Activity-based CHK1 kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
CHK1
Enzyme
Human CHK1
HGNC
CHEK1
Synonym
CHEK1
Substrates
Peptide substrate, [KKKVSRSGLYRSPSMPENLNRPR], 20 µM
ATP 10 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
Compounds | IC50 (nM) |
---|---|
Staurosporine | 0.3 |
Ro 31-8220 | 18.7 |
GW 5074 | 5,400 |
H-89 | 1,200 |
Rottlerin | >100,000 |
Scientific Information
O14757 (http://www.uniprot.org/uniprot/O14757)
Screening Location
Malvern, USA
Reference compound IC50 for CHK1
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