BIO-2007817

BIO-2007817 : Molecular glue activator for PRKN and phospho-ubiquitin

Structure

SERP Rating

In Cells

(2 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.

Probe BIO-2007817 is in the process of SERP review.

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Information

PRKN

Molecular Glues

up to 10 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O60260

Target Class: Ubiquitin-protein ligase

Target SubClass: Parkinson disease protein

Potency: Kd

Potency Value: 10 nM

Potency Assay: Isothermal Titration Calorimetry (ITC)

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

Target aliases:

E3 ubiquitin-protein ligase parkin, PARK2, PRKN, P ...

DOI Reference: 10.1038/s41467-024-51889-3

Uniprot ID: O60260

Target Class: Ubiquitin-protein ligase

Target SubClass: Parkinson disease protein

Potency: EC50

Potency Value: 150 nM

Potency Assay: Parkin autoubiquitination assays

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

Target aliases:

E3 ubiquitin-protein ligase parkin, PARK2, PRKN, P ...

DOI Reference: 10.1038/s41467-024-51889-3

Uniprot ID: O60260

Target Class: Ubiquitin-protein ligase

Target SubClass: Parkinson disease protein

Potency Assay: 2D NMR with 15N-labeled R0RB:2×pUb showing that BIO-2007817 binds at the same location as BIO-1975900 for which a crystal stricture has been obtained.

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

Target aliases:

E3 ubiquitin-protein ligase parkin, PARK2, PRKN, P ...

DOI Reference: 10.1038/s41467-024-51889-3

In Cell Validations

In Vivo Data

No in Vivo Validations

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 31 Oct 2024 )

SERP Ratings

In Cell Rating

SERP Comments:

BIO-2007817 is one of the best compounds for assessing parkin activity in cells, as it has a unique activation mechanism by gluing parkin and pUb. However, its activity might not be sufficient. Even at a concentration of 10 micromolar, parkin activity does not fully recover in cells with dysfunctional mutations.

(last updated: 5 Nov 2024 )