| DB00191 | Phentermine | approved, illicit | yes | inhibitor | Details |
| DB00234 | Reboxetine | approved, experimental | yes | inhibitor | Details |
| DB00289 | Atomoxetine | approved | yes | inhibitor | Details |
| DB00344 | Protriptyline | approved | yes | inhibitor | Details |
| DB00458 | Imipramine | approved | yes | inhibitor | Details |
| DB00579 | Mazindol | approved, investigational | yes | inhibitor | Details |
| DB00830 | Phenmetrazine | approved, illicit | yes | inhibitor | Details |
| DB00937 | Diethylpropion | approved, illicit | yes | inhibitor | Details |
| DB00193 | Tramadol | approved, investigational | yes | inhibitor | Details |
| DB00226 | Guanadrel | approved | yes | partial agonist | Details |
| DB00285 | Venlafaxine | approved | yes | inhibitor | Details |
| DB00321 | Amitriptyline | approved | yes | inhibitor | Details |
| DB00422 | Methylphenidate | approved, investigational | unknown | inhibitor | Details |
| DB00476 | Duloxetine | approved | yes | inhibitor | Details |
| DB00540 | Nortriptyline | approved | yes | inhibitor | Details |
| DB00543 | Amoxapine | approved | unknown | inhibitor | Details |
| DB00726 | Trimipramine | approved | yes | inhibitor | Details |
| DB00907 | Cocaine | approved, illicit | yes | inhibitor | Details |
| DB00934 | Maprotiline | approved, investigational | yes | inhibitor | Details |
| DB01105 | Sibutramine | approved, illicit, investigational, withdrawn | yes | inhibitor | Details |
| DB01142 | Doxepin | approved, investigational | yes | inhibitor | Details |
| DB01149 | Nefazodone | approved, withdrawn | yes | inhibitor | Details |
| DB01151 | Desipramine | approved, investigational | yes | inhibitor | Details |
| DB01156 | Bupropion | approved | yes | inhibitor | Details |
| DB01170 | Guanethidine | approved | yes | inducer | Details |
| DB01242 | Clomipramine | approved, investigational, vet_approved | unknown | inhibitor | Details |
| DB00715 | Paroxetine | approved, investigational | unknown | inhibitor | Details |
| DB04836 | Amineptine | illicit, withdrawn | unknown | | Details |
| DB04840 | Debrisoquine | approved, investigational | yes | inducer | Details |
| DB04889 | Bicifadine | investigational | unknown | | Details |
| DB04896 | Milnacipran | approved, investigational | yes | inhibitor | Details |
| DB05012 | XEN-2174 | investigational | unknown | | Details |
| DB05688 | CRx-119 | investigational | unknown | | Details |
| DB12305 | Dasotraline | investigational | unknown | | Details |
| DB06156 | Tesofensine | investigational | unknown | | Details |
| DB05964 | Amitifadine | investigational | unknown | | Details |
| DB05642 | DDP-225 | investigational | unknown | | Details |
| DB06204 | Tapentadol | approved | unknown | inhibitor | Details |
| DB06333 | Trodusquemine | investigational | unknown | | Details |
| DB04821 | Nomifensine | approved, withdrawn | unknown | | Details |
| DB01175 | Escitalopram | approved | unknown | inhibitor | Details |
| DB01114 | Chlorpheniramine | approved | unknown | inhibitor | Details |
| DB01381 | Ginkgo biloba | approved, investigational, nutraceutical | unknown | inhibitor | Details |
| DB01173 | Orphenadrine | approved | yes | inhibitor | Details |
| DB06700 | Desvenlafaxine | approved, investigational | yes | inhibitor | Details |
| DB06148 | Mianserin | approved, investigational | unknown | inhibitor | Details |
| DB06701 | Dexmethylphenidate | approved, investigational | yes | inhibitor | Details |
| DB00852 | Pseudoephedrine | approved | yes | inhibitor | Details |
| DB01576 | Dextroamphetamine | approved, illicit | yes | negative modulator | Details |
| DB01579 | Phendimetrazine | approved, illicit | yes | negative modulator | Details |
| DB01363 | Ephedra sinica root | nutraceutical | yes | negative modulator | Details |
| DB01442 | MMDA | experimental, illicit | yes | negative modulator | Details |
| DB01577 | Metamfetamine | approved, illicit, withdrawn | yes | negative modulator | Details |
| DB01454 | Midomafetamine | experimental, illicit, investigational | yes | negative modulator | Details |
| DB01364 | Ephedrine | approved | unknown | inverse agonist | Details |
| DB00368 | Norepinephrine | approved | unknown | substrate | Details |
| DB06262 | Droxidopa | approved, investigational | unknown | substrate | Details |
| DB01454 | Midomafetamine | experimental, illicit, investigational | unknown | | Details |
| DB06704 | Iobenguane | approved, investigational | no | substrate | Details |
| DB08918 | Levomilnacipran | approved, investigational | yes | inhibitor | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00182 | Amphetamine | approved, illicit, investigational | unknown | agonistsubstrate | Details |
| DB00514 | Dextromethorphan | approved | unknown | inhibitor | Details |
| DB00988 | Dopamine | approved | unknown | inhibitor | Details |
| DB00454 | Meperidine | approved | unknown | inhibitor | Details |
| DB01221 | Ketamine | approved, vet_approved | unknown | inhibitor | Details |
| DB09068 | Vortioxetine | approved, investigational | unknown | blocker | Details |
| DB09546 | Iobenguane sulfate I-123 | approved, investigational | no | substrate | Details |
| DB09167 | Dosulepin | approved | yes | inhibitor | Details |
| DB09185 | Viloxazine | approved, investigational, withdrawn | yes | inhibitor | Details |
| DB09194 | Etoperidone | withdrawn | no | inhibitor | Details |
| DB13931 | Netarsudil | approved | yes | inhibitor | Details |
| DB09225 | Zotepine | approved, investigational, withdrawn | yes | antagonist | Details |
| DB09363 | Rauwolfia serpentina root | investigational | unknown | inhibitor | Details |
| DB00245 | Benzatropine | approved | no | inhibitor | Details |
| DB14754 | Solriamfetol | approved | unknown | | Details |
| DB00924 | Cyclobenzaprine | approved | unknown | inhibitor | Details |
| DB01104 | Sertraline | approved | unknown | inhibitordownregulator | Details |
| DB00852 | Pseudoephedrine | approved | unknown | inhibitor | Details |
| DB00540 | Nortriptyline | approved | unknown | substrateinhibitor | Details |
| DB00721 | Procaine | approved, investigational, vet_approved | unknown | inhibitor | Details |
| DB16629 | Serdexmethylphenidate | approved | yes | inhibitor | Details |