Assay Detail
Binding
CHEMBL1918878
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Inhibition of HSP90beta in human SKBR3 cells assessed as down regulation of HER2 expression levels after 24 hrs by FACS analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.93 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917878 | — | — | 1 | 7.52 |
| CHEMBL1917729 | — | — | 1 | 6.05 |
| CHEMBL1917727 | — | — | 1 | 5.89 |
| CHEMBL1917728 | — | — | 1 | 5.89 |
| CHEMBL1917726 | — | — | 1 | 4.30 |
| CHEMBL1917724 | — | — | 1 | - |
| CHEMBL1917725 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917878 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1917729 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1917727 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1917728 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1917726 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL1917724 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1917725 | — | IC50 | > | 50000.0 | nM | - |