Activity-based ERBB2 (D769H) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ERBB2 (D769H)
Enzyme
Human ERBB2 (D769H)
HGNC
ERBB2 (D769H)
Synonym
HER2, MLN19, NEU, NGL
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 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 | 64.9 |
| Afatinib | 1 |
| Gefitinib | 10.6 |
| Lapatinib | 37.4 |
| Dacomitinib | 12.2 |
Scientific Information
P04626 (http://www.uniprot.org/uniprot/P04626)
Screening Location
Malvern, PA, USA
Reference compound inhibition of ERBB2 (D769H)
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