| Lometrexol | IC50 | 5.77 [1], 14.0 [2], 220.0 [3], 14000.0 [4] |
| Lometrexol | Ki | 6.0 [1], 60.0 [2], 130.0 [3] |
| Pemetrexed | IC50 | 30.0 [1], 30000.0 [2] |
| Pemetrexed | Ki | 380.0 [1], 1000.0 [2] |
| N-(4-((3-(2,4-Diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl)amino)benzoyl)glutamic acid | IC50 | 3000.0 [1] |
| N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic Acid | IC50 | 5.6 [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 acid | IC50 | 2.0 [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 acid | Ki | 68.0 [1] |
| Ddathf | IC50 | 220.0 [1] |
| 2-[[4-[(2-Methyl-4-oxo-3H-quinazolin-6-yl)methyl-prop-2-ynylamino]benzoyl]amino]pentanedioic acid | IC50 | 17000.0 [1] |
| (2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 3.46 [1], 630.0 [2] |
| Dideazaacyclotetrahydrofolic acid | IC50 | 1600.0 [1] |
| Dideazaacyclotetrahydrofolic acid | Ki | 1700.0 [1] |
| N-{4-[4-(2-Amino-4-Oxo-1,4-Dihydrothieno[2,3-D]pyrimidin-6-Yl)butyl]benzoyl}-L-Glutamic Acid | IC50 | 13.3 [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 acid | IC50 | 2.4 [1] |
| (2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid | Ki | 13.0 [1] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acid | IC50 | 2.6 [1] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acid | Ki | 9.1 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl-formylamino]benzoyl]amino]pentanedioic acid | IC50 | 7600.0 [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 acid | IC50 | 20000.0 [1] |
| 2-[[4-[3-(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pteridin-6-yl)propyl]benzoyl]amino]pentanedioic acid | IC50 | 0.0 [1], 0.01 [2] |
| (S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acid | IC50 | 82.0 [1] |
| (S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acid | Ki | 5500.0 [1] |
| (S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acid | IC50 | 101.0 [1] |
| (S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acid | Ki | 6500.0 [1] |
| Methotrexate | IC50 | 20000.0 [1] |
| 2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-formylamino]benzoyl]amino]pentanedioic acid | Ki | 4000.0 [1] |
| Dideazafolate | Ki | 2000.0 [1] |
| 2-{4-[(2-Amino-4-hydroxy-pyrido[3,2-d]pyrimidin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acid | IC50 | 20000.0 [1] |
| 5,10-Dideazafolic acid | IC50 | 16.2 [1] |
| (2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]amino]pentanedioic acid | IC50 | 18.0 [1] |
| 2-[[4-[(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)methyl-methyl-amino]benzoyl]amino]pentanedioic acid | IC50 | 30000.0 [1] |
| (2S)-2-[[4-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]amino]pentanedioic acid | IC50 | 7.2 [1] |
| (2S)-2-[[4-[6-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]amino]pentanedioic acid | IC50 | 8.6 [1] |
| 2-[[4-[(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)methylamino]benzoyl]amino]pentanedioic acid | IC50 | 30000.0 [1] |
| 1,5-Dihydroimidazo[4,5-C][1,2,6]thiadiazin-4(3h)-One 2,2-Dioxide | Ki | 100000.0 [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 acid | Ki | 130.0 [1] |
| Doptcga | IC50 | 2060.0 [1] |
| Doptzga | IC50 | 140.0 [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 acid | IC50 | 4800.0 [1] |
| 2-[[4-[Acetyl-[(2-amino-4-oxo-3H-quinazolin-6-yl)methyl]amino]benzoyl]amino]pentanedioic acid | Ki | 1300.0 [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-one | Ki | 100000.0 [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 phosphate | Ki | 4800.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propoxy]benzoyl]amino]pentanedioic acid | IC50 | 5300.0 [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 acid | Ki | 15.0 [1] |
| (2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]thiophene-2-carbonyl]amino]pentanedioic acid | Ki | 35.0 [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)benzamide | Ki | 5000.0 [1] |
| (2S)-2-[[4-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]benzoyl]amino]pentanedioic acid | Ki | 38.0 [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 acid | Ki | 30.0 [1] |
| (2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-3-ethylthiophene-2-carbonyl]amino]pentanedioic acid | Ki | 14.0 [1] |
| 2-[[4-[6-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]amino]acetic acid | Ki | 21000.0 [1] |
| (2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-4-methylthiophene-2-carbonyl]amino]pentanedioic acid | Ki | 32.0 [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 acid | Ki | 28.0 [1] |
| (2S)-2-[[4-[2-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]ethyl]benzoyl]amino]pentanedioic acid | Ki | 30000.0 [1] |
| (2S)-2-[[3-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]benzoyl]amino]pentanedioic acid | Ki | 825.0 [1] |
| (2S)-2-[[5-[3-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]propyl]-3-methylthiophene-2-carbonyl]amino]pentanedioic acid | Ki | 8.5 [1] |
| (2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methylsulfanylbutyl]benzoyl]amino]pentanedioic acid | Ki | 180.0 [1] |
| (2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methylsulfanylbutyl]benzoyl]amino]pentanedioic acid | Ki | 210.0 [1] |
| (2S)-2-[[4-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 1.79 [1] |
| (2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-3-carbonyl]amino]pentanedioic acid | IC50 | 2.03 [1] |
| (S)-2-(7-(2-Amino-4-Oxo-4,7-Dihydro-3h-Pyrrolo[2,3-D]pyrimidin-6-Yl)heptanamido)pentanedioic Acid | IC50 | 2.89 [1] |
| (S)-2-(8-(2-Amino-4-Oxo-4,7-Dihydro-3h-Pyrrolo[2,3-D]pyrimidin-6-Yl)octanamido)pentanedioic Acid | IC50 | 5.49 [1] |
| 2-[[4-[4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)butylamino]benzoyl]amino]pentanedioic acid | IC50 | 18200.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl-methylamino]benzoyl]amino]pentanedioic acid | IC50 | 4300.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylsulfanyl]benzoyl]amino]pentanedioic acid | IC50 | 2600.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-fluorobenzoyl]amino]pentanedioic acid | IC50 | 3500.0 [1] |
| 2-[[2-Chloro-4-[3-(2,4-diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]benzoyl]amino]pentanedioic acid | IC50 | 6600.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-methylbenzoyl]amino]pentanedioic acid | IC50 | 6100.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-2-fluorobenzoyl]amino]pentanedioic acid | IC50 | 3100.0 [1] |
| 2-[[4-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propylamino]-3-methoxybenzoyl]amino]pentanedioic acid | IC50 | 18700.0 [1] |
| (2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 7650.0 [1] |
| 2-[[4-[3-(3-Amino-5-oxo-4H-1,2,4-triazin-6-yl)-2-oxopyrrolidin-1-yl]benzoyl]amino]pentanedioic acid | IC50 | 100000.0 [1] |
| (2S)-2-[[4-[5-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-oxopentan-2-yl]benzoyl]amino]pentanedioic acid | Ki | 14.0 [1] |
| 2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acid | IC50 | 85900.0 [1] |
| 2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-methylamino]methyl]benzoyl]amino]pentanedioic acid | IC50 | 100000.0 [1] |
| 2-[[4-[[(2-Amino-4-oxo-3H-pyrido[2,3-d]pyrimidin-6-yl)-formylamino]methyl]benzoyl]amino]pentanedioic acid | IC50 | 100000.0 [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 acid | IC50 | 5300.0 [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 acid | IC50 | 26000.0 [1] |
| (2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-hydroxybutyl]benzoyl]amino]pentanedioic acid | Ki | 1400.0 [1] |
| (2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-hydroxybutyl]benzoyl]amino]pentanedioic acid | Ki | 1100.0 [1] |
| (2S)-2-[[4-[(1R)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methoxybutyl]benzoyl]amino]pentanedioic acid | Ki | 850.0 [1] |
| (2S)-2-[[4-[2-[3-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)propyl]-1,3-dithian-2-yl]benzoyl]amino]pentanedioic acid | Ki | 1100.0 [1] |
| (2S)-2-[[4-[(1S)-4-(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)-1-methoxybutyl]benzoyl]amino]pentanedioic acid | Ki | 1200.0 [1] |
| 10-Trifluoroacetyl-DDACTHF | Ki | 30.0 [1] |
| 2-[[4-[3-(4-Amino-6-oxo-1H-pyrimidin-5-yl)propylamino]benzoyl]amino]pentanedioic acid | IC50 | 52000.0 [1] |
| 2,6-Diamino-5-[2-(2-nitro-4,5-difluorophenylamino)ethyl]-3,4-dihydropyrimidine-4-one | Ki | 35000.0 [1] |
| 2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-[(4-fluoro-3-nitrophenyl)methyl]amino]benzoyl]amino]pentanedioic acid | Ki | 100000.0 [1] |
| 2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methyl-[(3-fluoro-4-nitrophenyl)methyl]amino]benzoyl]amino]pentanedioic acid | Ki | 45000.0 [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 acid | Ki | 15.0 [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 acid | Ki | 2.0 [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 acid | Ki | 3.4 [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 acid | Ki | 3.0 [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 acid | Ki | 35.0 [1] |
| (2S)-2-[[5-[2-[(2,4-Diamino-6-oxo-1H-pyrimidin-5-yl)sulfanyl]ethyl]thiophene-2-carbonyl]amino]pentanedioic acid | Ki | 2000.0 [1] |
| 2-[[4-[2-(2-Amino-4-oxo-3H-pyrido[3,2-d]pyrimidin-6-yl)ethylamino]benzoyl]amino]pentanedioic acid | IC50 | 40000.0 [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 acid | IC50 | 20000.0 [1] |
| 2-[[4-[(2-Amino-4-oxo-5,6,7,8-tetrahydro-3H-pyrido[3,2-d]pyrimidin-6-yl)methylamino]benzoyl]amino]pentanedioic acid | IC50 | 20000.0 [1] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acid | IC50 | 12.0 [1] |
| (2S)-2-[[4-[(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)methyl]benzoyl]amino]pentanedioic acid | IC50 | 1000.0 [1] |
| 2-{4-[3-(2-Amino-4-oxo-3,4-dihydro-pteridin-6-yl)-propyl]-benzoylamino}-pentanedioic acid | IC50 | 25000.0 [1] |