| DB00422 | Methylphenidate | approved, investigational | yes | inhibitor | Details |
| DB00745 | Modafinil | approved, investigational | yes | inhibitor | Details |
| DB01156 | Bupropion | approved | yes | inhibitor | Details |
| DB00191 | Phentermine | approved, illicit | yes | inhibitor | Details |
| DB00476 | Duloxetine | approved | unknown | inhibitor | Details |
| DB00579 | Mazindol | approved, investigational | yes | inhibitor | Details |
| DB00721 | Procaine | approved, investigational, vet_approved | yes | inhibitor | Details |
| DB00830 | Phenmetrazine | approved, illicit | yes | inhibitor | Details |
| DB00907 | Cocaine | approved, illicit | yes | inhibitor | Details |
| DB00937 | Diethylpropion | approved, illicit | yes | inhibitor | Details |
| DB01161 | Chloroprocaine | approved, investigational | unknown | inhibitor | Details |
| DB00182 | Amphetamine | approved, illicit, investigational | yes | negative modulator | Details |
| DB00245 | Benzatropine | approved | yes | inhibitor | Details |
| DB01463 | Fencamfamin | experimental, illicit, withdrawn | yes | inhibitor | Details |
| DB04947 | Altropane | investigational | unknown | | Details |
| DB01576 | Dextroamphetamine | approved, illicit | yes | negative modulator | Details |
| DB12305 | Dasotraline | investigational | unknown | | Details |
| DB06156 | Tesofensine | investigational | unknown | | Details |
| DB06333 | Trodusquemine | investigational | unknown | | Details |
| DB01149 | Nefazodone | approved, withdrawn | unknown | inhibitor | Details |
| DB04821 | Nomifensine | approved, withdrawn | unknown | | Details |
| DB01104 | Sertraline | approved | unknown | inhibitorbinder | Details |
| DB01146 | Diphenylpyraline | approved, investigational | unknown | inhibitor | Details |
| DB01175 | Escitalopram | approved | no | inhibitor | Details |
| DB00726 | Trimipramine | approved | unknown | inhibitor | Details |
| DB01114 | Chlorpheniramine | approved | unknown | inhibitor | Details |
| DB01105 | Sibutramine | approved, illicit, investigational, withdrawn | yes | inhibitor | Details |
| DB00285 | Venlafaxine | approved | unknown | inhibitor | Details |
| DB00988 | Dopamine | approved | yes | inducer | Details |
| DB00865 | Benzphetamine | approved, illicit | unknown | inhibitor | Details |
| DB06701 | Dexmethylphenidate | approved, investigational | yes | inhibitor | Details |
| DB01454 | Midomafetamine | experimental, illicit, investigational | unknown | negative modulator | Details |
| DB00852 | Pseudoephedrine | approved | yes | inhibitor | Details |
| DB01472 | 4-Methoxyamphetamine | experimental, illicit | yes | inhibitor | Details |
| DB01577 | Metamfetamine | approved, illicit, withdrawn | yes | negative modulator | Details |
| DB01363 | Ephedra sinica root | nutraceutical | yes | negative modulator | Details |
| DB01442 | MMDA | experimental, illicit | yes | negative modulator | Details |
| DB01454 | Midomafetamine | experimental, illicit, investigational | unknown | | Details |
| DB08824 | Ioflupane I-123 | approved | no | | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00458 | Imipramine | approved | unknown | inhibitor | Details |
| DB00454 | Meperidine | approved | unknown | inhibitor | Details |
| DB00543 | Amoxapine | approved | unknown | binder | Details |
| DB06148 | Mianserin | approved, investigational | unknown | binder | Details |
| DB06413 | Armodafinil | approved, investigational | yes | antagonistinhibitor | Details |
| DB03701 | Vanoxerine | investigational | yes | antagonist | Details |
| DB09194 | Etoperidone | withdrawn | no | inhibitor | Details |
| DB14754 | Solriamfetol | approved | unknown | | Details |
| DB01576 | Dextroamphetamine | approved, illicit | unknown | | Details |
| DB06700 | Desvenlafaxine | approved, investigational | unknown | inhibitor | Details |
| DB01238 | Aripiprazole | approved, investigational | unknown | modulator | Details |
| DB00852 | Pseudoephedrine | approved | unknown | inhibitor | Details |
| DB00907 | Cocaine | approved, illicit | no | inhibitor | Details |
| DB00721 | Procaine | approved, investigational, vet_approved | unknown | inhibitor | Details |
| DB16629 | Serdexmethylphenidate | approved | yes | inhibitor | Details |