Assay Detail
Functional
CHEMBL828486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of yeast Hsp90 ATPase activity
21
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Saccharomyces cerevisiae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
ATP-dependent molecular chaperone HSP82 (CHEMBL3536) ↗| Type | SINGLE PROTEIN |
| Organism | Saccharomyces cerevisiae S288c |
Publication
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.15 | 5.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361941 | — | — | 1 | 5.81 |
| CHEMBL191228 | — | — | 1 | 5.80 |
| CHEMBL364882 | — | — | 1 | 5.78 |
| CHEMBL190249 | — | — | 1 | 5.62 |
| CHEMBL188495 | — | — | 1 | 5.62 |
| CHEMBL278315 | GELDANAMYCIN | 2.0 | 2 | 5.32 |
| CHEMBL109480 | TANESPIMYCIN | 3.0 | 2 | 5.18 |
| CHEMBL399530 | — | — | 2 | 5.15 |
| CHEMBL189078 | — | — | 1 | 4.89 |
| CHEMBL187674 | — | — | 1 | 4.65 |
| CHEMBL187678 | — | — | 1 | 4.59 |
| CHEMBL190919 | — | — | 1 | 4.34 |
| CHEMBL188965 | — | — | 1 | 4.22 |
| CHEMBL187408 | — | — | 1 | - |
| CHEMBL191074 | — | — | 1 | - |
| CHEMBL362576 | — | — | 1 | - |
| CHEMBL187670 | — | — | 1 | - |
| CHEMBL188773 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361941 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL191228 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL364882 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL190249 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL188495 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL278315 | GELDANAMYCIN | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL278315 | GELDANAMYCIN | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL109480 | TANESPIMYCIN | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL399530 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL109480 | TANESPIMYCIN | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL399530 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL189078 | — | IC50 | = | 12850.0 | nM | 4.89 |
| CHEMBL187674 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL187678 | — | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL190919 | — | IC50 | = | 46100.0 | nM | 4.34 |
| CHEMBL188965 | — | IC50 | = | 60800.0 | nM | 4.22 |
| CHEMBL191074 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL188773 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL187408 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL362576 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL187670 | — | IC50 | > | 100000.0 | nM | - |