ML277

ML277 : Activator of KCNQ1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ML277 is in the process of SERP review.

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Information

KCNQ1

Activator

up to 1 uM

Probe Availability:

MCULE

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Within target family: Highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel. Outside target family: Ricerca’s Lead Profiling Screen (binding assay panel of 68 GPCRs, ion channels and transporters) - % inhibition at 10 μM, species: Adenosine, A3 (73%, human); Calcium Channel L-type (52%, rat); Cannabinoid, CB1 (97%, human); Potassium channel, hERG (80%, human); Serotonin (5-hydroxytryptamine), 5-HT2B (66%, human); Transporter, dopamine (DAT) (54%, human)

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Data included in the paper demonstrate high turnover in human and rat microsomes which preclude consideration as in vivo tool. Selectivity data are provided for close family members and a panel of 68 GPCRs, ion channels and transporters. No selectivity vs. other protein classes provided. KCNQ characterisation was conducted using automated electrophysiology platform rather than more detailed biophysical analysis.

(last updated: 28 Nov 2022 )