PF-05105679

PF-05105679 : Antagonist of TRPM8

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 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 PF-05105679 is in the process of SERP review.

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Information

TRPM8

Antagonist

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: Q7Z2W7

Target Class: Ion Channel

Target SubClass: Cation Channel

Potency: IC50

Potency Value: 103 nM

Potency Assay: Inhibition of binding to TRPM8

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

Target aliases:

Transient receptor potential cation channel subfam ...

DOI Reference: 10.1021/ml500479v

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Selective over related family at 10 µM: TRPV1, TRPA1 (Ca+ mobilization assays and single-cell patch-clamp studies against both voltage-and agonist-driven activation). Clean Millipore Ion channel CardiacProfiler panel at 10 µM. Selectivity outside target family: Clean CEREP Ligand Profile screen (90 targets): No greater than 36 % inhibition at 10 µM for any off-target. One hit in the GPCR scan: GABA/PBR (Ki = 1022.12 nM)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Good probe which progressed to clinical trials. Good to also have a control molecule but would also expect data on the distomer (inactive enantiomer) as a control. Efficacy from oral dosing would also be beneficial.

(last updated: 28 Jan 2022 )