BI-1347

BI-1347 : Inhibitor of CDK8 and CDK19

Structure

SERP Rating

Probe BI-1347 is in the process of SERP review.

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Information

CDK8
CDK19

Inhibitor

up to 1 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P49336

Target Class: Kinase

Target SubClass: CMGC

Potency: Kd

Potency Value: 0.77 nM

Potency Assay: Biochemical assay

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

Target aliases:

Cyclin-dependent kinase 8, CDK8, CDK8_HUMAN, Prote ...

DOI Reference: 10.1021/acsmedchemlett.9b00480

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Invitrogen® panel: 369 kinases screened @ 10 µM Selected IC50 measured @ Invitrogen®: CDK8 IC50 = 1.5 nM; CDK11 IC50 = 1.7 nM; MLCK IC50 = 531 nM; AURKB IC50 = 809 nM; FLT3 IC50 = 1360 nM; ICK IC50 = 2390 nM; STK16 IC50 = 3550 nM Eurofins Safety Panel 44™ External screen covering 44 targets: @ 10 µM

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SERP ratings and comments

No SERP comments found for BI-1347