Compound name
CC-671
Protein family
Protein Kinase
Target name
CLK2
Affinity biochemical (nM)
6
Affinity on-target cellular (nM)
15
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000642a
SMILES
CC1=NC2=C(O1)C=C(C=C2)C3=CNC4=C3C(=NC(=N4)NC5=C(C=C(C=C5)C(=O)NC)OC)OC6CCCC6
InChIKey
CWJLAVRXVFHDSJ-UHFFFAOYSA-N
NCBI gene ID
1196
UniProt ID
P49760
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
LanthaScreen Eu kinase binding assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.7b01223
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ActivX KiNative profiling assay (in HCT-116 cell line (CRL-1619))
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (Invitrogen)
Selectivity platform number of targets
255
Selectivity remarks
Screened at 3 µM, closest targets as % inhibition: CLK1 (99%), DYRK1A/B (94/98%), DYRK3 (95%), PHKG (96%); In vitro follow-up (Invitrogen): IC50(DYRK3) = 99 nM, IC50(DYRK1A/B) = 104/157 nM, IC50(PHKG) = 136 nM, IC50(CLK3) = 300 nM; Cellular selectivity: IC50(JNK1/2/3) = 0.68 µM, IC50(CAMKK2) = 1.10 µM, IC50(PIP4K2C) = 1.30 µM (ActivX KiNative profiling assay (in HCT-116 cell line (CRL-1619))
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.7b01223
Selectivity Number of Off-targets
5