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GLPG4970 | GLPG4970 : Inhibitor of SIK2, SIK3
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
  • IC50:0.3 nM
  • Ki:0.7 nM
  • EC50:16 M
  • IC50:3.6 nM
  • IC50:8.1 nM
  • IC50:83 nM
SIK3
  • IC50:0.7 nM
  • Ki:1.2 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The inhibition of enzymatic activity by GLPG4970 at 1 μM was assessed against a panel of 380 kinases ...
In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family: SIK1/SIK2 selectivity ×16.3, SIK1/SIK3 selectivity x7, SIK2/SIK3 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family (NanoBRET): SIK1/SIK2 selectivity ×191, SIK1/SIK3 selectivity x10 ...

Potency
Cellular
In Vitro

SIK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c01401

SIK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c01401

In Vivo Validations

Mouse
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 3.8 h
Systemic clearance: 1.6 L/h/kg
Fb : 96.4%
Bioavailability: 43.0% PO
Volume of Distribution at Steady-State: 9.0 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c01401

Rat
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 4.7 h
Systemic clearance: 3.3 L/h/Kg
Fb : 95.2%
Bioavailability: 21.0% PO
Volume of Distribution at Steady-State: 22.0 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c01401

Dog
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 6.6 h
Systemic clearance: 1.9 L/h/Kg
Fb : 90.4%
Bioavailability: 41.0% PO
Volume of Distribution at Steady-State: 18.0 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c01401

Orthogonal Probes def

MRIA9

Chemical Information

Molecular Formula C29H31F3N4O2
SMILEs COc1cc(-c2cc(-c3ccc4c(c3)CN(C)C(C)(C)C4)cnc2N)cc2c1C(=O)N(CC(F)(F)F)CC2
InChI InChI=1S/C29H31F3N4O2/c1-28(2)13-19-6-5-17(9-22(19)15-35(28)3)21-11-23(26(33)34-14-21)20-10-18-7-8-36(16-29(30,31)32)27(37)25(18)24(12-20)38-4/h5-6,9-12,14H,7-8,13,15-16H2,1-4H3,(H2,33,34)
Molecular weight 524.24 Da
AlogP 5.333500000000004
HBond acceptors 6
HBond donors 2
Atoms 69

References

Publications

Cross References

Expert Reviews

No SERP comments found for GLPG4970

Probe GLPG4970 is in the process of SERP review.

Please continue to check back for new reviews and commentary.