Defactinib

Inhibitor of PTK2, PTK2B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe Defactinib is in the process of SERP review.

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Information

PTK2
PTK2B

Inhibitor

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q05397

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 0.2 nM

Potency Assay: Binding versus recombinant human enzyme kinase domain

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

Target aliases:

Focal adhesion kinase 1, FAK1, FAK, PTK2, FAK1_HUM ...

DOI Reference: 10.1093/jnci/djt210

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Profiling against an Invitrogen panel at 10 µM and 1 µM: Strongest inhibition found for NTRK1 (IC50 = 56 nM) and MAP3K9 (IC50 = 75.3 nM). Selectivity outside target family: Cerep profile against 122 human receptors, ion channels, enzymes, and uptake sites: the closest off-target is ADORA3 (Adenosine A3) (Ki = 27 nM); Clean GPCR scan

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Please keep in mind that other kinases will be inhibited along with FAK. No kinome-wide cellular profiling has been done for this compound, however, based on the biochemical and cell free profiling, one should note that FLT3, CLK2, JAK kinases, TRK kinases will likely be potently inhibited along with FAK. Use caution when interpreting phenotypic results when using defactinib (same with nearly every kinase inhibitor).

(last updated: 23 Apr 2022 )