TASIMELTEON

TASIMELTEON : Agonist of MTNR1A and MTNR1B

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

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.

Information

MTNR1A
MTNR1B

Agonist

up to 100 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): No significant responses (≥50% inhibition or stimulation) were observed in any radioligand receptor binding assay and enzyme assays, except for both melatonin receptors MT1 and MT2.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This is an approved drug, which is active on both MT1 and MT2. It is a very potent and selective compound.

(last updated: 7 Apr 2025 )

SERP Ratings

In Cell Rating

(last updated: 1 May 2025 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Good functional potency for MT1 and MT2. Higher potency for MT2 but would not recommend as selective over MT1. Selectivity over GPCR analogues is tested but not quantified other than 'below 50%' effect.

(last updated: 14 Oct 2025 )

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)