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Assay Detail

CHEMBL5502965

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

Functional
Inhibition of human TMD8 cells proliferation incubated for 35 to 72 hrs by CellTiter-Glo luminescent cell viability assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TMD8
Confidence 1 — Organism
Curated By Autocuration

Target

TMD8 (CHEMBL4296503)
Type CELL-LINE
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 16 8.68 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557842 1 9.38
CHEMBL5557589 1 9.20
CHEMBL5555942 1 9.18
CHEMBL5518143 1 9.12
CHEMBL5532458 1 9.09
CHEMBL5527884 1 9.03
CHEMBL5537092 1 8.75
CHEMBL5532361 1 8.62
CHEMBL5517827 1 8.53
CHEMBL5558638 1 7.90
CHEMBL5532190 1 7.74
CHEMBL5555488 1 7.58
CHEMBL5556300 1 -
CHEMBL5550053 1 -
CHEMBL5505923 1 -
CHEMBL5557093 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557842 IC50 = 0.42 nM 9.38
CHEMBL5557589 IC50 = 0.63 nM 9.20
CHEMBL5555942 IC50 = 0.66 nM 9.18
CHEMBL5518143 IC50 = 0.76 nM 9.12
CHEMBL5532458 IC50 = 0.82 nM 9.09
CHEMBL5527884 IC50 = 0.94 nM 9.03
CHEMBL5537092 IC50 = 1.79 nM 8.75
CHEMBL5532361 IC50 = 2.39 nM 8.62
CHEMBL5517827 IC50 = 2.94 nM 8.53
CHEMBL5558638 IC50 = 12.5 nM 7.90
CHEMBL5532190 IC50 = 18.38 nM 7.74
CHEMBL5555488 IC50 = 26.38 nM 7.58
CHEMBL5556300 IC50 > 1000.0 nM -
CHEMBL5550053 IC50 > 1000.0 nM -
CHEMBL5505923 IC50 > 1000.0 nM -
CHEMBL5557093 IC50 > 1000.0 nM -