AH078

AH078 : Degrader (PROTAC) of CSNK1D, CSNK1E

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe AH078 is in the process of SERP review.

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Information

CSNK1D
CSNK1E

Degrader (PROTAC)

1 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 (cells): Selectivity within target family: AH078 is not able to degrade CK1a at low concentrations (Dmax 35%) Selectivity of AH078, performed quantitative proteomics analyses was performed using the glioma cell line U-87 and the metastatic breast adenocarcinoma cell line MDA-MB-231 quantifying 9574 and 9777 different protein groups respectively. Only CK1δ and CK1ε, but not CK1α nor any other detected proteins, were significantly reduced, demonstrating exclusive degradation selectivity of AH078 over more than 9000 other proteins that were precisely quantified in both cell lines.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This probe has been well characterised for degradation of CKIdelta and CKIepsilon, with biochemical experiments and proteomics demonstrating selectivity over other members of the family, including CKIalpha, at the recommended concentrations. Additionally, a negative control compound exists (AH081), making this probe well placed for biological studies. However, the reported Dmax value is only 70%, which is below the ideal threshold for chemical probe degraders.

(last updated: 6 Feb 2026 )