| DB00247 | Methysergide | approved | yes | antagonist | Details |
| DB00370 | Mirtazapine | approved | yes | antagonist | Details |
| DB00434 | Cyproheptadine | approved | yes | antagonist | Details |
| DB00656 | Trazodone | approved, investigational | yes | antagonist | Details |
| DB00924 | Cyclobenzaprine | approved | yes | antagonist | Details |
| DB01149 | Nefazodone | approved, withdrawn | yes | antagonist | Details |
| DB01224 | Quetiapine | approved | yes | antagonist | Details |
| DB00246 | Ziprasidone | approved | yes | antagonist | Details |
| DB00334 | Olanzapine | approved, investigational | yes | antagonist | Details |
| DB00363 | Clozapine | approved | yes | antagonist | Details |
| DB00420 | Promazine | approved, vet_approved | unknown | antagonist | Details |
| DB00477 | Chlorpromazine | approved, investigational, vet_approved | yes | antagonist | Details |
| DB00679 | Thioridazine | approved, withdrawn | yes | antagonist | Details |
| DB00777 | Propiomazine | approved | unknown | antagonist | Details |
| DB00805 | Minaprine | approved | yes | antagonist | Details |
| DB00933 | Mesoridazine | approved, investigational | yes | antagonist | Details |
| DB01238 | Aripiprazole | approved, investigational | yes | antagonist | Details |
| DB01267 | Paliperidone | approved | yes | antagonist | Details |
| DB00696 | Ergotamine | approved | yes | agonist | Details |
| DB00715 | Paroxetine | approved, investigational | unknown | agonist | Details |
| DB00843 | Donepezil | approved | unknown | inducer | Details |
| DB01242 | Clomipramine | approved, investigational, vet_approved | yes | antagonist | Details |
| DB01442 | MMDA | experimental, illicit | yes | agonist | Details |
| DB01239 | Chlorprothixene | approved, experimental, investigational, withdrawn | yes | antagonist | Details |
| DB00751 | Epinastine | approved, investigational | unknown | antagonist | Details |
| DB05227 | APD791 | investigational | unknown | | Details |
| DB06144 | Sertindole | approved, investigational, withdrawn | yes | antagonist | Details |
| DB04908 | Flibanserin | approved, investigational | yes | antagonist | Details |
| DB12555 | Nelotanserin | investigational | unknown | | Details |
| DB06148 | Mianserin | approved, investigational | unknown | antagonist | Details |
| DB05079 | HY10275 | investigational | unknown | | Details |
| DB05316 | Pimavanserin | approved, investigational | yes | inverse agonist | Details |
| DB04946 | Iloperidone | approved | yes | antagonist | Details |
| DB05687 | BL-1020 | investigational | unknown | | Details |
| DB05492 | Epicept NP-1 | investigational | unknown | | Details |
| DB00604 | Cisapride | approved, investigational, withdrawn | yes | agonist | Details |
| DB06077 | Lumateperone | approved, investigational | yes | antagonist | Details |
| DB06109 | YKP-1358 | investigational | unknown | | Details |
| DB06216 | Asenapine | approved | yes | antagonist | Details |
| DB06229 | Ocaperidone | investigational | unknown | | Details |
| DB12177 | Eplivanserin | investigational | unknown | | Details |
| DB06512 | Deramciclane | investigational | unknown | antagonist | Details |
| DB04599 | Aniracetam | experimental | unknown | | Details |
| DB06446 | Dotarizine | investigational | unknown | | Details |
| DB01186 | Pergolide | approved, investigational, vet_approved, withdrawn | unknown | agonist | Details |
| DB01200 | Bromocriptine | approved, investigational, withdrawn | unknown | agonist | Details |
| DB00589 | Lisuride | approved, investigational | yes | agonist | Details |
| DB00248 | Cabergoline | approved | unknown | agonist | Details |
| DB00714 | Apomorphine | approved, investigational | unknown | agonist | Details |
| DB00875 | Flupentixol | approved, investigational, withdrawn | yes | antagonist | Details |
| DB00502 | Haloperidol | approved | unknown | other/unknown | Details |
| DB01403 | Methotrimeprazine | approved, investigational | unknown | antagonist | Details |
| DB01618 | Molindone | approved | unknown | antagonist | Details |
| DB01488 | Dimethyltryptamine | experimental, illicit | unknown | | Details |
| DB01624 | Zuclopenthixol | approved, investigational | unknown | antagonist | Details |
| DB00408 | Loxapine | approved | yes | antagonist | Details |
| DB00321 | Amitriptyline | approved | yes | antagonist | Details |
| DB01142 | Doxepin | approved, investigational | unknown | antagonist | Details |
| DB01151 | Desipramine | approved, investigational | yes | antagonist | Details |
| DB00458 | Imipramine | approved | unknown | antagonist | Details |
| DB00540 | Nortriptyline | approved | yes | antagonist | Details |
| DB00409 | Remoxipride | approved, withdrawn | unknown | other/unknown | Details |
| DB00726 | Trimipramine | approved | unknown | agonist | Details |
| DB01392 | Yohimbine | approved, investigational, vet_approved | unknown | antagonist | Details |
| DB01079 | Tegaserod | approved, investigational, withdrawn | unknown | antagonist | Details |
| DB04842 | Fluspirilene | approved, investigational | unknown | antagonist | Details |
| DB06288 | Amisulpride | approved, investigational | yes | antagonist | Details |
| DB01614 | Acepromazine | experimental, vet_approved | yes | antagonist | Details |
| DB01621 | Pipotiazine | approved, investigational | yes | antagonist | Details |
| DB01623 | Thiothixene | approved | unknown | antagonist | Details |
| DB01454 | Midomafetamine | experimental, illicit, investigational | unknown | agonist | Details |
| DB08810 | Cinitapride | investigational | yes | antagonist | Details |
| DB08815 | Lurasidone | approved, investigational | yes | antagonist | Details |
| DB08927 | Amperozide | experimental | unknown | antagonist | Details |
| DB00543 | Amoxapine | approved | unknown | antagonist | Details |
| DB00934 | Maprotiline | approved, investigational | unknown | binder | Details |
| DB09016 | Butriptyline | approved, withdrawn | yes | antagonist | Details |
| DB09128 | Brexpiprazole | approved, investigational | unknown | antagonist | Details |
| DB08922 | Perospirone | experimental | yes | inverse agonist | Details |
| DB09167 | Dosulepin | approved | yes | antagonist | Details |
| DB00574 | Fenfluramine | approved, illicit, investigational, withdrawn | unknown | agonist | Details |
| DB08839 | Serotonin | investigational, nutraceutical | unknown | | Details |
| DB12465 | Ketanserin | investigational | unknown | inverse agonist | Details |
| DB12693 | Ritanserin | investigational | unknown | inverse agonist | Details |
| DB12163 | Sarpogrelate | investigational | unknown | inverse agonist | Details |
| DB00623 | Fluphenazine | approved | unknown | | Details |
| DB01537 | 4-Bromo-2,5-dimethoxyphenethylamine | experimental, illicit | unknown | partial agonist | Details |
| DB09194 | Etoperidone | withdrawn | yes | antagonist | Details |
| DB09223 | Blonanserin | investigational | yes | antagonist | Details |
| DB13940 | 2,5-Dimethoxy-4-ethylthioamphetamine | experimental | unknown | agonist | Details |
| DB09061 | Cannabidiol | approved, investigational | unknown | agonist | Details |
| DB13948 | N-(2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine | experimental | unknown | agonist | Details |
| DB09195 | Lorpiprazole | approved | yes | antagonist | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB09225 | Zotepine | approved, investigational, withdrawn | yes | antagonist | Details |
| DB09286 | Pipamperone | investigational | unknown | agonist | Details |
| DB06153 | Pizotifen | approved | unknown | antagonist | Details |
| DB14010 | 5-methoxy-N,N-dimethyltryptamine | experimental, illicit | unknown | agonist | Details |
| DB14011 | Nabiximols | investigational | unknown | | Details |
| DB14009 | Medical Cannabis | experimental, investigational | unknown | | Details |
| DB14185 | Aripiprazole lauroxil | approved, investigational | yes | antagonist | Details |
| DB01175 | Escitalopram | approved | unknown | inhibitor | Details |
| DB00734 | Risperidone | approved, investigational | yes | antagonist | Details |
| DB00315 | Zolmitriptan | approved, investigational | no | agonist | Details |
| DB16351 | Volinanserin | investigational | unknown | antagonist | Details |
| DB00320 | Dihydroergotamine | approved, investigational | unknown | agonist | Details |
| DB06016 | Cariprazine | approved, investigational | unknown | antagonist | Details |