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Assay Detail

CHEMBL4150745

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

Binding
Binding affinity to fluorescently labeled recombinant BCL6 BTB domain (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 10 mins by microscale thermophoresis method
3
Total Activities
3
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

B-cell lymphoma 6 protein (CHEMBL4105786)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design.
Cheng H, Linhares BM, Yu W, Cardenas MG, Ai Y, Jiang W, Winkler A, Cohen S, Melnick A, MacKerell A, Cierpicki T, Xue F.
J Med Chem (2018) 61 : 7573 -7588
PubMed 29969259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 4.84 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061302 1 5.16
CHEMBL4168460 1 4.52
CHEMBL4066375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061302 Kd = 7000.0 nM 5.16
CHEMBL4168460 Kd = 30000.0 nM 4.52
CHEMBL4066375 Kd = 129000.0 nM -