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Assay Detail

CHEMBL5502964

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

Functional
Inhibition of CD69 expression on CD19+ B-cells in human whole blood pretreated for 60 mins followed by anti-IgD stimulation and measured after 18 to 22 hrs by flow cytometry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Cell Type CD19 positive B cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 18 9.74 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5550053 1 10.59
CHEMBL5557589 1 10.44
CHEMBL5518143 1 10.44
CHEMBL5557842 1 10.12
CHEMBL5532458 1 10.10
CHEMBL5527884 1 10.06
CHEMBL5537092 1 9.80
CHEMBL5555942 1 9.62
CHEMBL5532190 1 9.59
CHEMBL5555488 1 9.59
CHEMBL5558638 1 9.48
CHEMBL5532361 1 9.32
CHEMBL5517827 1 9.13
CHEMBL5549912 1 9.04
CHEMBL5556300 1 8.76
CHEMBL5505923 1 -
CHEMBL5557093 1 -
CHEMBL5512502 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5550053 IC50 = 0.026 nM 10.59
CHEMBL5557589 IC50 = 0.036 nM 10.44
CHEMBL5518143 IC50 = 0.036 nM 10.44
CHEMBL5557842 IC50 = 0.075 nM 10.12
CHEMBL5532458 IC50 = 0.079 nM 10.10
CHEMBL5527884 IC50 = 0.087 nM 10.06
CHEMBL5537092 IC50 = 0.157 nM 9.80
CHEMBL5555942 IC50 = 0.241 nM 9.62
CHEMBL5532190 IC50 = 0.257 nM 9.59
CHEMBL5555488 IC50 = 0.256 nM 9.59
CHEMBL5558638 IC50 = 0.333 nM 9.48
CHEMBL5532361 IC50 = 0.478 nM 9.32
CHEMBL5517827 IC50 = 0.736 nM 9.13
CHEMBL5549912 IC50 = 0.91 nM 9.04
CHEMBL5556300 IC50 = 1.72 nM 8.76
CHEMBL5505923 IC50 > 10.0 nM -
CHEMBL5557093 IC50 > 10.0 nM -
CHEMBL5512502 IC50 > 10.0 nM -