Drug target · SLC6A4
SERT
Sodium-dependent serotonin transporter
11 compounds in the CNS pipeline act on SERT.
Compounds targeting SERT
| Compound | Action | Affinity | Lead program | Developer |
|---|---|---|---|---|
| Methylone (TSND-201)primaryPsychedelic | Releaser | — | Phase 3Post-traumatic stress disorder | Transcend Therapeutics, Inc. |
| DT402primaryPsychedelic | Releaser | EC50 340 nM | Phase 2Autism spectrum disorder | Definium Therapeutics, Inc. |
| EMP-01 (oral R-MDMA)primaryPsychedelic | Releaser | — | Phase 2Social anxiety disorder | EmpathBio, Inc. |
| OPC-64005primarySmall molecule | Reuptake inhibitor | — | DiscontinuedMajor depressive disorder | Otsuka Pharmaceutical Co., Ltd. |
| CentanafadineSmall molecule | Reuptake inhibitor | IC50 83 nM | ApprovedAttention-deficit/hyperactivity disorder | Otsuka Pharmaceutical Co., Ltd. |
| Lumateperone (ITI-007)Small molecule | Inhibitor | Ki 63 nM | ApprovedSchizophrenia | Intra-Cellular Therapies, Inc. |
| AXS-12 (reboxetine)Small molecule | Reuptake inhibitor | — | Filed (NDA)Narcolepsy | Axsome Therapeutics, Inc. |
| AXS-14 (esreboxetine)Small molecule | Reuptake inhibitor | — | Phase 3Fibromyalgia | Axsome Therapeutics, Inc. |
| Bretisilocin (GM-2505)Psychedelic | Releaser | EC50 8.4 nM | Phase 2Major depressive disorder | Gilgamesh Pharmaceuticals, Inc. |
| ITI-1284 (deulumateperone)Small molecule | Inhibitor | — | Phase 2Agitation in Alzheimer's disease | Intra-Cellular Therapies, Inc. |
| AmpreloxetineSmall molecule | Reuptake inhibitor | pKi 8.5 | DiscontinuedMultiple System Atrophy | Theravance Biopharma, Inc. |