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GLPG4970

GLPG4970 : Inhibitor of SIK2, SIK3

Structure

Information

  • SIK2
  • SIK3
  • Inhibitor
  • up to 100 nM

In Vitro Validations

Uniprot ID: Q9H0K1
Target Class: Kinase
Target SubClass: CAMK
Potency: IC50
Potency Value: 0.3 nM
Potency Assay: Biochemical assay (ADP-Glo assay)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Serine/threonine-protein kinase SIK2, SNF1LK2, QIK ...

DOI Reference: 10.1021/acs.jmedchem.5c01401

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
The inhibition of enzymatic activity by GLPG4970 at 1 μM was assessed against a panel of 380 kinases. Several kinases showed more than 50% inhibition at 1 μM. IC50 was determined for all kinases with inhibition equal or higher than 50% at 1 μM. Only three kinases had IC50 less than 30-fold higher than IC50 values for both SIK2 and SIK3: Unc-51-like kinase 2 (ULK2, IC50 = 4 nM), receptor-interacting serine/threonine-protein kinase 2 (RIPK2, IC50 = 8 nM), and cyclin G-associated kinase (GAK, IC50 = 15.8 nM).
Probe Selectivity in Vitro:
Selectivity within target family: SIK1/SIK2 selectivity ×16.3, SIK1/SIK3 selectivity x7, SIK2/SIK3 selectivity ×0.4
Potency assay, off target (cells): Selectivity within target family (NanoBRET): SIK1/SIK2 selectivity ×191, SIK1/SIK3 selectivity x105, SIK2/SIK3 selectivity ×0.7
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SERP ratings and comments

No SERP comments found for GLPG4970