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ONO-6830634

ONO-6830634 : Activator of KCNK2 and KCNK10

Structure

Information

  • KCNK2
  • KCNK10
  • Activator
  • up to 5 uM
  • Reviewer recommended concentration: 1-10 µM

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): 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). However its use as an in vivo (periphery) TREK tool compound should be caveated that no in vitro metabolism data or PK data is reported for it. Those intending to use it for a probe will need to do in vitro and in vivo PK characterisation to have any confidence in the probe.

(last updated: 13 Aug 2025 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

ONO-6830634 is a useful probe to study the role TREK-1 and TREK-2 in cells. The compound is potent and selective. It may also be applicable in vivo. However, prior to its use in animal studies, in vitro and in vivo characterisation data need to be generated or published.

(last updated: 20 Aug 2025 )