Empesertib

Empesertib : Inhibitor of TTK

Structure

SERP Rating

Probe Empesertib is in the process of SERP review.

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Information

Inhibitor

100 nM

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Probe Availability:

In Vitro Validations

Uniprot ID: P33981

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 1.7 nM

Potency Assay: HTRF-based MPS1 assay with an ATP concentration of 2 mM

PDB ID for probe-target interaction (3D structure): 6TNB

Structure-activity relationship: yes

Target aliases:

Dual specificity protein kinase TTK, MPS1L1, MPS1, ...

DOI Reference: 10.1021/acs.jmedchem.9b02035

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : % inh. JNK2 54% @ 1 uM, JNK3 84% @ 1 uM

Probe Selectivity in Vitro:

Empesertib only inhibits two kinases, JNK2 and JNK3, more than 50% at a concentration of 1 μmol/L and no other kinase at 100 nmol/L in the Millipore kinase panel of 230 kinases

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No SERP comments found for Empesertib