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Assay Detail

CHEMBL5223601

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

Binding
Inhibition of human BCL6 BTP domain measured by TR-FRET assay
16
Total Activities
16
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

Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.
Ai Y, Hwang L, MacKerell AD, Melnick A, Xue F.
J Med Chem (2021) 64 : 4333 -4358
PubMed 33844535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.86 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4094351 1 8.54
CHEMBL5184651 1 8.05
CHEMBL4064865 1 7.96
CHEMBL4092565 1 7.92
CHEMBL4100303 1 7.89
CHEMBL5277976 1 7.34
CHEMBL5273385 1 7.20
CHEMBL5207356 1 6.92
CHEMBL4061857 1 6.46
CHEMBL4077836 1 6.43
CHEMBL4445645 1 6.28
CHEMBL4547183 1 6.12
CHEMBL4572689 1 6.07
CHEMBL4542555 1 5.47
CHEMBL4065661 1 4.21
CHEMBL1721570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4094351 IC50 = 2.9 nM 8.54
CHEMBL5184651 IC50 = 8.9 nM 8.05
CHEMBL4064865 IC50 = 11.0 nM 7.96
CHEMBL4092565 IC50 = 12.0 nM 7.92
CHEMBL4100303 IC50 = 13.0 nM 7.89
CHEMBL5277976 IC50 = 46.0 nM 7.34
CHEMBL5273385 IC50 = 63.0 nM 7.20
CHEMBL5207356 IC50 = 120.0 nM 6.92
CHEMBL4061857 IC50 = 350.0 nM 6.46
CHEMBL4077836 IC50 = 370.0 nM 6.43
CHEMBL4445645 IC50 = 520.0 nM 6.28
CHEMBL4547183 IC50 = 760.0 nM 6.12
CHEMBL4572689 IC50 = 860.0 nM 6.07
CHEMBL4542555 IC50 = 3400.0 nM 5.47
CHEMBL4065661 IC50 = 61000.0 nM 4.21
CHEMBL1721570 IC50 = 830000.0 nM -