Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4345696

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

Binding
Inhibition of recombinant His-tagged human BCL6 expressed in Escherichia coli BL21 AI cell incubated for 2 hrs by TR-FRET assay
44
Total Activities
44
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

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.
Bellenie BR, Cheung KJ, Varela A, Pierrat OA, Collie GW, Box GM, Bright MD, Gowan S, Hayes A, Rodrigues MJ, Shetty KN, Carter M, Davis OA, Henley AT, Innocenti P, Johnson LD, Liu M, de Klerk S, Le Bihan YV, Lloyd MG, McAndrew PC, Shehu E, Talbot R, Woodward HL, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Hoelder S.
J Med Chem (2020) 63 : 4047 -4068
PubMed 32275432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.07 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4559074 1 7.07
CHEMBL4574515 1 7.01
CHEMBL4465387 1 6.89
CHEMBL4476234 1 6.82
CHEMBL4458261 1 6.72
CHEMBL4573672 1 6.70
CHEMBL4524719 1 6.64
CHEMBL4451702 1 6.58
CHEMBL4463841 1 6.57
CHEMBL4587209 1 6.51
CHEMBL4439574 1 6.48
CHEMBL4466680 1 6.41
CHEMBL4482923 1 6.40
CHEMBL4583696 1 6.40
CHEMBL4450499 1 6.37
CHEMBL4475529 1 6.32
CHEMBL4445645 1 6.28
CHEMBL4459012 1 6.19
CHEMBL4483413 1 6.17
CHEMBL4525209 1 6.15
CHEMBL4548894 1 6.15
CHEMBL4547183 1 6.12
CHEMBL4467613 1 6.10
CHEMBL4572689 1 6.07
CHEMBL4475438 1 6.03
CHEMBL4457011 1 6.02
CHEMBL4469177 1 6.00
CHEMBL4451202 1 6.00
CHEMBL4531272 1 5.92
CHEMBL4576646 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4559074 IC50 = 86.0 nM 7.07
CHEMBL4574515 IC50 = 97.0 nM 7.01
CHEMBL4465387 IC50 = 130.0 nM 6.89
CHEMBL4476234 IC50 = 150.0 nM 6.82
CHEMBL4458261 IC50 = 190.0 nM 6.72
CHEMBL4573672 IC50 = 200.0 nM 6.70
CHEMBL4524719 IC50 = 230.0 nM 6.64
CHEMBL4451702 IC50 = 260.0 nM 6.58
CHEMBL4463841 IC50 = 270.0 nM 6.57
CHEMBL4587209 IC50 = 310.0 nM 6.51
CHEMBL4439574 IC50 = 330.0 nM 6.48
CHEMBL4466680 IC50 = 390.0 nM 6.41
CHEMBL4482923 IC50 = 400.0 nM 6.40
CHEMBL4583696 IC50 = 400.0 nM 6.40
CHEMBL4450499 IC50 = 430.0 nM 6.37
CHEMBL4475529 IC50 = 480.0 nM 6.32
CHEMBL4445645 IC50 = 520.0 nM 6.28
CHEMBL4459012 IC50 = 640.0 nM 6.19
CHEMBL4483413 IC50 = 680.0 nM 6.17
CHEMBL4525209 IC50 = 710.0 nM 6.15
CHEMBL4548894 IC50 = 710.0 nM 6.15
CHEMBL4547183 IC50 = 760.0 nM 6.12
CHEMBL4467613 IC50 = 790.0 nM 6.10
CHEMBL4572689 IC50 = 860.0 nM 6.07
CHEMBL4475438 IC50 = 930.0 nM 6.03
CHEMBL4457011 IC50 = 960.0 nM 6.02
CHEMBL4469177 IC50 = 1000.0 nM 6.00
CHEMBL4451202 IC50 = 990.0 nM 6.00
CHEMBL4531272 IC50 = 1200.0 nM 5.92
CHEMBL4576646 IC50 = 1400.0 nM 5.85
CHEMBL4457356 IC50 = 1400.0 nM 5.85
CHEMBL4550751 IC50 = 1700.0 nM 5.77
CHEMBL4556514 IC50 = 1900.0 nM 5.72
CHEMBL4456923 IC50 = 2100.0 nM 5.68
CHEMBL4554124 IC50 = 2500.0 nM 5.60
CHEMBL4555389 IC50 = 3400.0 nM 5.47
CHEMBL4542555 IC50 = 3400.0 nM 5.47
CHEMBL4560573 IC50 = 3500.0 nM 5.46
CHEMBL4521627 IC50 = 3900.0 nM 5.41
CHEMBL4437454 IC50 = 4500.0 nM 5.35
CHEMBL4550911 IC50 = 4600.0 nM 5.34
CHEMBL4525917 IC50 = 5400.0 nM 5.27
CHEMBL4473868 IC50 = 6600.0 nM 5.18
CHEMBL4556362 IC50 = 37000.0 nM 4.43