EMD 1214063

EMD 1214063 : Inhibitor of MET

Structure

SERP Rating

Probe EMD 1214063 is in the process of SERP review.

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Information

Inhibitor

up to 100 nM

In Vitro Validations

Uniprot ID: P08581

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: IC50

Potency Value: 3 nM

Potency Assay: Biochemical Assay

PDB ID for probe-target interaction (3D structure): 4R1V, 8AU3, 8AU5, 8AW1

Target aliases:

Hepatocyte growth factor receptor, MET, MET_HUMAN, ...

DOI Reference: 10.1158/1078-0432.CCR-12-3247

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Kinase inhibition by EMD 1214063 (1 and 10 μM) was assessed in vitro using a panel of 242 different kinases. Only 5 of the other 241 kinases were inhibited by EMD 1214063 by more than 50%, namely IRAK4, TrkA, Axl, IRAK1, and Mer.

Probe Selectivity in Vitro:

Formal IC50 determinations conducted with these kinases resulted in IC50 values ranging from 615 to 2,272 nM. Such high IC50 values make it unlikely that EMD 1214063 will achieve in vivo pharmacologically relevant inhibitory activity on IRAK4, TrkA, Axl, IRAK1, and Mer.

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SERP ratings and comments

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