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Assay Detail

CHEMBL5046589

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

Binding
Displacement of tracer K5 from NLuc fused TBK1 (unknown origin) expressed in HEK293 cells by NanoBRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD.
J Med Chem (2022) 65 : 1313 -1328
PubMed 34333981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.81 6.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079920 1 6.49
CHEMBL4446892 1 6.47
CHEMBL5085430 1 6.47
CHEMBL5093111 1 5.69
CHEMBL3916849 1 5.63
CHEMBL5090046 1 5.59
CHEMBL5079601 1 5.57
CHEMBL5079149 1 5.21
CHEMBL5084750 1 5.13
CHEMBL5086901 1 -
CHEMBL5083125 1 -
CHEMBL5088682 1 -
CHEMBL5085698 1 -
CHEMBL5089987 1 -
CHEMBL5087433 1 -
CHEMBL5075360 1 -
CHEMBL5087006 1 -
CHEMBL5091582 1 -
CHEMBL5091688 1 -
CHEMBL5072178 1 -
CHEMBL5088930 1 -
CHEMBL5076165 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079920 IC50 = 321.0 nM 6.49
CHEMBL4446892 IC50 = 339.0 nM 6.47
CHEMBL5085430 IC50 = 338.0 nM 6.47
CHEMBL5093111 IC50 = 2050.0 nM 5.69
CHEMBL3916849 IC50 = 2327.0 nM 5.63
CHEMBL5090046 IC50 = 2580.0 nM 5.59
CHEMBL5079601 IC50 = 2680.0 nM 5.57
CHEMBL5079149 IC50 = 6170.0 nM 5.21
CHEMBL5084750 IC50 = 7456.0 nM 5.13
CHEMBL5086901 IC50 > 10000.0 nM -
CHEMBL5083125 IC50 > 10000.0 nM -
CHEMBL5088682 IC50 > 10000.0 nM -
CHEMBL5085698 IC50 > 10000.0 nM -
CHEMBL5089987 IC50 > 10000.0 nM -
CHEMBL5087433 IC50 > 10000.0 nM -
CHEMBL5075360 IC50 > 10000.0 nM -
CHEMBL5087006 IC50 > 10000.0 nM -
CHEMBL5091582 IC50 > 10000.0 nM -
CHEMBL5091688 IC50 > 10000.0 nM -
CHEMBL5072178 IC50 > 10000.0 nM -
CHEMBL5088930 IC50 > 10000.0 nM -
CHEMBL5076165 IC50 > 10000.0 nM -