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Assay Detail

CHEMBL4015787

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

Binding
Inhibition of GAL4 DNA binding domain fused BCL6 BTB domain (unknown origin) expressed in HEK 293T/17 cells after 24 hrs by Bright-Glo luciferase cell reporter assay
31
Total Activities
18
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
IC50 31 5.99 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100303 2 7.10
CHEMBL4092565 2 7.00
CHEMBL4073463 2 6.90
CHEMBL4064865 2 6.70
CHEMBL4062105 2 6.40
CHEMBL4096773 2 6.32
CHEMBL4083842 2 6.10
CHEMBL4084806 2 5.96
CHEMBL4094351 1 5.70
CHEMBL4102754 2 5.50
CHEMBL4101172 1 5.40
CHEMBL4090962 2 5.40
CHEMBL4078747 2 5.30
CHEMBL4063061 2 5.21
CHEMBL4093418 1 5.20
CHEMBL4083173 1 5.00
CHEMBL4085689 1 4.80
CHEMBL4061302 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100303 IC50 = 79.43 nM 7.10
CHEMBL4100303 IC50 = 87.0 nM 7.06
CHEMBL4092565 IC50 = 100.0 nM 7.00
CHEMBL4092565 IC50 = 100.0 nM 7.00
CHEMBL4073463 IC50 = 125.89 nM 6.90
CHEMBL4073463 IC50 = 140.0 nM 6.85
CHEMBL4064865 IC50 = 199.53 nM 6.70
CHEMBL4064865 IC50 = 200.0 nM 6.70
CHEMBL4062105 IC50 = 398.11 nM 6.40
CHEMBL4062105 IC50 = 430.0 nM 6.37
CHEMBL4096773 IC50 = 480.0 nM 6.32
CHEMBL4096773 IC50 = 501.19 nM 6.30
CHEMBL4083842 IC50 = 794.33 nM 6.10
CHEMBL4083842 IC50 = 830.0 nM 6.08
CHEMBL4084806 IC50 = 1100.0 nM 5.96
CHEMBL4084806 IC50 = 1258.93 nM 5.90
CHEMBL4094351 IC50 = 1995.26 nM 5.70
CHEMBL4102754 IC50 = 3162.28 nM 5.50
CHEMBL4102754 IC50 = 3200.0 nM 5.50
CHEMBL4090962 IC50 = 3981.07 nM 5.40
CHEMBL4101172 IC50 = 3981.07 nM 5.40
CHEMBL4090962 IC50 = 4100.0 nM 5.39
CHEMBL4078747 IC50 = 5011.87 nM 5.30
CHEMBL4078747 IC50 = 5000.0 nM 5.30
CHEMBL4063061 IC50 = 6100.0 nM 5.21
CHEMBL4063061 IC50 = 6309.57 nM 5.20
CHEMBL4093418 IC50 = 6309.57 nM 5.20
CHEMBL4083173 IC50 = 10000.0 nM 5.00
CHEMBL4085689 IC50 = 15848.93 nM 4.80
CHEMBL4061302 IC50 > 30000.0 nM -
CHEMBL4061302 IC50 > 31622.78 nM -