IR-2

IR-2 : Degrader (PROTAC) of BTK

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 IR-2 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

Degrader (PROTAC)

100 nM

In Vitro Validations

Uniprot ID: Q06187

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 14 nM

Potency Assay: Inhibition of BTK

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

Target aliases:

Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

DOI Reference: 10.1021/jacs.9b13907

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Quantitative label-free proteomics

Probe Selectivity in Vitro:

BTK was efficiently degraded by all the PROTACs we tested. IR-2 also degraded the known ibrutinib off-targets CSK, LYN, and BLK, while several other off-targets, such as LCK and PLK1, were not significantly affected.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 23 Mar 2022 )

SERP Ratings

In Cell Rating

(last updated: 26 Mar 2022 )