| DB00272 | Betazole | approved | yes | agonist | Details |
| DB00501 | Cimetidine | approved, investigational | yes | antagonist | Details |
| DB00585 | Nizatidine | approved | yes | antagonist | Details |
| DB00863 | Ranitidine | approved, withdrawn | yes | antagonist | Details |
| DB00927 | Famotidine | approved | yes | antagonist | Details |
| DB05381 | Histamine | approved, investigational | yes | agonist | Details |
| DB01142 | Doxepin | approved, investigational | yes | antagonist | Details |
| DB00751 | Epinastine | approved, investigational | yes | antagonist | Details |
| DB05369 | HZT-501 | investigational | unknown | | Details |
| DB06216 | Asenapine | approved | unknown | antagonist | Details |
| DB00940 | Methantheline | approved, investigational | yes | antagonist | Details |
| DB08805 | Metiamide | experimental | yes | antagonist | Details |
| DB08806 | Roxatidine acetate | experimental | yes | antagonist | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00321 | Amitriptyline | approved | unknown | blocker | Details |
| DB00797 | Tolazoline | approved, vet_approved | unknown | agonist | Details |
| DB01069 | Promethazine | approved, investigational | unknown | antagonist | Details |
| DB00768 | Olopatadine | approved | unknown | antagonist | Details |
| DB00972 | Azelastine | approved | unknown | inhibitor | Details |
| DB01238 | Aripiprazole | approved, investigational | unknown | ligand | Details |
| DB00434 | Cyproheptadine | approved | unknown | antagonist | Details |
| DB13760 | Niperotidine | experimental, investigational | unknown | antagonist | Details |
| DB09185 | Viloxazine | approved, investigational, withdrawn | unknown | antagonist | Details |