Compound name
SGC-CK2-2
Protein family
Protein Kinase
Target name
CSNK2A2
Affinity biochemical (nM)
1
Affinity on-target cellular (nM)
200
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001873a
SMILES
O=C(O)c1ccc2c(c1)nc(NCc1ccccc1)c1ncncc12
InChIKey
HEVVNKYNJCSHFA-UHFFFAOYSA-N
NCBI gene ID
1459
UniProt ID
P19784
Synonyms
CSNK2A1, CK2alpha'
Mode of action
Inhibitor
Negative control
SGC-CK2-2N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (Eurofins)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530
Affinity biochemical relation
>
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (intact HEK293T cells)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530
Affinity on-target cellular relation
=
Selectivity platform
DiscoverX scanMAX assay
Selectivity platform number of targets
403
Selectivity remarks
Screened at 1 µM, closest targets as % of control: CSNK2A1 (0.1%), CK2A2 (0.2%), DAPK3 (6.5%), HIPK1 (10%), DAPK2 (11%), HIPK3 (16%), MYLK4 (20%), PIK3CG (23%), PIK3C2G (25%), DYRK1A (28%), HIPK2 (30%), DRAK2 (30%), YSK4 (34%), https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DAPK3) = 1500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK1) = 1800 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DAPK2) = 1500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK3) = 900 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(MYLK4) > 10000 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(PIK3CG) = 5300 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(PIK3C2G) = 4500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DYRK1A) = 760 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK2) = 600 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DRAK2) = 1800 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(YSK4) = 37000 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DAPK3) = 1500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK1) = 1800 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DAPK2) = 1500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK3) = 900 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(MYLK4) > 10000 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(PIK3CG) = 5300 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(PIK3C2G) = 4500 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DYRK1A) = 760 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(HIPK2) = 600 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DRAK2) = 1800 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(YSK4) = 37000 nM, https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00530
Selectivity Number of Off-targets
3