ONO-6830634

ONO-6830634 : Activator of KCNK2 and KCNK10

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe ONO-6830634 is in the process of SERP review.

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Information

KCNK2
KCNK10

Activator

up to 5 uM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Compound 20 was >91-fold selective in the K2P 86Rb flux panel against TASK-1, TASK-2, TASK-3, and TWIK-2 over TREK-1/2. The only off-target activity in the K2P family was at TRESK, where compound 20 showed micromolar inhibitor activity and was 85-fold selective against TRAAK over TREK-1.

Potency assay (off target): Panel of 72 targets including GPCRs, ion channels, transporters and nuclear hormones was performed on related compound ONO-2920632 (VU6011887, Compound 19b) at 30 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This appears to be a highly selective human dual TREK-1/2 probe, which is very selective against the K2P ion channel family and 72 GPCRs, ion channels and transporters (Eurofins Lead Profiling panel). Further the reported PK in mouse, rat and dog and unbound levels in the brain are consistent with the reported efficacy in a mouse acetic acid writhing assay at an oral dose of 3 mg/kg. It should be noted that the authors report activity against the human TREK-1 and TREK-2 receptors and activity against the mouse equivalent receptors has not been measured.

(last updated: 13 Aug 2025 )