| DB00187 | Esmolol | approved, withdrawn | yes | antagonist | Details |
| DB00195 | Betaxolol | approved, investigational | yes | antagonist | Details |
| DB00221 | Isoetharine | approved | yes | agonist | Details |
| DB00264 | Metoprolol | approved, investigational | yes | antagonist | Details |
| DB00335 | Atenolol | approved | yes | antagonist | Details |
| DB00373 | Timolol | approved | yes | antagonist | Details |
| DB00571 | Propranolol | approved, investigational | yes | antagonist | Details |
| DB00612 | Bisoprolol | approved | yes | antagonist | Details |
| DB00841 | Dobutamine | approved | yes | agonist | Details |
| DB00866 | Alprenolol | experimental, withdrawn | yes | antagonist | Details |
| DB00960 | Pindolol | approved, investigational | yes | partial agonist | Details |
| DB01064 | Isoprenaline | approved, investigational | yes | agonist | Details |
| DB01102 | Arbutamine | approved | yes | agonist | Details |
| DB01193 | Acebutolol | approved, investigational | yes | partial agonist | Details |
| DB01203 | Nadolol | approved | yes | antagonist | Details |
| DB01210 | Levobunolol | approved | yes | antagonist | Details |
| DB01214 | Metipranolol | approved | yes | antagonist | Details |
| DB00521 | Carteolol | approved | yes | antagonistpartial agonist | Details |
| DB00598 | Labetalol | approved | yes | antagonist | Details |
| DB00668 | Epinephrine | approved, vet_approved | yes | agonist | Details |
| DB01136 | Carvedilol | approved, investigational | yes | antagonist | Details |
| DB01151 | Desipramine | approved, investigational | unknown | other | Details |
| DB01295 | Bevantolol | experimental | yes | antagonist | Details |
| DB01297 | Practolol | approved | yes | antagonist | Details |
| DB01580 | Oxprenolol | approved | yes | antagonist | Details |
| DB01359 | Penbutolol | approved, investigational | yes | antagonistpartial agonist | Details |
| DB00368 | Norepinephrine | approved | yes | agonist | Details |
| DB04855 | Dronedarone | approved | unknown | antagonist | Details |
| DB04861 | Nebivolol | approved, investigational | yes | antagonist | Details |
| DB06262 | Droxidopa | approved, investigational | yes | agonist | Details |
| DB01001 | Salbutamol | approved, vet_approved | unknown | agonist | Details |
| DB00489 | Sotalol | approved | yes | antagonist | Details |
| DB01291 | Pirbuterol | approved | unknown | agonist | Details |
| DB01288 | Fenoterol | approved, investigational | unknown | agonist | Details |
| DB00397 | Phenylpropanolamine | approved, vet_approved, withdrawn | unknown | agonist | Details |
| DB01407 | Clenbuterol | approved, investigational, vet_approved | unknown | agonist | Details |
| DB08347 | 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile | experimental | unknown | | Details |
| DB08558 | 2-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOL | experimental | unknown | | Details |
| DB08807 | Bopindolol | experimental | yes | antagonistpartial agonist | Details |
| DB08808 | Bupranolol | experimental | yes | antagonist | Details |
| DB00852 | Pseudoephedrine | approved | unknown | agonistpartial agonist | Details |
| DB04846 | Celiprolol | approved, investigational | yes | antagonist | Details |
| DB01363 | Ephedra sinica root | nutraceutical | yes | agonist | Details |
| DB06216 | Asenapine | approved | unknown | antagonist | Details |
| DB00408 | Loxapine | approved | unknown | binder | Details |
| DB00248 | Cabergoline | approved | unknown | binder | Details |
| DB09068 | Vortioxetine | approved, investigational | unknown | ligand | Details |
| DB09013 | Befunolol | experimental | unknown | | Details |
| DB00983 | Formoterol | approved, investigational | unknown | agonist | Details |
| DB00938 | Salmeterol | approved | unknown | inverse agonist | Details |
| DB00871 | Terbutaline | approved | unknown | antagonist | Details |
| DB01917 | Putrescine | experimental | unknown | | Details |
| DB03566 | Spermidine | experimental | unknown | | Details |
| DB00127 | Spermine | experimental, nutraceutical | unknown | | Details |
| DB01182 | Propafenone | approved | unknown | antagonist | Details |
| DB09351 | Levobetaxolol | approved, investigational | yes | antagonist | Details |
| DB13781 | Xamoterol | approved | yes | partial agonist | Details |
| DB09204 | Arotinolol | investigational | yes | antagonist | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB11124 | Racepinephrine | approved | yes | agonist | Details |
| DB11278 | DL-Methylephedrine | approved | yes | agonist | Details |
| DB00243 | Ranolazine | approved, investigational | no | antagonist | Details |
| DB01238 | Aripiprazole | approved, investigational | unknown | ligand | Details |
| DB01364 | Ephedrine | approved | yes | agonist | Details |
| DB08893 | Mirabegron | approved | unknown | agonist | Details |