| Methotrexate | IC50 | 106.0 [1], 211.0 [2] |
| Pemetrexed | IC50 | 60.0 [1], 254.0 [2] |
| Raltitrexed | IC50 | 22.0 [1], 746.0 [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 | 0.17 [1], 126.0 [2], 1000.0 [3] |
| 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], 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 | 0.34 [1], 557.0 [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 | 0.1 [1], 654.0 [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 | 3.6 [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 | 1000.0 [1] |
| 4-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanoic acid | IC50 | 1000.0 [1] |
| (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 | 347.0 [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 | 1000.0 [1] |
| (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 | 0.58 [1], 471.0 [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 | 37.41 [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 | 1000.0 [1] |
| (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 | 839.1 [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 | 18.8 [1], 1000.0 [2] |
| (S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acid | IC50 | 17.5 [1], 1000.0 [2] |
| (S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acid | IC50 | 54.3 [1], 1000.0 [2] |