Drug target · HTR1A
5-HT1A
5-hydroxytryptamine receptor 1A
9 compounds in the CNS pipeline act on 5-HT1A.
Compounds targeting 5-HT1A
| Compound | Action | Affinity | Lead program | Developer |
|---|---|---|---|---|
| BPL-003 (intranasal 5-MeO-DMT benzoate)primaryPsychedelic | Agonist | Ki 1.9 nM | Phase 2Treatment-resistant depression | Beckley Psytech Limited |
| BrexpiprazoleSmall molecule | Partial agonist | Ki 0.12 nM | Filed (NDA)Post-traumatic stress disorder | Otsuka Pharmaceutical Co., Ltd. |
| Brilaroxazine (RP5063)Small molecule | Partial agonist | Ki 1.5 nM | Phase 3Schizophrenia | Reviva Pharmaceuticals Holdings, Inc. |
| Lysergide D-tartrate (MM120 / LSD)Psychedelic | Agonist | pKi 9 | Phase 3Generalized anxiety disorder | Definium Therapeutics, Inc. |
| Psilocybin (COMP360)Psychedelic | Agonist | — | Phase 3Treatment-resistant depression | COMPASS Pathways plc |
| Ulotaront (SEP-363856)Small molecule | Agonist | Ki 284 nM | Phase 2/3Generalized anxiety disorder | Otsuka Pharmaceutical Co., Ltd. |
| Mebufotenin (inhaled 5-MeO-DMT, GH001)Psychedelic | Agonist | — | Phase 2Treatment-resistant depression | GH Research PLC |
| VLS-01Psychedelic | Agonist | — | Phase 2Treatment-resistant depression | Atai Beckley N.V. (AtaiBeckley) |
| ELE-101 (intravenous psilocin benzoate)Psychedelic | Agonist | — | Phase 1/2Major depressive disorder | Beckley Psytech Limited |