CDK12+Cyclin K NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.
Target Overview
Target
CDK12+Cyclin K
HGNC Symbol
CDK12/CCNK complex
Synonyms
CRKRS; CRK7
Cell Line
HEK293 human epithelial cell line from ATCC
Assay Properties
Assay Format
384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay
Assay Protocol
HEK293 cells transiently co-expressing NanoLuc- CDK12 fusion vector and Cyclin K Vector were seeded into the wells of 384-well plates. The cells were pretreated with the NanoBRET Tracer K-12 and then treated with reference compound AT7519 for 1 hour. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism 4 program based on a sigmoidal dose response equation.
Readout
Binding of compound to target kinase
Reference Compound IC50s
| Compounds | IC50 (M) |
|---|---|
| AT7519 | 1.484e-006 |
Screening Location
Malvern, USA
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