Assay Detail
Binding
CHEMBL5054286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of biotin-tagged MRPEPATIAQELRRIGDEFNA from C-terminal His-tagged human BCL-2 (1` to 211 residues) 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 | 8.90 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443684 | NAVITOCLAX | 3.0 | 1 | 9.19 |
| CHEMBL5077514 | — | — | 1 | 8.91 |
| CHEMBL5073297 | — | — | 1 | 8.83 |
| CHEMBL5087367 | — | — | 1 | 8.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443684 | NAVITOCLAX | Kd | = | 0.65 | nM | 9.19 |
| CHEMBL5077514 | — | Kd | = | 1.22 | nM | 8.91 |
| CHEMBL5073297 | — | Kd | = | 1.47 | nM | 8.83 |
| CHEMBL5087367 | — | Kd | = | 2.25 | nM | 8.65 |