TAK-861

TAK-861 : Agonist of HCRTR2

Structure

SERP Rating

In Cells

(0 ratings)

In Model Organisms

(1 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.

Probe TAK-861 is in the process of SERP review.

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Information

HCRTR2

Agonist

up to1 uM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: 3000-fold selective over OX1R Selectivity outside target family: Evaluation of the activity of TAK-861 on various enzymes, receptors, and ion channels (102 targets in total) in in vitro assays revealed that TAK-861 at 10 μM did not induce more than 50% inhibition or stimulation of these targets, except cannabinoid CB1 (58% inhibition) and progesterone receptor B (62% inhibition)

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SERP ratings and comments

SERP Ratings

In Model Organisms

SERP Comments:

This probe targets an extracellular protein and therefore does not require an intracellular evaluation. TAK-861 has also been tested on male cynomolgus monkey (1 mg/kg, p.o.)

(last updated: 5 Feb 2025 )