Assay Detail
Functional
CHEMBL867913
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Upregulation of Hsp70 in SKBR3 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.28 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | 2.0 | 1 | 8.40 |
| CHEMBL339231 | — | — | 1 | 7.77 |
| CHEMBL109480 | TANESPIMYCIN | 3.0 | 1 | 7.66 |
| CHEMBL377559 | RETASPIMYCIN HYDROCHLORIDE | 3.0 | 1 | 7.66 |
| CHEMBL209356 | — | — | 1 | 7.24 |
| CHEMBL211295 | — | — | 1 | 6.99 |
| CHEMBL211296 | — | — | 1 | 6.85 |
| CHEMBL378936 | — | — | 1 | 6.51 |
| CHEMBL378935 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL339231 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL109480 | TANESPIMYCIN | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL377559 | RETASPIMYCIN HYDROCHLORIDE | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL209356 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL211295 | — | EC50 | = | 102.0 | nM | 6.99 |
| CHEMBL211296 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL378936 | — | EC50 | = | 311.0 | nM | 6.51 |
| CHEMBL378935 | — | EC50 | = | 384.0 | nM | 6.42 |