Assay Detail
Binding
CHEMBL3379281
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Inhibition of HSP90 in human MDA-kb2 cells assessed as reduction in glucocorticoid receptor-dependent luciferase expression after 18 hrs by firefly luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-kb2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.00 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3360777 | — | — | 1 | 6.14 |
| CHEMBL3360774 | — | — | 1 | 4.98 |
| CHEMBL389471 | COUMERMYCIN A1 | — | 1 | 4.82 |
| CHEMBL3360770 | — | — | 1 | 4.80 |
| CHEMBL3360775 | — | — | 1 | 4.78 |
| CHEMBL3360767 | — | — | 1 | 4.73 |
| CHEMBL3360769 | — | — | 1 | 4.73 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | - |
| CHEMBL278315 | GELDANAMYCIN | 2.0 | 1 | - |
| CHEMBL3360762 | — | — | 1 | - |
| CHEMBL3360771 | — | — | 1 | - |
| CHEMBL3360772 | — | — | 1 | - |
| CHEMBL3360773 | — | — | 1 | - |
| CHEMBL3360776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3360777 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3360774 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL389471 | COUMERMYCIN A1 | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL3360770 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL3360775 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL3360767 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL3360769 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 231000.0 | nM | - |
| CHEMBL278315 | GELDANAMYCIN | IC50 | < | 10.0 | nM | - |
| CHEMBL3360762 | — | IC50 | > | 160000.0 | nM | - |
| CHEMBL3360771 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL3360772 | — | IC50 | > | 67000.0 | nM | - |
| CHEMBL3360773 | — | IC50 | = | 121000.0 | nM | - |
| CHEMBL3360776 | — | IC50 | > | 27000.0 | nM | - |