ML252

ML252 : Inhibitor of KCNQ2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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 ML252 is in the process of SERP review.

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Information

KCNQ2

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

(S)-5 was evaluated on Ricerca Bioscience’s Lead Profiling Screen, which is a radioligand binding assay profiling >68 GPCRs, ion channels, and transporters. (S)-5 was found to bind with only one of the 68 assays conducted (melantonin, MT1, 61% inhibition at 10 μM). Several ion channels are included in this profiling assay (calcium channel, L- and N-type; potassium channel (KATP and hERG)), which were not inhibited by (S)-5. KCNQ1 2.92 ± 3.90 uM KCNQ1/E1 8.12 ± 1.47 uM KCNQ2/Q3 0.12 ± 0.02 uM KCNQ4 0.20 ± 0.06 uM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The compound has not a clean selectivity profile with regards to the related target KCNQ4. It also has suboptimal in vivo properties with a medium to high clearance and can only be administered ip. A negative control compound such as cpd 56 would be a useful addition.

(last updated: 24 Jun 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The selectivity of the compound for KCNQ2 over other KCNQs remains to be optimized.

(last updated: 9 Jul 2022 )