| Pemetrexed | IC50 | 42.0 [1], 388.0 [2], 894.0 [3] |
| Methotrexate | IC50 | 114.0 [1], 216.0 [2], 461.0 [3] |
| Raltitrexed | IC50 | 15.0 [1], 1000.0 [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 | IC50 | 0.31 [1], 0.38 [2], 173.0 [3], 1000.0 [4] |
| Pralatrexate | IC50 | 168.0 [1], 1000.0 [2] |
| N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic Acid | IC50 | 6.3 [1], 1000.0 [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 | 0.33 [1], 494.0 [2] |
| (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 | 0.61 [1], 506.0 [2] |
| (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 | 9.5 [1], 1000.0 [2] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acid | IC50 | 55.7 [1], 1000.0 [2] |
| 4-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanoic acid | IC50 | 27.4 [1], 1000.0 [2] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanedioic acid | IC50 | 6.6 [1], 1000.0 [2] |
| 5-[3-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-propyl]-thiophene-2-carboxylic acid | IC50 | 661.0 [1], 1000.0 [2] |
| (2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid | IC50 | 1.27 [1], 687.0 [2] |
| (2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-3-carbonyl]amino]pentanedioic acid | IC50 | 15.02 [1], 1000.0 [2] |
| (2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid | IC50 | 1000.0 [1] |
| (2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid | IC50 | 186.0 [1], 1000.0 [2] |
| (2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-3-carbonyl]amino]pentanedioic acid | IC50 | 449.0 [1], 1000.0 [2] |
| (2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid | IC50 | 4.43 [1], 1000.0 [2] |
| (S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acid | IC50 | 154.0 [1], 1000.0 [2] |
| (S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acid | IC50 | 148.0 [1], 1000.0 [2] |
| (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 | 1.82 [1] |
| (2S)-2-[[5-[(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)methyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 1000.0 [1] |
| (2S)-2-[[5-[2-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 550.0 [1] |
| (2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 109.0 [1] |
| (2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 49.3 [1] |
| (2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 45.5 [1] |
| (2S)-2-[[5-[6-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)hexyl]thiophene-2-carbonyl]amino]pentanedioic acid | IC50 | 1000.0 [1] |