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Assay Detail

CHEMBL5338300

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

Functional
Antiinflammatory activity against LPS-stimulated human whole blood assessed as inhibition of LPS-stimulated TNF-alpha production pretreated for 30 mins followed by LPS challenge and measured after 2 hrs
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
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 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5393771 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5393771 IC50 = 1000.0 nM 6.00