Compound name
SGC-CK2-1
Protein family
Protein Kinase
Target name
CSNK2A1
Affinity biochemical (nM)
4.2
Affinity on-target cellular (nM)
36
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001183a
SMILES
CC1=CC=C(NC2=NC3=C(C#N)C=NN3C(NC4CC4)=C2)C=C1NC(CC)=O
InChIKey
YKDZIFFKQUNVHH-UHFFFAOYSA-N
NCBI gene ID
1457
UniProt ID
P68400
Synonyms
Cka1, Cka2
Mode of action
Inhibitor
Negative control
SGC-CK2-1N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (Eurofins at 10 µM ATP)
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S2451945620305225?via%3Dihub
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/pii/S2451945620305225?via%3Dihub
Affinity on-target cellular relation
=
Selectivity platform
ScanMAX (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, S-Score(10) = 0.007 at 1 µM, closest targets as % of inhibition: STK17A (100%), DYRK2 (86%), PLK4 (77%), HIPK2 (72%), MEK5 (72%), HIPK1 (68%), HIPK3 (66%); In-cellulo follow-up of closest targets (NanoBRET assay in HEK293T cells): IC50(STK17A) >10000 nM, IC50(DYRK2) = 440 nM, IC50(PLK4) >10000 nM, IC50(HIPK2) = 3400 nM, IC50(MEK5) n.d., IC50(HIPK1) = 3700 nM, IC50(HIPK3) = 8100 nM; In-vitro follow-up of MEK5 in enzymatic assay: 0% inhibition at 1 µM (https://www.sciencedirect.com/science/article/pii/S2451945620305225?via%3Dihub);
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S2451945620305225?via%3Dihub