4-[2-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]ethyl]benzoyl]amino]pentanedioic acidKi30000.0 [1]
(2S)-2-[[3-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]benzoyl]amino]pentanedioic acidKi825.0 [1]
(2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-3-methylthiophene-2-carbonyl]amino]pentanedioic acidKi8.5 [1]
(2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methylsulfanylbutyl]benzoyl]amino]pentanedioic acidKi180.0 [1]
(2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methylsulfanylbutyl]benzoyl]amino]pentanedioic acidKi210.0 [1]
(2S)-2-[[4-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acidIC501.79 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-3-carbonyl]amino]pentanedioic acidIC502.03 [1]
(S)-2-(7-(2-Amino-4-Oxo-4,7-Dihydro-3h-Pyrrolo[2,3-D]pyrimidin-6-Yl)heptanamido)pentanedioic AcidIC502.89 [1]
(S)-2-(8-(2-Amino-4-Oxo-4,7-Dihydro-3h-Pyrrolo[2,3-D]pyrimidin-6-Yl)octanamido)pentanedioic AcidIC505.49 [1]
2-[[4-[4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)butylamino]benzoyl]amino]pentanedioic acidIC5018200.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl-methylamino]benzoyl]amino]pentanedioic acidIC504300.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylsulfanyl]benzoyl]amino]pentanedioic acidIC502600.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-fluorobenzoyl]amino]pentanedioic acidIC503500.0 [1]
2-[[2-Chloro-4-[3-(2,4-diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]benzoyl]amino]pentanedioic acidIC506600.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-methylbenzoyl]amino]pentanedioic acidIC506100.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-2-fluorobenzoyl]amino]pentanedioic acidIC503100.0 [1]
2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-methoxybenzoyl]amino]pentanedioic acidIC5018700.0 [1]
(2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acidIC507650.0 [1]
2-[[4-[3-(3-Amino-5-oxo-4H-1,2,4-triazin-6-yl)-2-oxopyrrolidin-1-yl]benzoyl]amino]pentanedioic acidIC50100000.0 [1]
(2S)-2-[[4-[5-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-oxopentan-2-yl]benzoyl]amino]pentanedioic acidKi14.0 [1]
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acidIC5085900.0 [1]
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-methylamino]methyl]benzoyl]amino]pentanedioic acidIC50100000.0 [1]
2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-formylamino]methyl]benzoyl]amino]pentanedioic acidIC50100000.0 [1]
2-[[4-[[(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[2,3-d]pyrimidin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acidIC505300.0 [1]
2-[[4-[[(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[2,3-d]pyrimidin-6-yl)-methylamino]methyl]benzoyl]amino]pentanedioic acidIC5026000.0 [1]
(2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-hydroxybutyl]benzoyl]amino]pentanedioic acidKi1400.0 [1]
(2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-hydroxybutyl]benzoyl]amino]pentanedioic acidKi1100.0 [1]
(2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methoxybutyl]benzoyl]amino]pentanedioic acidKi850.0 [1]
(2S)-2-[[4-[2-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl]-1,3-dithian-2-yl]benzoyl]amino]pentanedioic acidKi1100.0 [1]
(2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methoxybutyl]benzoyl]amino]pentanedioic acidKi1200.0 [1]
10-Trifluoroacetyl-DDACTHFKi30.0 [1]
2-[[4-[3-(4-Amino-6-oxo-1H-pyrimidin-5-yl)propylamino]benzoyl]amino]pentanedioic acidIC5052000.0 [1]
2,6-Diamino-5-[2-(2-nitro-4,5-difluorophenylamino)ethyl]-3,4-dihydropyrimidine-4-oneKi35000.0 [1]
2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-[(4-fluoro-3-nitrophenyl)methyl]amino]benzoyl]amino]pentanedioic acidKi100000.0 [1]
2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-[(3-fluoro-4-nitrophenyl)methyl]amino]benzoyl]amino]pentanedioic acidKi45000.0 [1]
(2S)-2-[[5-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]-4-methylthiophene-2-carbonyl]amino]pentanedioic acidKi15.0 [1]
(2R)-2-[[5-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]-4-methylthiophene-2-carbonyl]amino]pentanedioic acidKi2.0 [1]
2-[[3-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]benzoyl]amino]pentanedioic acidKi3.4 [1]
(2R)-2-[[5-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acidKi3.0 [1]
2-[[4-[2-(2-Amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]benzoyl]amino]pentanedioic acidKi35.0 [1]
(2S)-2-[[5-[2-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]ethyl]thiophene-2-carbonyl]amino]pentanedioic acidKi2000.0 [1]
2-[[4-[2-(2-Amino-4-oxo-3H-pyrido[3,2-d]pyrimidin-6-yl)ethylamino]benzoyl]amino]pentanedioic acidIC5040000.0 [1]
2-[[4-[2-(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[3,2-d]pyrimidin-6-yl)ethylamino]benzoyl]amino]pentanedioic acidIC5020000.0 [1]
2-[[4-[(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[3,2-d]pyrimidin-6-yl)methylamino]benzoyl]amino]pentanedioic acidIC5020000.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acidIC5012.0 [1]
(2S)-2-[[4-[(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)methyl]benzoyl]amino]pentanedioic acidIC501000.0 [1]
2-{4-[3-(2-Amino-4-oxo-3,4-dihydro-pteridin-6-yl)-propyl]-benzoylamino}-pentanedioic acidIC5025000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ GAR transformylase Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/gar-transformylase-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ GAR transformylase Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gar-transformylase-inhibitors-ic50-ki.
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