Activity-based GRK1 kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
GRK1
Enzyme
Human GRK1
HGNC
GRK1
Synonym
RHOK
Substrates
Casein, 2 mg/ml
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 | 67 |
| Ro 31-8220 | 4,200 |
| GW5074 | >20,000 |
| H-89 | >20,000 |
| Rottlerin | >20,000 |
Scientific Information
Q15835 (http://www.uniprot.org/uniprot/Q15835)
Screening Location
Malvern, USA
Reference compound IC50 for GRK1
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