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Assay Detail

CHEMBL4364415

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

Binding
Inhibition of TBK1 in TLR3-stimulated human PBMC assessed as decrease in poly(I:C)-induced IFNalpha secretion preincubated for 1 hr followed by poly(I:C) addition and measured after 16 hrs by FACS based cytometric bead array method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase TBK1 (CHEMBL5408)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.
Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B, Kasparcova V, Ramanjulu JM, Pesiridis GS, Muelbaier M, Bergamini G.
ACS Med Chem Lett (2019) 10 : 780 -785
PubMed 31097999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.10 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446892 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446892 IC50 = 794.33 nM 6.10