Drug target · SLC6A4

SERT

Serotonin transporter

10 compounds in the CNS pipeline act on SERT.

Compounds targeting SERT

CompoundActionAffinityLead programDeveloper
Methylone (TSND-201)primaryPsychedelicReleaserPhase 3Post-traumatic stress disorderTranscend Therapeutics, Inc.
DT402primaryPsychedelicReleaserEC50 340 nMPhase 2Autism spectrum disorderDefinium Therapeutics, Inc.
EMP-01 (oral R-MDMA)primaryPsychedelicReleaserPhase 2Social anxiety disorderEmpathBio, Inc.
OPC-64005primarySmall moleculeReuptake inhibitorDiscontinuedMajor depressive disorderOtsuka Pharmaceutical Co., Ltd.
Lumateperone (ITI-007)Small moleculeInhibitorKi 63 nMApprovedSchizophreniaIntra-Cellular Therapies, Inc.
AXS-12 (reboxetine)Small moleculeReuptake inhibitorFiled (NDA)NarcolepsyAxsome Therapeutics, Inc.
CentanafadineSmall moleculeReuptake inhibitorIC50 83 nMFiled (NDA)Attention-deficit/hyperactivity disorderOtsuka Pharmaceutical Co., Ltd.
AXS-14 (esreboxetine)Small moleculeReuptake inhibitorPhase 3FibromyalgiaAxsome Therapeutics, Inc.
Bretisilocin (GM-2505)PsychedelicReleaserEC50 8.4 nMPhase 2Major depressive disorderGilgamesh Pharmaceuticals, Inc.
ITI-1284 (deulumateperone)Small moleculeInhibitorPhase 2Alzheimer's diseaseIntra-Cellular Therapies, Inc.