SGC-CK1γ-1 |
SGC-CK1γ-1 : Inhibitor of CSNK1G1, CSNK1G2, CSNK1G3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CSNK1G1 |
|
|
| CSNK1G2 |
| |
| CSNK1G3 |
|
Inhibitor
up to 5 uM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity was assessed in a panel of 192 kinases via a NanoBRET assay selectivity panel (K192) at ...
Selectivity Assessment Description:
SGC-CK1γ-1 demonstrated excellent selectivity across three biological replicates of K192 assays. The ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
SGC-CK1γ-1 was screened in a larger NanoBRET panel of 240 kinases (K240). Cpd 14 maintained strong i ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
<ultiplexed inhibitor bead and mass spectrometry (MIB/MS) screen was used to further assed Cpd 14.
Selectivity Assessment Description:
Cumulatively, across both the MIB/MS and K240, it was possible to assess the binding of SGC-CK1γ-1 t ...
Potency Cellular
In Vitro
CSNK1G1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c02609
CSNK1G2
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c02609
CSNK1G3
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c02609
Negative Control Compounds
SGC-CK1γ-1N
Notes: SGC-CK1γ-1N (cpd 5) bears structural similarity to 14 and exhibits no affinity for all CK1γ isoforms. In the K240 screen, only one kinase was identified to manifest >30% fractional occupancy: TTK (37%).
SMILES:
N#CC1=CC=C(NC(NC2=CC=C(N3CCOCC3)C=C2OC)=N4)C4=C1
Chemical Information
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