Compound name
CC-671
Protein family
Protein Kinase
Target name
TTK
Affinity biochemical (nM)
5
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
7272
UniProt ID
P33981
Synonyms
MPS1, MPS1L1, CT96, MPH1
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
=
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