| DB00293 | Raltitrexed | approved, investigational | yes | inhibitor | Details |
| DB00322 | Floxuridine | approved | yes | | Details |
| DB00544 | Fluorouracil | approved | yes | other/unknown | Details |
| DB00642 | Pemetrexed | approved, investigational | yes | inhibitor | Details |
| DB01101 | Capecitabine | approved, investigational | yes | inhibitor | Details |
| DB00441 | Gemcitabine | approved | unknown | inhibitor | Details |
| DB03800 | Deoxyuridine monophosphate | experimental | unknown | | Details |
| DB04530 | S,S-(2-Hydroxyethyl)Thiocysteine | experimental | unknown | | Details |
| DB01643 | Thymidine monophosphate | experimental | unknown | | Details |
| DB00432 | Trifluridine | approved, investigational | yes | inhibitor | Details |
| DB05308 | ANX-510 | investigational | unknown | | Details |
| DB05116 | Thymectacin | investigational | unknown | | Details |
| DB05457 | OSI-7904L | investigational | unknown | | Details |
| DB03541 | 10-Propargyl-5,8-Dideazafolic Acid | experimental | unknown | | Details |
| DB07577 | 2,4-Diamino-5-phenyl-6-ethylpyrimidine | experimental | unknown | | Details |
| DB08478 | N-[2-Chloro-5-(trifluoromethyl)phenyl]imidodicarbonimidic diamide | experimental | unknown | | Details |
| DB08479 | N-(3,5-dimethoxyphenyl)imidodicarbonimidic diamide | experimental | unknown | | Details |
| DB08734 | 6,6-DIMETHYL-1-[3-(2,4,5-TRICHLOROPHENOXY)PROPOXY]-1,6-DIHYDRO-1,3,5-TRIAZINE-2,4-DIAMINE | experimental | unknown | | Details |
| DB00544 | Fluorouracil | approved | unknown | substrate | Details |
| DB00563 | Methotrexate | approved | unknown | substrate | Details |
| DB06813 | Pralatrexate | approved, investigational | unknown | substrateinhibitor | Details |
| DB09327 | Tegafur-uracil | approved, investigational | yes | antagonist | Details |
| DB09256 | Tegafur | approved, investigational | yes | inhibitor | Details |
| DB00563 | Methotrexate | approved | yes | inhibitor | Details |