MEZIGDOMIDE

MEZIGDOMIDE : Degrader of CRBN

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MEZIGDOMIDE is in the process of SERP review.

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Information

CRBN

Degrader, CELMoD

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q96SW2

Target Class: post-translational modification

Target SubClass: E3 Ligase

Potency: IC50

Potency Value: 37.2 nM

Potency Assay: FRET Binding affinity assay

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

Target aliases:

Protein cereblon, CRBN, CRBN_HUMAN

DOI Reference: 10.1021/acs.jmedchem.9b01928

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 24 Oct 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The (R) and (S) enantiomers racemize on the timescale of course in cell culture, therefore, for in vitro experiments, the N-methylated compound, or another related inactive analogue may be a better negative control to use. While phenotypic selectivity is shown (low toxicity in PMBCs), target selectivity by proteomics or western is not shown in the paper. Therefore the concentration at which there may be off-target effects (if any) is not known.

(last updated: 15 Nov 2022 )