APL5125 |
APL5125 : Inhibitor of CSNK2A
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CSNK2A1 |
|
|
Inhibitor
100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
CK2a =0.095 ± 0.052;
CLK2 129 ± 67;
DAPK3 =60 ± 25;
HIPK3 =1,002 ± 550;
DYRK2= 833 ± 305
Selectivity Assessment Description:
ADP-Glo Assay
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Screening at 100 nM (i.e., 1000-fold CK2α Ki) against 468 kinases using the KINOMEscanTM scanMAX pan ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Screening at 1 μM against a panel of 87 enzymes, ion channels, receptors and transporters (SafetyScr ...
Potency Cellular
In Vitro
CSNK2A1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c01807
In Vivo Validations
Mouse
Dose: 3 mg/kg
Route of delivery:
Intravenous
Plasma half life:
1.6 h
Systemic clearance:
12.6 mL/min/Kg
Volume of Distribution at Steady-State:
0.32 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c01807
Rat
Dose: 3 mg/kg
Route of delivery:
Intravenous
Plasma half life:
2.5 h (Avg)
Systemic clearance:
6.9 mL/min/Kg (Avg)
Volume of Distribution at Steady-State:
0.38 L/Kg (Avg)
DOI Reference: 10.1021/acs.jmedchem.5c01807
Dog
Dose: 3 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
3.8 h
Systemic clearance:
2.8 mL/min/Kg
Volume of Distribution at Steady-State:
0.35 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c01807
Chemical Information
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