Chemical Probes logo
APL5125 | APL5125 : Inhibitor of CSNK2A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CSNK2A1
  • IC50:0.35 nM
  • Kd:1.4 nM
  • Ki:0.095 ± 0.052 nM
  • IC50:5.56 nM
  • GI50:325 ± 110 nM
  • IC50:27.8 nM
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

Molecular Formula C27H24F5N3O5
SMILEs O=C(O)c1ccc2c(c1)nc(OCCOCCCCNCc1cc(F)c(OC(F)(F)F)c(F)c1)c1ccncc12
InChI InChI=1S/C27H24F5N3O5/c28-21-11-16(12-22(29)24(21)40-27(30,31)32)14-33-6-1-2-8-38-9-10-39-25-19-5-7-34-15-20(19)18-4-3-17(26(36)37)13-23(18)35-25/h3-5,7,11-13,15,33H,1-2,6,8-10,14H2,(H,36,37)
Molecular weight 565.16 Da
AlogP 5.623400000000005
HBond acceptors 8
HBond donors 2
Atoms 64

Expert Reviews

by SERP
(on 2 May 2026)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 13 May 2026)
Cellular Use Rating
In Model Organisms
An inactive control would render this probe more useful. A more comprehensive PK study of the molecule in mice (different vehicles with PK data) would be advisable particularly as mice are the most widely...
If you wish to explore AI-generated evaluations, please visit the page on our collaborator Compound VALET.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria