Compound name
SGC-CLK-1 (UNC-CAF-170 )
Protein family
Protein Kinase
Target name
CLK1
Affinity biochemical (nM)
41
Affinity on-target cellular (nM)
165
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000724a
SMILES
COC1=NN2N=CC(C3=NC(NC4=CC(C(F)(F)F)=CC(OC)=C4)=NC=C3)=C2C=C1
InChIKey
GJYVLTPTDBQQCY-UHFFFAOYSA-N
NCBI gene ID
1195
UniProt ID
P49759
Mode of action
Inhibitor
Negative control
SGC-CLK-1N (UNC-CAF-225 )
Affinity biochemical definition
IC50
Affinity biochemical assay type
Binding assays (Luceome Biotechniology)
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/SGC-CLK-1
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 1 µM, closest targets as % of contr.: MAPK15 (21%), HIPK1 (31%), HIPK2 (34%), NEK7 (40%), PIP5K2B (50%), STK16 (53%), S(35) = 0.02; Follow-up IC50s in cellular NanoBRET assays: IC50(HIPK1/2) >10 µM, IC50(STK16) = 167 nM (partial inhibition), others NA;
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/SGC-CLK-1
Selectivity Number of Off-targets
0