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Assay Detail

CHEMBL4345698

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

Binding
Inhibition of recombinant human Nanoluc-tagged BCL6/Halo-tagged SMRT transfected in human HEK293T cells assessed as reduction in BCL6/SMRT interaction incubated for 6 hrs by NANOBRET assay
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

BCL-6/NCOR2 (CHEMBL4523673)
Type PROTEIN-PROTEIN INTERACTION
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 17 5.46 6.22
DC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4574515 1 6.22
CHEMBL4458261 1 5.81
CHEMBL4451702 1 5.75
CHEMBL4476234 1 5.75
CHEMBL4463841 1 5.64
CHEMBL4583696 1 5.60
CHEMBL4450499 1 5.57
CHEMBL4467613 1 5.34
CHEMBL4475529 1 5.34
CHEMBL4475438 1 5.30
CHEMBL4548894 1 5.23
CHEMBL4459012 1 4.89
CHEMBL4547183 1 4.52
CHEMBL4531272 1 -
CHEMBL4457356 1 -
CHEMBL4560573 1 -
CHEMBL4469177 1 -
CHEMBL4542555 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4574515 IC50 = 600.0 nM 6.22
CHEMBL4458261 IC50 = 1550.0 nM 5.81
CHEMBL4451702 IC50 = 1800.0 nM 5.75
CHEMBL4476234 IC50 = 1760.0 nM 5.75
CHEMBL4463841 IC50 = 2300.0 nM 5.64
CHEMBL4583696 IC50 = 2500.0 nM 5.60
CHEMBL4450499 IC50 = 2700.0 nM 5.57
CHEMBL4467613 IC50 = 4600.0 nM 5.34
CHEMBL4475529 IC50 = 4600.0 nM 5.34
CHEMBL4475438 IC50 = 5000.0 nM 5.30
CHEMBL4548894 IC50 = 5900.0 nM 5.23
CHEMBL4459012 IC50 = 13000.0 nM 4.89
CHEMBL4547183 IC50 = 30000.0 nM 4.52
CHEMBL4531272 IC50 - -
CHEMBL4457356 IC50 - -
CHEMBL4560573 IC50 - -
CHEMBL4469177 IC50 - -
CHEMBL4542555 DC50 > 30.0 uM -