ULIXERTINIB

ULIXERTINIB : Inhibitor of MAPK1, MAPK3

Structure

SERP Rating

Probe ULIXERTINIB is in the process of SERP review.

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Information

MAPK1
MAPK3

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: P28482

Target Class: Kinase

Target SubClass: CMGC

Potency Value: Km 0.3 nM

Potency Assay: ERK2 biochemical assay

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

Target aliases:

Mitogen-activated protein kinase 1, PRKM2, PRKM1, ...

DOI Reference: 10.1021/acs.jmedchem.5b00466

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

BVD-523 demonstrated ERK1/2 kinase selectivity based on biochemical counter-screens against 75 kinases, in addition to ERK1 and ERK2. The ATP concentrations were approximately equal to the Km in all assays. Kinases inhibited to greater than 50% by 2 μM BVD-523 were retested to generate Ki values. Twelve of the 14 kinases had a Ki of <1 μM. The selectivity of BVD-523 for ERK2 was >7,000-fold for all kinases tested except ERK1, which was inhibited with a Ki of <0.3 nM (10-fold). DOI: 10.1158/1535-7163.MCT-17-0456

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