Chemical Probes logo
TASIMELTEON | TASIMELTEON : Agonist of MTNR1A and MTNR1B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MTNR1A
    • Ki:0.35 nM
    • Ki: 0.304 nM
    • EC50:0.74 nM
    MTNR1B
      • Ki:0.17 nM
      • Ki:0.0692 ± 0.007 nM
      • EC50:0.1 nM
      Agonist
      up to 100 nM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      No significant responses (≥50% inhibition or stimulation) were observed in any radioligand receptor ...

      Potency
      Cellular
      In Vitro

      MTNR1A

      Mode of Action: Agonist

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.neuropharm.2014.12.004

      MTNR1B

      Mode of Action: Agonist

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.neuropharm.2014.12.004

      Chemical Information

      Molecular Formula C15H19NO2
      SMILEs CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2
      InChI InChI=1S/C15H19NO2/c1-2-15(17)16-9-10-8-13(10)11-4-3-5-14-12(11)6-7-18-14/h3-5,10,13H,2,6-9H2,1H3,(H,16,17)/t10-,13+/m0/s1
      Molecular weight 245.14 Da
      AlogP 2.2512
      HBond acceptors 3
      HBond donors 1
      Atoms 37

      References

      Publications

      Cross References

      Expert Reviews

      by SERP
      (on 7 Apr 2025 )
      Cellular Use Rating
      This is an approved drug, which is active on both MT1 and MT2. It is a very potent and selective compound.
      by SERP
      (on 1 May 2025 )
      Cellular Use Rating
      ( The reviewer did not leave any comments )
      by SERP+
      (on 14 Oct 2025 )
      Cellular Use Rating
      ...

      Portal Comments

      A study by Vachharajani et al. (2003; J. Pharm. Sci.) reports the use of BMS-214778 (Tasimelteon) in rats and monkeys.

      (last updated: 21 Oct 2025)

      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria