Homer

Homer : Degrader (PROTAC) of WDR5

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 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

WDR5

Degrader (PROTAC)

up to 1 uM
Reviewer recommended concentration: Dependent on the cell line of interest, higher concentrations might be required

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P61964

Target Class: WD40 Repeat

Target SubClass: --

Potency: Kd

Potency Value: 18 nM

Potency Assay: ITC

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

Target aliases:

WD repeat-containing protein 5, BIG3, WDR5, WDR5_H ...

DOI Reference: 10.1021/acs.jmedchem.1c00146

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Quantitative Proteomics revealed that only WDR5 is significantly and substantially depleted by Homer treatment.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

I strongly encourage the usage of the available negative control compound (nc_VHL) that are incapable of binding VHL. This compound has near-identical physicochemical properties and retains any residual inhibitory activity on WDR5.

(last updated: 14 Apr 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

Recommended to use with both provided negative controls.

(last updated: 21 Apr 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

We recommend using this compound with its two negative controls, however, if a complete knockout is required, it will only result in a Dmax of 58%. In VHL-overexpressing cells, it was shown that the Dmax increases up to around 80%.

(last updated: 20 Feb 2025 )