- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: example 129 [WO2011069063A2]  | SEP-363856 (parent molecule) | SEP-856 | SEP363856
Compound class: Synthetic organic
Comment: Ulotaront (SEP-363856) is an orally active and brain-penetrant psychotropic agent with a novel mechanism of action. It acts as a trace amine-associated receptor 1 (TAAR1) agonist with additional 5-HT1A receptor agonist activity, and agonism at both of these receptors appears to be required for its clinical effects [2-3]. SEP-363856 is being developed by Sunovion Pharmaceuticals and PsychoGenics, and was granted FDA Breakthrough Therapy Designation as an anti-schizophrenia therapeutic in May 2019. The lack of D2 receptor activity distinguishes SEP-363856 from current antipsychotic medications.
In the Dedic et al. article from 2019 SEP-363856 refers to the hydrochloride salt. We show the parent molecule here. This S enantiomer is more active at TAAR1 compared to the R stereoenantiomer .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Correll CU, Koblan KS, Hopkins SC, Li Y, Heather Dworak, Goldman R, Loebel A. (2021)
Safety and effectiveness of ulotaront (SEP-363856) in schizophrenia: results of a 6-month, open-label extension study.
NPJ Schizophr, 7 (1): 63. [PMID:34887427]
2. Dedic N, Jones PG, Hopkins SC, Lew R, Shao L, Campbell JE, Spear KL, Large TH, Campbell UC, Hanania T et al.. (2019)
SEP-363856, a Novel Psychotropic Agent with a Unique, Non-D2 Receptor Mechanism of Action.
J Pharmacol Exp Ther, 371 (1): 1-14. [PMID:31371483]
3. Heffernan MLR, Herman LW, Brown S, Jones PG, Shao L, Hewitt MC, Campbell JE, Dedic N, Hopkins SC, Koblan KS et al.. (2022)
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.
ACS Med Chem Lett, 13 (1): 92-98. [PMID:35047111]
4. Krogmann A, Peters L, von Hardenberg L, Bödeker K, Nöhles VB, Correll CU. (2019)
Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities.
CNS Spectr, 24 (S1): 38-69. [PMID:31482779]
5. Kwan C, Huot P. (2022)
An overview of the active clinical trials for Parkinson's disease psychosis.
Neurodegener Dis Manag, 12 (4): 165-170. [PMID:35592949]
6. Shao L, Campbell JE, Hewitt MC, Campbell U, Hanania TG. (2011)
Multicyclic compounds and methods of use thereof.
Patent number: WO2011069063A2. Assignee: Pgi Drug Discovery LLC, Sunovion Pharmaceuticals Inc. Priority date: 04/12/2009. Publication date: 09/06/2011.