Assay Detail
Binding
CHEMBL984452
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Inhibition of Hsp90 in human SKBR3 cells assessed as interaction with Cy3b-conjugated geldanamycin by FP assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.18 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL515000 | — | — | 1 | 6.26 |
| CHEMBL371915 | — | — | 1 | 6.16 |
| CHEMBL478665 | — | — | 1 | 5.89 |
| CHEMBL476157 | — | — | 1 | 5.77 |
| CHEMBL478879 | — | — | 1 | 5.75 |
| CHEMBL478664 | — | — | 1 | 5.60 |
| CHEMBL476359 | — | — | 1 | 5.36 |
| CHEMBL444355 | — | — | 1 | 5.35 |
| CHEMBL477824 | — | — | 1 | 5.03 |
| CHEMBL477825 | — | — | 1 | 5.02 |
| CHEMBL476368 | — | — | 1 | 4.84 |
| CHEMBL476574 | — | — | 1 | 4.71 |
| CHEMBL478890 | — | — | 1 | 4.71 |
| CHEMBL514704 | — | — | 1 | 4.60 |
| CHEMBL490783 | — | — | 1 | 4.58 |
| CHEMBL489767 | — | — | 1 | 4.57 |
| CHEMBL478891 | — | — | 1 | 4.55 |
| CHEMBL476369 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL515000 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL371915 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL478665 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL476157 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL478879 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL478664 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL476359 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL444355 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL477824 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL477825 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL476368 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL476574 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL478890 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL514704 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL490783 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL489767 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL478891 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL476369 | — | IC50 | = | 31300.0 | nM | 4.50 |