| DB01273 | Varenicline | approved, investigational | yes | partial agonist | Details |
| DB00184 | Nicotine | approved | yes | agonist | Details |
| DB05458 | Pozanicline | investigational | unknown | | Details |
| DB05740 | RPI-78M | investigational | unknown | | Details |
| DB01351 | Amobarbital | approved, illicit | unknown | antagonist | Details |
| DB00312 | Pentobarbital | approved, investigational, vet_approved | unknown | antagonist | Details |
| DB00241 | Butalbital | approved, illicit | unknown | antagonist | Details |
| DB00306 | Talbutal | approved, illicit | unknown | antagonist | Details |
| DB00418 | Secobarbital | approved, vet_approved | unknown | antagonist | Details |
| DB00463 | Metharbital | withdrawn | unknown | antagonist | Details |
| DB00599 | Thiopental | approved, vet_approved | unknown | antagonist | Details |
| DB00794 | Primidone | approved, vet_approved | unknown | antagonist | Details |
| DB00849 | Methylphenobarbital | approved | unknown | antagonist | Details |
| DB01174 | Phenobarbital | approved, investigational | unknown | antagonist | Details |
| DB01352 | Aprobarbital | experimental, illicit | unknown | antagonist | Details |
| DB01353 | Butobarbital | approved, illicit | unknown | antagonist | Details |
| DB01354 | Heptabarbital | experimental | unknown | antagonist | Details |
| DB01355 | Hexobarbital | experimental | unknown | antagonist | Details |
| DB01483 | Barbital | illicit | unknown | antagonist | Details |
| DB01496 | Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione | experimental, illicit | unknown | antagonist | Details |
| DB00514 | Dextromethorphan | approved | unknown | antagonist | Details |
| DB09028 | Cytisine | experimental | unknown | agonist | Details |
| DB00898 | Ethanol | approved | unknown | | Details |
| DB00783 | Estradiol | approved, investigational, vet_approved | unknown | binder | Details |
| DB00564 | Carbamazepine | approved, investigational | unknown | | Details |
| DB01245 | Decamethonium | approved | unknown | | Details |
| DB00657 | Mecamylamine | approved, investigational | unknown | | Details |
| DB00981 | Physostigmine | approved, investigational | unknown | | Details |
| DB00572 | Atropine | approved, vet_approved | unknown | | Details |
| DB00747 | Scopolamine | approved, investigational | unknown | inhibitorinducer | Details |
| DB07720 | Epibatidine | experimental | unknown | agonist | Details |
| DB13952 | Estradiol acetate | approved, investigational, vet_approved | unknown | | Details |
| DB13953 | Estradiol benzoate | approved, investigational, vet_approved | unknown | | Details |
| DB13954 | Estradiol cypionate | approved, investigational, vet_approved | unknown | | Details |
| DB13955 | Estradiol dienanthate | approved, investigational, vet_approved | unknown | | Details |
| DB13956 | Estradiol valerate | approved, investigational, vet_approved | unknown | | Details |
| DB00915 | Amantadine | approved | unknown | antagonist | Details |
| DB00753 | Isoflurane | approved, vet_approved | unknown | antagonist | Details |
| DB00333 | Methadone | approved | unknown | antagonist | Details |