PEXIDARTINIB

PEXIDARTINIB : ATP-competitive of CSF1R

Structure

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Information

CSF1R

ATP-competitive

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P07333

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 13 nM

Potency Assay: Enzymatic assay with 100μM ATP

PDB ID for probe-target interaction (3D structure): 4R7H, 7KHG

Target aliases:

Macrophage colony-stimulating factor 1 receptor, F ...

DOI Reference: 10.1056/NEJMoa1411366

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: KIT

Potency end-point : IC50 27 nM

Potency assay (off target): SelectScreen profiling Invitrogen of 227 kinases was carried out showing the following IC50s (uM): CSF1R 0.013. KIT 0.027, CDK19 0.14, FLT3 0.16, KDR 0.44, LCK 0.86, FLT1 0.88, TRKC 0.89

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(last updated: 18 Oct 2022 )