AXL-IN-68

AXL-IN-68 : Inhibitor of AXL

Structure

SERP Rating

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Information

Inhibitor

up to 100 nM

In Vitro Validations

Uniprot ID: P30530

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: IC50

Potency Value: 5.3 nM

Potency Assay: AXL HTFR assay in the presence of 700 μM ATP

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

Target aliases:

Tyrosine-protein kinase receptor UFO, UFO, AXL, UF ...

DOI Reference: 10.1021/acs.jmedchem.5c00238

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Cpd 68 was evaluated for selectivity against a large panel of 403 mutant and nonmutant kinases to determine potential off-target activity. 68 showed <35% of control activity (indicative of stronger binding) against 8 other kinase targets (excluding MERTK and TYRO3), with only one kinase (DRAK1) showing a <50-fold selectivity ratio against AXL upon KD determination.

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