Compound name
T3-CLK
Protein family
Protein Kinase
Target name
CLK2
Affinity biochemical (nM)
15
Affinity on-target cellular (nM)
17
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000321b
SMILES
CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5ccncc5)ccc4n3)cc2)CC1
InChIKey
IEFFSHLHNYVSEF-UHFFFAOYSA-N
NCBI gene ID
1196
UniProt ID
P49760
Mode of action
Inhibitor
Negative control
T3-CLK-N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/T3-CLK
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 100 nM, closest targets as % of contr.: DYRK1A (0.3%), DYRK1B (4.4%), MAP2K5 (4.9%), KIT (14%), MAP3K5 (19%), PDGFRB (24%), PDGFRA (29%); IC50 follow up in cellular NanoBRET assays: IC50(DYRK1A) = 32 nM, IC50(DYRK1B) = 67 nM, IC50(MAP2K5) >10 µM, IC50(KIT) = 2.44 µM, IC50(MAP3K5) >10 µM, IC50(PDGFRB) = 3 µM, IC50(PDGFRA) = 2.52 µM
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/T3-CLK
Selectivity Number of Off-targets
2