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GPLG3970 | GPLG3970 : Inhibitor of SIK2, SIK3
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SIK2
  • IC50:7.8 nM
  • EC50:254 nM
SIK3
  • IC50:3.8 nM
  • EC50:79 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective agains SIK1 IC50 282.8 nM The inhibition of enzymatic activity by GPLG3970 at a concentrat ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
NanoBRET assay SIK1 IC50 >17500 nM

Potency
Cellular
In Vitro

SIK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02246

SIK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02246

In Vivo Validations

Mouse
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 0.555 h IV, 1.28 h PO
Systemic clearance: 5.57 L/h/Kg
Area Under the Curve:: 402 IV, 1380 PO ng·h/mL
Bioavailability: 68.7%
Volume of Distribution at Steady-State: 2.51 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c02246

Rat
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 1.42 h IV, 3.61 h PO
Systemic clearance: 7.64 L/h/Kg
Area Under the Curve:: 759 ng·h/mL IV, 2120 ng·h/mL PO
Bioavailability: 55.9%
Volume of Distribution at Steady-State: 2.82 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c02246

Dog
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 4.28 h IV, 4.63 h PO
Systemic clearance: 1.57 L/h/Kg
Area Under the Curve:: 897 ng·h/mL IV, 1840 ng·h/mL PO
Bioavailability: 41.0%
Volume of Distribution at Steady-State: 2.89 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c02246

Chemical Information

Molecular Formula C25H27F3N4O4
SMILEs COc1cc(-c2cnc3cc(OCCN4CCOCC4)ccn23)cc2c1C(=O)N(CC(F)(F)F)CC2
InChI InChI=1S/C25H27F3N4O4/c1-34-21-13-18(12-17-2-4-31(16-25(26,27)28)24(33)23(17)21)20-15-29-22-14-19(3-5-32(20)22)36-11-8-30-6-9-35-10-7-30/h3,5,12-15H,2,4,6-11,16H2,1H3
Molecular weight 504.20 Da
AlogP 0.0
HBond acceptors 8
HBond donors --
Atoms 63

References

Publications

Cross References

canSAR

Expert Reviews

by SERP
(on 1 Jul 2024 )
Cellular Use Rating
In Model Organisms
GLPG3970 is an advanced molecule which was tested in clinical trials up to Phase 2. As such it is suitable for both cellular and in vivo use to study its main targets SIK2 and SIK3. GLPG3970 displayed...
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