PF-4800567

ATP-competitive inhibitor of CSNK1E

Structure

SERP Rating

In Cells

(3 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.

Information

CSNK1E

ATP-competitive inhibitor

Probe Availability:

In Vitro Validations

Uniprot ID: P49674

Target Class: Protein kinase

Target SubClass: CK1

Potency: IC50

Potency Value: 32 nM

Potency Assay: In vitro kinase assay

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

Target aliases:

Casein kinase I isoform epsilon, CSNK1E, KC1E_HUMA ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 CSNK1D 711 nM

Potency assay (off target): In vitro kinase assay; 50 additional kinases were tested at 1 and 1 uM. PF-4800567 inhibited 69% of EGFR activity at 1 uM and 83% at 10 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The probe has cellular activity at 2.7 uM, but a target potency of triple-digit nM. Selectivity is ~ 20X at the biochemical level and ~ 10X at the cellular level for CK1d/e. No cellular target-engagement data is provided; therefore, it must be assumed to be insufficiently cell-active and insufficiently selective to act as a probe.

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This probe is weakly active in cells (2.7 uM), and mice dosed subcutaneously show only minor effects due to treatment. This probe needs improvement before using in cellular or in vivo models.

(last updated: 31 May 2016 )

SERP Ratings

In Cell Rating

SERP Comments:

This compound also significantly inhibits EGFR.

(last updated: 15 Jan 2017 )