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Assay Detail

CHEMBL5168562

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

Binding
Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay
20
Total Activities
20
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

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
IC50 20 8.02 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204505 1 8.82
CHEMBL5205388 1 8.66
CHEMBL5171519 1 8.60
CHEMBL5196650 1 8.54
CHEMBL5194697 1 8.54
CHEMBL5181921 1 8.52
CHEMBL5193571 1 8.48
CHEMBL5208698 1 8.46
CHEMBL5205212 1 8.44
CHEMBL5205838 1 8.44
CHEMBL5203177 1 8.39
CHEMBL5174171 1 8.34
CHEMBL5171631 1 8.22
CHEMBL5180823 1 8.00
CHEMBL5172688 1 7.61
CHEMBL5172641 1 7.44
CHEMBL4559074 1 7.07
CHEMBL5200057 1 7.02
CHEMBL5187061 1 6.62
CHEMBL4445645 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204505 IC50 = 1.5 nM 8.82
CHEMBL5205388 IC50 = 2.2 nM 8.66
CHEMBL5171519 IC50 = 2.5 nM 8.60
CHEMBL5196650 IC50 = 2.9 nM 8.54
CHEMBL5194697 IC50 = 2.9 nM 8.54
CHEMBL5181921 IC50 = 3.0 nM 8.52
CHEMBL5193571 IC50 = 3.3 nM 8.48
CHEMBL5208698 IC50 = 3.5 nM 8.46
CHEMBL5205212 IC50 = 3.6 nM 8.44
CHEMBL5205838 IC50 = 3.6 nM 8.44
CHEMBL5203177 IC50 = 4.1 nM 8.39
CHEMBL5174171 IC50 = 4.6 nM 8.34
CHEMBL5171631 IC50 = 6.0 nM 8.22
CHEMBL5180823 IC50 = 9.9 nM 8.00
CHEMBL5172688 IC50 = 24.6 nM 7.61
CHEMBL5172641 IC50 = 36.5 nM 7.44
CHEMBL4559074 IC50 = 86.0 nM 7.07
CHEMBL5200057 IC50 = 95.0 nM 7.02
CHEMBL5187061 IC50 = 238.0 nM 6.62
CHEMBL4445645 IC50 = 523.0 nM 6.28