| DB00772 | Malathion | approved, investigational | yes | inhibitor | Details |
| DB03672 | 9-N-Phenylmethylamino-Tacrine | experimental | unknown | | Details |
| DB00122 | Choline | approved, nutraceutical | unknown | product of | Details |
| DB00989 | Rivastigmine | approved, investigational | yes | inhibitor | Details |
| DB00677 | Isoflurophate | approved, investigational, withdrawn | yes | inhibitor | Details |
| DB00941 | Hexafluronium | approved | yes | inhibitor | Details |
| DB00944 | Demecarium | approved | unknown | inhibitor | Details |
| DB01057 | Echothiophate | approved | yes | inhibitor | Details |
| DB02811 | Diethyl phosphonate | experimental | unknown | | Details |
| DB03568 | Butyric Acid | experimental, investigational | unknown | | Details |
| DB03814 | 2-(N-morpholino)ethanesulfonic acid | experimental | unknown | | Details |
| DB03822 | Ethyl dihydrogen phosphate | experimental | unknown | | Details |
| DB04250 | Butyrylthiocholine | experimental | unknown | substrate | Details |
| DB01400 | Neostigmine | approved, vet_approved | unknown | inhibitor | Details |
| DB00202 | Succinylcholine | approved | no | substrate | Details |
| DB00358 | Mefloquine | approved, investigational | unknown | inhibitor | Details |
| DB00392 | Profenamine | approved | unknown | inhibitor | Details |
| DB00477 | Chlorpromazine | approved, investigational, vet_approved | unknown | inhibitor | Details |
| DB00527 | Cinchocaine | approved, vet_approved | unknown | inhibitor | Details |
| DB00871 | Terbutaline | approved | unknown | inhibitor | Details |
| DB01035 | Procainamide | approved | unknown | inhibitor | Details |
| DB01116 | Trimethaphan | approved, investigational | unknown | substrate | Details |
| DB01122 | Ambenonium | approved | unknown | inhibitor | Details |
| DB01337 | Pancuronium | approved | unknown | inhibitor | Details |
| DB01408 | Bambuterol | investigational | unknown | substrateinhibitor | Details |
| DB03568 | Butyric Acid | experimental, investigational | unknown | ligand | Details |
| DB03822 | Ethyl dihydrogen phosphate | experimental | unknown | ligand | Details |
| DB04250 | Butyrylthiocholine | experimental | unknown | substrate | Details |
| DB03976 | Phosphorylisopropane | experimental | unknown | ligand | Details |
| DB00382 | Tacrine | approved, investigational, withdrawn | yes | inhibitor | Details |
| DB00449 | Dipivefrin | approved | yes | substrate | Details |
| DB07681 | DODECANESULFONATE ION | experimental | unknown | | Details |
| DB07940 | 9-(3-IODOBENZYLAMINO)-1,2,3,4-TETRAHYDROACRIDINE | experimental | unknown | | Details |
| DB08200 | (1R)-menthyl hexyl phosphonate group | experimental | unknown | | Details |
| DB08201 | (1S)-menthyl hexyl phosphonate group | experimental | unknown | | Details |
| DB08658 | Ethyl hydrogen diethylamidophosphate | experimental | unknown | | Details |
| DB02845 | Methylphosphinic Acid | experimental | unknown | | Details |
| DB02845 | Methylphosphinic Acid | experimental | unknown | inhibitor | Details |
| DB00545 | Pyridostigmine | approved, investigational | yes | inhibitor | Details |
| DB00674 | Galantamine | approved | unknown | inhibitor | Details |
| DB00677 | Isoflurophate | approved, investigational, withdrawn | unknown | inhibitor | Details |
| DB00733 | Pralidoxime | approved, vet_approved | yes | activator | Details |
| DB01010 | Edrophonium | approved | yes | inhibitor | Details |
| DB01226 | Mivacurium | approved | unknown | | Details |
| DB04892 | Phenserine | investigational | unknown | inhibitor | Details |
| DB06756 | Betaine | approved, investigational, nutraceutical | unknown | inhibitor | Details |
| DB06774 | Capsaicin | approved | unknown | inhibitor | Details |
| DB01161 | Chloroprocaine | approved, investigational | unknown | substrate | Details |
| DB00856 | Chlorphenesin | approved, experimental | unknown | inducer | Details |
| DB04920 | Clevidipine | approved, investigational | unknown | substrate | Details |
| DB00979 | Cyclopentolate | approved | unknown | substrate | Details |
| DB01245 | Decamethonium | approved | unknown | inhibitor | Details |
| DB00711 | Diethylcarbamazine | approved, investigational, vet_approved | unknown | inhibitor | Details |
| DB01135 | Doxacurium | approved | unknown | substrate | Details |
| DB01364 | Ephedrine | approved | unknown | substrate | Details |
| DB00585 | Nizatidine | approved | unknown | inhibitor | Details |
| DB00892 | Oxybuprocaine | approved, investigational | unknown | substrate | Details |
| DB00082 | Pegvisomant | approved | unknown | inhibitor | Details |
| DB00183 | Pentagastrin | approved | unknown | inducer | Details |
| DB00790 | Perindopril | approved | unknown | inhibitor | Details |
| DB01338 | Pipecuronium | approved | unknown | inhibitor | Details |
| DB00515 | Cisplatin | approved | unknown | inhibitor | Details |
| DB00721 | Procaine | approved, investigational, vet_approved | unknown | substrateinhibitor | Details |
| DB00178 | Ramipril | approved | unknown | inhibitor | Details |
| DB05386 | Regramostim | investigational | unknown | inhibitor | Details |
| DB05875 | Sar9, Met (O2)11-Substance P | investigational | unknown | substrate | Details |
| DB00391 | Sulpiride | approved, investigational | unknown | inhibitor | Details |
| DB00620 | Triamcinolone | approved, vet_approved | unknown | inducer | Details |
| DB00508 | Triflupromazine | approved, vet_approved | unknown | inhibitor | Details |
| DB08893 | Mirabegron | approved | no | substrate | Details |
| DB08897 | Aclidinium | approved | no | substrate | Details |
| DB00762 | Irinotecan | approved, investigational | unknown | substrate | Details |
| DB11397 | Dichlorvos | vet_approved | unknown | | Details |
| DB09205 | Moxisylyte | approved, investigational | no | substrate | Details |
| DB01221 | Ketamine | approved, vet_approved | yes | inhibitor | Details |
| DB09288 | Propacetamol | experimental | no | substrate | Details |
| DB14006 | Choline salicylate | approved, nutraceutical | unknown | product of | Details |
| DB11148 | Butamben | approved, withdrawn | no | substrate | Details |
| DB01199 | Tubocurarine | approved | no | substrate | Details |
| DB06692 | Aprotinin | approved, investigational, withdrawn | no | inhibitor | Details |
| DB04572 | Thiotepa | approved, investigational | no | inhibitor | Details |
| DB00888 | Mechlorethamine | approved, investigational | no | inhibitor | Details |
| DB14031 | Tretamine | experimental | no | inhibitor | Details |
| DB00907 | Cocaine | approved, illicit | no | substrate | Details |
| DB00843 | Donepezil | approved | unknown | inducer | Details |
| DB00868 | Benzonatate | approved | no | substrate | Details |
| DB00545 | Pyridostigmine | approved, investigational | no | substrate | Details |
| DB01226 | Mivacurium | approved | unknown | substrate | Details |
| DB03128 | Acetylcholine | approved, investigational | no | substrate | Details |
| DB01064 | Isoprenaline | approved, investigational | no | inhibitor | Details |
| DB01408 | Bambuterol | investigational | unknown | inhibitor | Details |
| DB06636 | Isavuconazonium | approved, investigational | no | substrate | Details |