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Assay Detail

CHEMBL5338273

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of SIK2 (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase SIK2 (CHEMBL5699)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Peixoto C, Joncour A, Temal-Laib T, Tirera A, Dos Santos A, Jary H, Bucher D, Laenen W, Pereira Fernandes A, Lavazais S, Delachaume C, Merciris D, Saccomani C, Drennan M, López-Ramos M, Wakselman E, Dupont S, Borgonovi M, Roca Magadan C, Monjardet A, Brys R, De Vos S, Andrews M, Jimenez JM, Amantini D, Desroy N.
J Med Chem (2024) 67 : 5233 -5258
PubMed 38552030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.06 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5407103 1 9.40
CHEMBL5405960 1 8.72
CHEMBL5398906 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5407103 IC50 = 0.4 nM 9.40
CHEMBL5405960 IC50 = 1.9 nM 8.72
CHEMBL5398906 IC50 < 1.0 nM -