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Assay Detail

CHEMBL5338294

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

Binding
Inhibition of SIK in human U2OS cells assessed as CRTC3 nuclear translocation measured after 1 hr by high content imaging analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 1 5.77 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5393771 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5393771 EC50 = 1703.0 nM 5.77