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Assay Detail

CHEMBL4015779

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

Binding
Binding affinity to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance spectrometry
10
Total Activities
10
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

Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X.
J Med Chem (2017) 60 : 4386 -4402
PubMed 28485934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 6.94 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066850 1 8.47
CHEMBL4090962 1 8.30
CHEMBL4094351 1 8.19
CHEMBL4093431 1 7.66
CHEMBL4072699 1 6.41
CHEMBL4077836 1 6.30
CHEMBL4061857 1 5.96
CHEMBL4084572 1 4.22
CHEMBL4071527 1 -
CHEMBL4092313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066850 Kd = 3.4 nM 8.47
CHEMBL4090962 Kd = 5.0 nM 8.30
CHEMBL4094351 Kd = 6.5 nM 8.19
CHEMBL4093431 Kd = 22.0 nM 7.66
CHEMBL4072699 Kd = 390.0 nM 6.41
CHEMBL4077836 Kd = 500.0 nM 6.30
CHEMBL4061857 Kd = 1100.0 nM 5.96
CHEMBL4084572 Kd = 60000.0 nM 4.22
CHEMBL4071527 Kd = 689000.0 nM -
CHEMBL4092313 Kd = 319000.0 nM -