Activity-based RET-CCDC6 (PTC1) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
-RET, CCDC6 (PTC1)
Enzyme
Human CCDC6-RET (PTC1) fusion
HGNC
RET-CCDC6
Synonym
CDHF12, CDHR16, HSCR1, MEN2A, MEN2B, MTC1, PTC, RET51
Substrates
Peptide substrate, [RRRRRRRRRRRVYSTDYYRLFNPS], 20 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
Compounds | IC50 (nM) |
---|---|
Staurosporine | 5.1 |
PP2 | 28 |
AG1478 | 450 |
EGFR/ErbB Inhibitor | >100,000 |
D-64406 | 140 |
Scientific Information
Screening Location
Malvern, USA
PDF