Ibrutinib

Covalent Inhibitor of BTK

Structure

SERP Rating

Probe Ibrutinib is in the process of SERP review.

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Information

Covalent Inhibitor

10 nM

DOI - 10.1073/pnas.1004594107

Probe Availability:

In Vitro Validations

Uniprot ID: Q06187

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 0.5 nM

Potency Assay: IC50s were measured using 33P filtration binding assay

PDB ID for probe-target interaction (3D structure): 5P9J

Target aliases:

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

DOI Reference: 10.1073/pnas.1004594107

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: BLK

Potency end-point : IC50 0.5 nM

Off Target: BMX

Potency end-point : IC50 0.8 nM

Probe Selectivity in Cell:

In primary cultures of T cells (which do not express Btk), up-regulation of CD69 induced by T cell receptor stimulus was blocked only by continuous exposure to PCI-32765 at 10 μM. These results indicate that PCI-32765 is more than 1,000-fold selective for inhibition of antigen receptor signaling in B cells over T cells, and that only B-cell inhibition is sustained following short duration treatment.

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