| DB06579 | Adipiplon | investigational | yes | partial agonist | Details |
| DB13983 | 5,7,2′-trihydroxy-6,8-dimethoxyflavone | experimental | unknown | ligand | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB00334 | Olanzapine | approved, investigational | no | inhibitor | Details |
| DB15489 | Mexazolam | experimental | yes | ligand | Details |
| DB00842 | Oxazepam | approved | yes | ligand | Details |
| DB00404 | Alprazolam | approved, illicit, investigational | yes | ligand | Details |
| DB00186 | Lorazepam | approved | yes | ligand | Details |
| DB00231 | Temazepam | approved, investigational | unknown | ligand | Details |
| DB00475 | Chlordiazepoxide | approved, illicit, investigational | yes | ligand | Details |
| DB00628 | Clorazepic acid | approved, illicit | yes | ligand | Details |
| DB00683 | Midazolam | approved, illicit | yes | ligand | Details |
| DB00690 | Flurazepam | approved, illicit, investigational | yes | ligand | Details |
| DB00829 | Diazepam | approved, illicit, investigational, vet_approved | yes | ligand | Details |
| DB00897 | Triazolam | approved, investigational | yes | ligand | Details |
| DB01068 | Clonazepam | approved, illicit | yes | ligand | Details |
| DB01215 | Estazolam | approved, illicit | yes | ligand | Details |
| DB01558 | Bromazepam | approved, illicit, investigational | yes | ligand | Details |
| DB01595 | Nitrazepam | approved | yes | ligand | Details |
| DB00349 | Clobazam | approved, illicit | yes | ligand | Details |
| DB01489 | Camazepam | experimental, illicit | yes | ligand | Details |
| DB01511 | Delorazepam | experimental, illicit | yes | ligand | Details |
| DB01544 | Flunitrazepam | approved, illicit | yes | ligand | Details |
| DB01588 | Prazepam | approved, illicit | yes | ligand | Details |
| DB09166 | Etizolam | experimental | yes | ligand | Details |
| DB13437 | Medazepam | experimental | yes | ligand | Details |
| DB13837 | Doxefazepam | experimental | yes | ligand | Details |
| DB13872 | Lormetazepam | approved | yes | ligand | Details |
| DB14028 | Nordazepam | experimental | yes | ligand | Details |
| DB00546 | Adinazolam | experimental | yes | ligand | Details |
| DB00801 | Halazepam | approved, illicit, withdrawn | unknown | ligand | Details |
| DB01545 | Ethyl loflazepate | experimental, illicit | yes | ligand | Details |
| DB01553 | Cloxazolam | experimental | yes | ligand | Details |
| DB01559 | Clotiazepam | approved, illicit | yes | ligand | Details |
| DB01587 | Ketazolam | approved | yes | ligand | Details |
| DB01594 | Cinolazepam | experimental | yes | ligand | Details |
| DB09017 | Brotizolam | investigational, withdrawn | yes | ligand | Details |
| DB13335 | Pinazepam | experimental | yes | ligand | Details |
| DB13643 | Loprazolam | experimental | unknown | ligand | Details |
| DB01589 | Quazepam | approved, illicit | yes | ligand | Details |
| DB14672 | Oxazepam acetate | experimental | yes | ligand | Details |
| DB12537 | 1,2-Benzodiazepine | approved, investigational | unknown | ligand | Details |
| DB14715 | Cinazepam | experimental | yes | ligand | Details |
| DB14719 | Bentazepam | experimental | yes | ligand | Details |
| DB12404 | Remimazolam | approved, investigational | yes | ligand | Details |
| DB00909 | Zonisamide | approved, investigational | unknown | binder | Details |