| DB00490 | Buspirone | approved, investigational | yes | partial agonist | Details |
| DB00216 | Eletriptan | approved, investigational | unknown | agonist | Details |
| DB00246 | Ziprasidone | approved | yes | agonist | Details |
| DB01238 | Aripiprazole | approved, investigational | unknown | partial agonist | Details |
| DB00247 | Methysergide | approved | yes | agonist | Details |
| DB00363 | Clozapine | approved | unknown | antagonist | Details |
| DB00589 | Lisuride | approved, investigational | unknown | agonist | Details |
| DB00656 | Trazodone | approved, investigational | yes | antagonistpartial agonist | Details |
| DB00866 | Alprenolol | experimental, withdrawn | yes | antagonist | Details |
| DB00960 | Pindolol | approved, investigational | unknown | antagonistinhibitorligand | Details |
| DB01224 | Quetiapine | approved | unknown | antagonistpartial agonist | Details |
| DB04884 | Dapoxetine | investigational | unknown | | Details |
| DB04888 | Bifeprunox | investigational | unknown | | Details |
| DB04908 | Flibanserin | approved, investigational | yes | agonist | Details |
| DB04970 | Lesopitron | investigational | unknown | | Details |
| DB12061 | Pardoprunox | investigational | unknown | | Details |
| DB05339 | MN-305 | investigational | unknown | | Details |
| DB05509 | LI-301 | investigational | unknown | | Details |
| DB00571 | Propranolol | approved, investigational | unknown | other/unknown | Details |
| DB06216 | Asenapine | approved | unknown | antagonist | Details |
| DB06393 | Xaliproden | investigational | unknown | | Details |
| DB06506 | Repinotan | investigational | unknown | | Details |
| DB06446 | Dotarizine | investigational | unknown | | Details |
| DB06454 | Sarizotan | investigational | unknown | | Details |
| DB06538 | Robalzotan | investigational | unknown | | Details |
| DB06684 | Vilazodone | approved | unknown | agonist | Details |
| DB01186 | Pergolide | approved, investigational, vet_approved, withdrawn | unknown | agonist | Details |
| DB01200 | Bromocriptine | approved, investigational, withdrawn | unknown | agonist | Details |
| DB00248 | Cabergoline | approved | unknown | agonist | Details |
| DB00413 | Pramipexole | approved, investigational | unknown | agonist | Details |
| DB05271 | Rotigotine | approved | unknown | agonist | Details |
| DB00714 | Apomorphine | approved, investigational | unknown | agonist | Details |
| DB01267 | Paliperidone | approved | unknown | antagonist | Details |
| DB01618 | Molindone | approved | unknown | antagonist | Details |
| DB00321 | Amitriptyline | approved | unknown | inhibitorinducer | Details |
| DB01142 | Doxepin | approved, investigational | unknown | antagonist | Details |
| DB01149 | Nefazodone | approved, withdrawn | yes | antagonist | Details |
| DB00540 | Nortriptyline | approved | unknown | antagonist | Details |
| DB00726 | Trimipramine | approved | unknown | antagonist | Details |
| DB01392 | Yohimbine | approved, investigational, vet_approved | unknown | partial agonist | Details |
| DB00952 | Naratriptan | approved, investigational | yes | agonist | Details |
| DB00315 | Zolmitriptan | approved, investigational | no | agonist | Details |
| DB00669 | Sumatriptan | approved, investigational | yes | agonist | Details |
| DB00477 | Chlorpromazine | approved, investigational, vet_approved | yes | antagonist | Details |
| DB08807 | Bopindolol | experimental | unknown | | Details |
| DB00904 | Ondansetron | approved, withdrawn | unknown | other/unknown | Details |
| DB01616 | Alverine | approved, investigational | yes | antagonist | Details |
| DB01614 | Acepromazine | experimental, vet_approved | yes | antagonist | Details |
| DB01621 | Pipotiazine | approved, investigational | yes | antagonist | Details |
| DB08810 | Cinitapride | investigational | yes | agonist | Details |
| DB04946 | Iloperidone | approved | unknown | antagonist | Details |
| DB08815 | Lurasidone | approved, investigational | unknown | antagonist | Details |
| DB01359 | Penbutolol | approved, investigational | yes | antagonist | Details |
| DB04829 | Lysergic acid diethylamide | illicit, investigational, withdrawn | unknown | | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00458 | Imipramine | approved | unknown | activator | Details |
| DB00543 | Amoxapine | approved | unknown | antagonist | Details |
| DB00988 | Dopamine | approved | unknown | binder | Details |
| DB00696 | Ergotamine | approved | unknown | agonist | Details |
| DB01151 | Desipramine | approved, investigational | unknown | binder | Details |
| DB06148 | Mianserin | approved, investigational | unknown | blocker | Details |
| DB09068 | Vortioxetine | approved, investigational | yes | agonist | Details |
| DB09128 | Brexpiprazole | approved, investigational | unknown | partial agonist | Details |
| DB08922 | Perospirone | experimental | yes | partial agonist | Details |
| DB09167 | Dosulepin | approved | yes | antagonist | Details |
| DB09061 | Cannabidiol | approved, investigational | unknown | agonist | Details |
| DB09244 | Pirlindole | experimental | unknown | antagonist | Details |
| DB06153 | Pizotifen | approved | unknown | partial agonist | Details |
| DB14010 | 5-methoxy-N,N-dimethyltryptamine | experimental, illicit | unknown | agonist | Details |
| DB14011 | Nabiximols | investigational | unknown | | Details |
| DB14009 | Medical Cannabis | experimental, investigational | unknown | | Details |
| DB11755 | Tetrahydrocannabivarin | investigational | yes | agonist | Details |
| DB04948 | Lofexidine | approved, investigational | no | agonist | Details |
| DB05562 | Naluzotan | investigational | unknown | agonist | Details |
| DB09289 | Tianeptine | investigational | unknown | inhibitor | Details |
| DB14185 | Aripiprazole lauroxil | approved, investigational | yes | partial agonist | Details |
| DB00422 | Methylphenidate | approved, investigational | unknown | | Details |
| DB00502 | Haloperidol | approved | unknown | | Details |
| DB01175 | Escitalopram | approved | unknown | inhibitor | Details |
| DB15665 | SEP-363856 | investigational | unknown | agonist | Details |
| DB00734 | Risperidone | approved, investigational | unknown | antagonist | Details |
| DB00574 | Fenfluramine | approved, illicit, investigational, withdrawn | no | agonist | Details |
| DB00935 | Oxymetazoline | approved, investigational | unknown | agonist | Details |
| DB16629 | Serdexmethylphenidate | approved | unknown | agonist | Details |
| DB00320 | Dihydroergotamine | approved, investigational | unknown | agonist | Details |
| DB06016 | Cariprazine | approved, investigational | unknown | partial agonist | Details |
| DB12540 | Lecozotan | investigational | unknown | antagonist | Details |
| DB00953 | Rizatriptan | approved | unknown | agonist | Details |
| DB12184 | Gepirone | approved, investigational | yes | partial agonist | Details |