Assay Detail
Binding
CHEMBL5054285
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Displacement of biotin-tagged LWAAQRYGRELRRMSDEFEGSFKGL from human BCL-XL expressed in Escherichia coli measured after 2 hrs by AlphaScreen assay
4
Total Activities
4
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
Discovery of a Novel BCL-X<sub>L</sub> PROTAC Degrader with Enhanced BCL-2 Inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 8.49 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443684 | NAVITOCLAX | 3.0 | 1 | 8.68 |
| CHEMBL5077514 | — | — | 1 | 8.59 |
| CHEMBL5073297 | — | — | 1 | 8.56 |
| CHEMBL5087367 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443684 | NAVITOCLAX | Kd | = | 2.07 | nM | 8.68 |
| CHEMBL5077514 | — | Kd | = | 2.59 | nM | 8.59 |
| CHEMBL5073297 | — | Kd | = | 2.75 | nM | 8.56 |
| CHEMBL5087367 | — | Kd | = | 7.58 | nM | 8.12 |