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Assay Detail

CHEMBL5503029

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

Binding
Inhibition of NF-kappaB activation in human TMD8 cells assessed as reduction in nucleus translocation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type TMD8
Subcellular Nucleus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Nuclear factor NF-kappa-B complex (CHEMBL2094258)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Himmelbauer MK, Bajrami B, Basile R, Capacci A, Chen T, Choi CK, Gilfillan R, Gonzalez-Lopez de Turiso F, Gu C, Hoemberger M, Johnson DS, Jones JH, Kadakia E, Kirkland M, Lin EY, Liu Y, Ma B, Magee T, Mantena S, Marx IE, Metrick CM, Mingueneau M, Murugan P, Muste CA, Nadella P, Nevalainen M, Parker Harp CR, Pattaropong V, Pietrasiewicz A, Prince RJ, Purgett TJ, Santoro JC, Schulz J, Sciabola S, Tang H, Vandeveer HG, Wang T, Yousaf Z, Helal CJ, Hopkins BT.
J Med Chem (2024) 67 : 8122 -8140
PubMed 38712838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.72 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5532458 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5532458 IC50 = 1.9 nM 8.72