Assay Detail
Binding
CHEMBL5168562
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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 |
Publication
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 <i>In Vivo</i>.
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 |