| DB00887 | Bumetanide | approved | unknown | antagonist | Details |
| DB01016 | Glyburide | approved | unknown | antagonist | Details |
| DB04941 | Crofelemer | approved | yes | antagonist | Details |
| DB04395 | Phosphoaminophosphonic Acid-Adenylate Ester | experimental | unknown | | Details |
| DB04522 | Dexfosfoserine | experimental | unknown | | Details |
| DB06266 | Lonidamine | investigational | unknown | | Details |
| DB08820 | Ivacaftor | approved | yes | potentiator | Details |
| DB01050 | Ibuprofen | approved | unknown | inhibitor | Details |
| DB09280 | Lumacaftor | approved | yes | modulator | Details |
| DB09213 | Dexibuprofen | approved, investigational | unknown | inhibitor | Details |
| DB02587 | Colforsin | experimental, investigational | unknown | inhibitor | Details |
| DB00171 | ATP | investigational, nutraceutical | unknown | cofactor | Details |
| DB11712 | Tezacaftor | approved, investigational | yes | activator | Details |
| DB15444 | Elexacaftor | approved, investigational | yes | modulator | Details |
| DB01645 | Genistein | investigational | unknown | activator | Details |