| DB00377 | Palonosetron | approved, investigational | yes | antagonist | Details |
| DB00757 | Dolasetron | approved, investigational | yes | antagonist | Details |
| DB00889 | Granisetron | approved, investigational | yes | antagonist | Details |
| DB00904 | Ondansetron | approved, withdrawn | yes | antagonist | Details |
| DB00969 | Alosetron | approved, withdrawn | yes | antagonist | Details |
| DB00721 | Procaine | approved, investigational, vet_approved | yes | antagonist | Details |
| DB00604 | Cisapride | approved, investigational, withdrawn | yes | agonist | Details |
| DB01199 | Tubocurarine | approved | yes | antagonist | Details |
| DB04885 | Cilansetron | investigational | unknown | | Details |
| DB04917 | Renzapride | investigational | unknown | | Details |
| DB05049 | DDP733 | investigational | unknown | | Details |
| DB05642 | DDP-225 | investigational | unknown | | Details |
| DB06204 | Tapentadol | approved | unknown | | Details |
| DB06422 | Ticalopride | investigational | unknown | | Details |
| DB00363 | Clozapine | approved | unknown | antagonist | Details |
| DB01238 | Aripiprazole | approved, investigational | unknown | antagonist | Details |
| DB00334 | Olanzapine | approved, investigational | unknown | antagonist | Details |
| DB01224 | Quetiapine | approved | unknown | ligand | Details |
| DB00728 | Rocuronium | approved | unknown | antagonist | Details |
| DB01043 | Memantine | approved, investigational | unknown | antagonist | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00543 | Amoxapine | approved | unknown | antagonist | Details |
| DB00726 | Trimipramine | approved | unknown | binder | Details |
| DB00333 | Methadone | approved | unknown | antagonist | Details |
| DB01233 | Metoclopramide | approved, investigational | yes | antagonist | Details |
| DB00898 | Ethanol | approved | unknown | | Details |
| DB09068 | Vortioxetine | approved, investigational | yes | antagonist | Details |
| DB11699 | Tropisetron | approved, investigational | yes | antagonist | Details |
| DB09290 | Ramosetron | investigational | unknown | antagonist | Details |
| DB00988 | Dopamine | approved | unknown | | Details |
| DB08839 | Serotonin | investigational, nutraceutical | unknown | | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB01221 | Ketamine | approved, vet_approved | yes | potentiator | Details |
| DB09061 | Cannabidiol | approved, investigational | unknown | antagonist | Details |
| DB14185 | Aripiprazole lauroxil | approved, investigational | unknown | | Details |
| DB01156 | Bupropion | approved | unknown | negative modulator | Details |