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Assay Detail

CHEMBL5168563

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

Binding
Degradation of BCL6 in human OCI-Ly1 cells incubated for 2 hrs by MSD assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type OCI-Ly1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

B-cell lymphoma 6 protein (CHEMBL4105786)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 <i>In Vivo</i>.
Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S.
J Med Chem (2022) 65 : 8191 -8207
PubMed 35653645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.87 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205388 1 9.15
CHEMBL5205212 1 8.66
CHEMBL5204505 1 8.57
CHEMBL5172641 1 8.20
CHEMBL5208698 1 8.15
CHEMBL5193571 1 8.01
CHEMBL5172688 1 7.49
CHEMBL5200057 1 7.46
CHEMBL4445645 1 7.27
CHEMBL4559074 1 7.10
CHEMBL5187061 1 6.56
CHEMBL5203177 1 -
CHEMBL5174171 1 -
CHEMBL5194697 1 -
CHEMBL5205838 1 -
CHEMBL5196650 1 -
CHEMBL5180823 1 -
CHEMBL5171631 1 -
CHEMBL5181921 1 -
CHEMBL5171519 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205388 EC50 = 0.7 nM 9.15
CHEMBL5205212 EC50 = 2.2 nM 8.66
CHEMBL5204505 EC50 = 2.7 nM 8.57
CHEMBL5172641 EC50 = 6.3 nM 8.20
CHEMBL5208698 EC50 = 7.1 nM 8.15
CHEMBL5193571 EC50 = 9.8 nM 8.01
CHEMBL5172688 EC50 = 32.6 nM 7.49
CHEMBL5200057 EC50 = 35.0 nM 7.46
CHEMBL4445645 EC50 = 54.0 nM 7.27
CHEMBL4559074 EC50 = 80.0 nM 7.10
CHEMBL5187061 EC50 = 276.0 nM 6.56
CHEMBL5203177 EC50 > 2000.0 nM -
CHEMBL5174171 EC50 > 2000.0 nM -
CHEMBL5194697 EC50 > 2000.0 nM -
CHEMBL5205838 EC50 > 2000.0 nM -
CHEMBL5196650 EC50 > 2000.0 nM -
CHEMBL5180823 EC50 > 2000.0 nM -
CHEMBL5171631 EC50 > 2000.0 nM -
CHEMBL5181921 EC50 > 2000.0 nM -
CHEMBL5171519 EC50 > 2000.0 nM -