Assay Detail
Binding
CHEMBL5628519
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Inhibition of 6His-tagged human HSP90alpha N-terminal domain (1 to 223 residues) expressed in Escherichia coli BL21 DE3 cells incubated for 24 hrs by fluorescence polarization 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 X10g as a selective PROTAC degrader of Hsp90α protein for treating breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.54 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1254575 | — | — | 1 | 6.39 |
| CHEMBL5633917 | — | — | 1 | 5.49 |
| CHEMBL1215467 | — | — | 1 | 5.26 |
| CHEMBL4474770 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1254575 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5633917 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL1215467 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4474770 | — | IC50 | = | 9550.0 | nM | 5.02 |