Activity-based BTK (T474I) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
BTK (T474I)
Enzyme
Human BTK (T474I)
HGNC
BTK (T474I)
Synonym
Tyrosine-protein kinase BTK, Bruton tyrosine kinase, Agammaglobulinaemia tyrosine kinase, ATK, B cell progenitor kinase, BPK, AGMX1, AT, PSCTK1
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/ml
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 9.3 |
| PP2 | 3,000 |
| AG1478 | 2,500 |
| EGFR/ErbB Inhibitor | 5.0 |
| D-64406 | 287,000 |
Scientific Information
Q06187 (http://www.uniprot.org/uniprot/Q06187)
Screening Location
Malvern, USA
Reference compound IC50 for BTK (T474I)
PDF