| Methotrexate | IC50 | 20.0 [1] |
| Methotrexate | Ki | 0.01 [1] |
| Trimethoprim | IC50 | 198000.0 [1] |
| Trimethoprim | Ki | 1380.0 [1] |
| Pemetrexed | IC50 | 6600.0 [1] |
| Pemetrexed | Ki | 7.0 [1], 7.2 [2] |
| Pyrimethamine | IC50 | 400.0 [1], 2600.0 [2], 4300.0 [3], 6000.0 [4] |
| Pyrimethamine | Ki | 98.0 [1] |
| Trimetrexate | IC50 | 12.2 [1] |
| Trimetrexate | Ki | 1.4 [1], 13.0 [2], 83.0 [3] |
| Aminopterin | IC50 | 25.0 [1] |
| Aminopterin | Ki | 0.0 [1], 0.21 [2] |
| L-Glutamic acid, N-(4-(((2-amino-1,4-dihydro-4-oxo-6-quinazolinyl)methyl)-2-propynylamino)benzoyl)- | IC50 | 1900.0 [1] |
| Piritrexim | IC50 | 2.0 [1], 3.0 [2] |
| Piritrexim | Ki | 0.03 [1], 33.0 [2], 38.0 [3] |
| N-[4-[2-(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid | IC50 | 1000.0 [1] |
| (2S)-2-[[4-[(2-Amino-6-methyl-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]amino]pentanedioic acid | IC50 | 2100.0 [1], 2200.0 [2] |
| Iclaprim | IC50 | 8.0 [1], 30000.0 [2] |
| Iclaprim | Ki | 775.0 [1] |
| 2,4-Diamino-5-(3-methoxybenzyl)pyrimidine | Ki | 9.6 [1], 300.0 [2], 1000.0 [3], 2300.0 [4] |
| 2,4-Diamino-5-[3-benzyloxybenzyl]pyrimidine | Ki | 11.0 [1], 65.0 [2], 200.0 [3], 1000.0 [4] |
| 2,4-Diamino-5-[3-octyloxybenzyl]pyrimidine | Ki | 24.0 [1], 97.0 [2], 1130.0 [3], 2400.0 [4] |
| 2,4-Diamino-5-[3-hexyloxybenzyl]pyrimidine | Ki | 9.8 [1], 171.0 [2], 600.0 [3], 1900.0 [4] |
| 2,4-Diamino-5-[3-butoxybenzyl]pyrimidine | Ki | 3.6 [1], 150.0 [2], 220.0 [3], 930.0 [4] |
| 2,4-Diamino-5-[3-heptyloxybenzyl]pyrimidine | Ki | 131.0 [1], 221.0 [2], 620.0 [3], 1330.0 [4] |
| Dpmabg | IC50 | 220.0 [1], 450.0 [2] |
| 5-(4-Propoxybenzyl)pyrimidine-2,4-diamine | Ki | 6.4 [1], 230.0 [2], 330.0 [3], 2900.0 [4] |
| 5-(4-Ethoxybenzyl)pyrimidine-2,4-diamine | Ki | 9.8 [1], 130.0 [2], 210.0 [3], 6000.0 [4] |
| 5-[3-(Nonyloxy)benzyl]pyrimidine-2,4-diamine | Ki | 36.0 [1], 360.0 [2], 990.0 [3] |
| 5-[3-(Decyloxy)benzyl]pyrimidine-2,4-diamine | Ki | 52.0 [1], 750.0 [2], 2220.0 [3], 3110.0 [4] |
| 5-[3-(Heptyloxy)benzyl]-6-methylpyrimidine-2,4-diamine | Ki | 75.0 [1], 370.0 [2], 1000.0 [3], 1500.0 [4] |
| 5-(3-Pentyloxy-benzyl)-pyrimidine-2,4-diamine | Ki | 7.1 [1], 140.0 [2], 210.0 [3], 1100.0 [4] |
| 5-(3-Ethoxybenzyl)pyrimidine-2,4-diamine | Ki | 8.6 [1], 156.0 [2], 430.0 [3], 1600.0 [4] |
| 5-(3-Propoxybenzyl)pyrimidine-2,4-diamine | Ki | 10.5 [1], 130.0 [2], 510.0 [3], 2400.0 [4] |
| 5-(3-Isopropoxybenzyl)pyrimidine-2,4-diamine | Ki | 8.8 [1], 23.0 [2], 160.0 [3], 1400.0 [4] |
| 5-[3-(Tetrahydro-pyran-2-yloxy)-benzyl]-pyrimidine-2,4-diamine | Ki | 13.0 [1], 93.0 [2], 360.0 [3], 1300.0 [4] |
| 5-[3-(Heptyloxy)benzyl]-6-ethylpyrimidine-2,4-diamine | Ki | 19.0 [1], 48.0 [2], 400.0 [3], 710.0 [4] |
| 5-[(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)methyl]pyrimidine-2,4-diamine | IC50 | 10.0 [1], 210.0 [2], 30000.0 [3] |
| Cycloguanil | Ki | 55.6 [1], 410.0 [2], 43000.0 [3] |
| 10-Propargyl-5,8-dideazafolic acid | IC50 | 1900.0 [1], 11000.0 [2] |
| Epiroprim | IC50 | 200.0 [1], 600000.0 [2] |
| Epiroprim | Ki | 58.88 [1] |
| 2-[[4-Carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acid | IC50 | 1.1 [1], 12.2 [2] |
| 2-[[4-Carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acid | Ki | 0.0 [1] |
| 2,4-Diamino-5-[3-hydroxybenzyl]pyrimidine | Ki | 750.0 [1], 990.0 [2], 3300.0 [3] |
| 2,4-Diamino-5-[2-Methoxy-5-(4-Carboxybutyloxy)benzyl]pyrimidine | IC50 | 5000.0 [1], 8000.0 [2] |
| 2-{4-[(2,4-Diamino-quinazolin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acid | IC50 | 4.5 [1] |
| 2-{4-[(2,4-Diamino-quinazolin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acid | Ki | 0.0 [1], 0.01 [2] |
| 2-(4-((2-Amino-4-hydroxyquinazolin-6-yl) methylthio)benzamido)pentanedioic acid | IC50 | 330.0 [1] |
| 5-[3-(3-Methoxy-5-phenyl-phenyl)but-1-ynyl]-6-methyl-pyrimidine-2,4-diamine | IC50 | 1700.0 [1] |
| 5-[3-(3-Methoxy-4-phenyl-phenyl)but-1-ynyl]-6-methyl-pyrimidine-2,4-diamine | IC50 | 1420.0 [1] |
| 2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methoxy]benzoyl]amino]pentanedioic acid | IC50 | 170.0 [1] |
| Furo[2,3d]pyrimidine antifolate | IC50 | 220.0 [1] |
| 5-[3-(2,5-Dimethoxyphenyl)prop-1-Yn-1-Yl]-6-Ethylpyrimidine-2,4-Diamine | IC50 | 1280.0 [1] |
| 5-[3-[3-Methoxy-5-(p-tolyl)phenyl]but-1-ynyl]-6-methyl-pyrimidine-2,4-diamine | IC50 | 1400.0 [1], 1410.0 [2] |
| 5-Amino-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanoic acid | IC50 | 1.0 [1], 2.5 [2], 160.0 [3] |
| 2,4-Diamino-5-[3-(3-methoxy-5-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | IC50 | 1360.0 [1] |
| 5-[3-[3-(2,6-Dimethylphenyl)-5-methoxy-phenyl]but-1-ynyl]-6-methyl-pyrimidine-2,4-diamine | IC50 | 1250.0 [1] |
| 2,4-Diamino-5-[3-(3-methoxy-5-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidine | IC50 | 7200.0 [1] |
| 5-[(3r)-3-(5-Methoxybiphenyl-3-Yl)but-1-Yn-1-Yl]-6-Methylpyrimidine-2,4-Diamine | IC50 | 1360.0 [1] |
| 2-(4-{[(2,4-Diamino-furo[2,3-d]pyrimidin-5-ylmethyl)-amino]-methyl}-benzoylamino)-pentanedioic acid | IC50 | 10000.0 [1], 30500.0 [2], 200000.0 [3] |
| 5-[(3S)-3-(3-Methoxy-5-phenylphenyl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine | IC50 | 1380.0 [1] |
| 5-[[(9R)-4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl]methyl]pyrimidine-2,4-diamine | IC50 | 2.8 [1], 9.8 [2], 1200.0 [3] |
| 5-[[7-Methoxy-4-(3-nitrophenyl)-3,4-dihydro-1H-isoquinolin-2-yl]methyl]pyrimidine-2,4-diamine | IC50 | 6.0 [1], 56.0 [2], 100000.0 [3] |
| 5-[(4,11-Dimethyl-2,4-dihydro-1H-pyrido[4,3-a]carbazol-3-yl)methyl]pyrimidine-2,4-diamine | IC50 | 4.0 [1], 10.0 [2], 85.0 [3] |
| 5-[(6,7-Dimethoxy-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl)methyl]pyrimidine-2,4-diamine | IC50 | 44.0 [1], 53.0 [2], 670.0 [3] |
| 5-[(7-Chloro-10-methylsulfanyl-3,4-dihydro-1H-pyrazino[1,2-a]indol-2-yl)methyl]pyrimidine-2,4-diamine | IC50 | 2.0 [1], 31.0 [2], 5200.0 [3] |
| 5-[(7-Benzyl-1-methyl-6-phenyl-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl)methyl]pyrimidine-2,4-diamine | IC50 | 450.0 [1], 550.0 [2], 18000.0 [3] |
| 5-[[(9S)-4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl]methyl]pyrimidine-2,4-diamine | IC50 | 21.0 [1], 29.0 [2], 520.0 [3] |
| 5-[[4-(2,4-Dichlorophenyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]methyl]pyrimidine-2,4-diamine | IC50 | 7.0 [1], 31.0 [2], 1700.0 [3] |
| 5-(1,3,4,9-Tetrahydropyrido[3,4-b]indol-2-ylmethyl)pyrimidine-2,4-diamine | IC50 | 4.0 [1], 47.0 [2], 180000.0 [3] |
| 2,4-Pyrimidinediamine, 5-[(3,4-dihydro-2(1H)-isoquinolinyl)methyl]- | IC50 | 1100.0 [1], 5500.0 [2], 100000.0 [3] |
| 5-[(4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl)methyl]pyrimidine-2,4-diamine | IC50 | 12.0 [1], 24.0 [2], 1400.0 [3] |
| Raltitrexed | IC50 | 21000.0 [1] |
| Edatrexato | IC50 | 2.6 [1], 4.4 [2] |
| 1,3,5-Triazine-2,4-diamine, 1-(3-chlorophenyl)-1,6-dihydro-6,6-dimethyl- | Ki | 93.33 [1], 100.0 [2] |
| 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine | Ki | 1.0 [1], 1000.0 [2] |
| N6-(2,5-Dimethoxy-benzyl)-N6-methyl-pyrido[2,3-D]pyrimidine-2,4,6-triamine | IC50 | 8500.0 [1] |
| 5-Methyl-6-(1-naphthylaminomethyl)pyrido[2,3-d]pyrimidine-2,4-diamine | IC50 | 4.3 [1], 100.0 [2] |
| 6-Methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-ynyl]pyrimidine-2,4-diamine | IC50 | 1380.0 [1] |
| 2-[[4-[[(2-Amino-4-oxo-3H-quinazolin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acid | IC50 | 110.0 [1] |
| 3-(2,4-Diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol | IC50 | 5710.0 [1] |
| 2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)-6-methylpyrimidine | IC50 | 400.0 [1] |
| 2,4-Diamino-5-(3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)-6-methylpyrimidine | IC50 | 1220.0 [1] |
| 5-[(4-Methylphenyl)sulfanyl]-2,4-quinazolinediamine | IC50 | 940.0 [1] |
| 2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)pyrimidine | IC50 | 1460.0 [1] |
| 2,4-Diamino-5-(3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)pyrimidine | IC50 | 1160.0 [1] |
| 2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)but-1-ynyl)pyrimidine | IC50 | 1460.0 [1] |
| 3-(2,4-Diaminopyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol | IC50 | 14300.0 [1] |
| 1,3-Diamino-7-(1-ethylpropyl)-8-methyl-7H-pyrrolo(3,2-f)quinazoline | Ki | 0.0 [1], 0.3 [2] |
| 6-Ethyl-5-[3-(3,4,5-Trimethoxyphenyl)prop-1-Yn-1-Yl]pyrimidine-2,4-Diamine | IC50 | 57.0 [1] |
| 5-Phenylsulfanyl-2,4-quinazolinediamine | IC50 | 620.0 [1] |
| 6-N-[(2,5-Dimethoxyphenyl)methyl]pyrido[2,3-d]pyrimidine-2,4,6-triamine | IC50 | 13000.0 [1] |
| 5-[3-[(2,4-Diaminopyrimidin-5-yl)methyl]-4-methoxy-phenyl]pent-4-ynoic acid | IC50 | 5000.0 [1], 30000.0 [2] |
| 6-Methyl-5-[(3R)-3-(3,4,5-trimethoxyphenyl)but-1-ynyl]pyrimidine-2,4-diamine | IC50 | 1380.0 [1] |
| 5-[3-(2,5-Dimethoxyphenyl)prop-1-ynyl]-6-methyl-pyrimidine-2,4-diamine | IC50 | 1300.0 [1] |
| 2-[[4-[(2,4-Diamino-5-chloroquinazolin-6-yl)methylamino]benzoyl]amino]pentanedioic acid | IC50 | 3.8 [1] |
| 6-N-[(3,4,5-Trimethoxyphenyl)methyl]pyrido[2,3-d]pyrimidine-2,4,6-triamine | IC50 | 76000.0 [1] |
| (2S)-2-[[4-[(2,4-Diamino-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)sulfanyl]benzoyl]amino]pentanedioic acid | IC50 | 210.0 [1] |
| 5-Amino-2-[[4-[(2-amino-5-chloro-4-oxo-3H-quinazolin-6-yl)methylamino]benzoyl]amino]pentanoic acid | IC50 | 430.0 [1] |