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Assay Detail

CHEMBL4336433

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

Binding
Inhibition of Bcl6 (unknown origin) by TR-FRET assay
4
Total Activities
4
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

Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.
Balazs AYS, Carbajo RJ, Davies NL, Dong Y, Hird AW, Johannes JW, Lamb ML, McCoull W, Raubo P, Robb GR, Packer MJ, Chiarparin E.
J Med Chem (2019) 62 : 9418 -9437
PubMed 31361481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.32 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4094351 1 8.54
CHEMBL4448503 1 7.60
CHEMBL4517433 1 6.72
CHEMBL4077836 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4094351 IC50 = 2.9 nM 8.54
CHEMBL4448503 IC50 = 25.0 nM 7.60
CHEMBL4517433 IC50 = 190.0 nM 6.72
CHEMBL4077836 IC50 = 370.0 nM 6.43