HS665

HS665 : Agonist of OPRK1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe HS665 is in the process of SERP review.

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Information

OPRK1

Agonist

up to 1 uM

In Vitro Validations

Uniprot ID: P41145

Target Class: GPCR

Target SubClass: Opioid receptor

Potency: Ki

Potency Value: 0.49 ± 0.20 nM

Potency Assay: Scintillation proximity assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Kappa-type opioid receptor, OPRK, OPRK1, OPRK_HUMA ...

DOI Reference: 10.1021/jm301258w

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): HS665 shows >1100-fold selectivity for KOP vs MOP receptors, and >20000-fold selectivity for KOP vs DOP receptors. Selective against Human Dopamine Receptors: D1 Ki >10000 nM, D2 Ki 450 ± 28 nM, D3 Ki 282 ± 34 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Data describing the selectivity profile of HS665 at MOP and DOP receptors has been provided, but an assessment of the selectivity against a broad panel of targets has not been shared. This would be particularly relevant for the interpretation of in vivo data (see below). A lipophilic base (Chemdraw logP 5) has a risk of off-target activity which may be enhanced through the combination with a low topological polar surface area (Chemdraw TPSA 23). An efficacious response has been demonstrated in a mouse model using the recommended dose, however free drug levels in the brain has not been shared to understand how these compare to the functional in vitro activity.

(last updated: 22 Nov 2023 )