Assay Detail
Binding
CHEMBL3242260
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Inhibition of HSP90 in HEK cells expressing full-length mHtt Q73 gene assessed as reduction of mHtt level after 24 hrs by Western blot analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.62 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3235355 | — | — | 1 | 7.72 |
| CHEMBL3235353 | — | — | 1 | 7.62 |
| CHEMBL3235354 | — | — | 1 | 7.44 |
| CHEMBL3235345 | — | — | 1 | 7.14 |
| CHEMBL3235361 | — | — | 1 | 7.10 |
| CHEMBL3235362 | — | — | 1 | 7.09 |
| CHEMBL3235338 | — | — | 1 | 7.05 |
| CHEMBL3235335 | — | — | 1 | 6.96 |
| CHEMBL3235334 | — | — | 1 | 6.92 |
| CHEMBL3235333 | — | — | 1 | 6.92 |
| CHEMBL3235343 | — | — | 1 | 6.85 |
| CHEMBL3235350 | — | — | 1 | 6.84 |
| CHEMBL3235339 | — | — | 1 | 6.72 |
| CHEMBL3235336 | — | — | 1 | 6.72 |
| CHEMBL3235356 | — | — | 1 | 6.71 |
| CHEMBL3235341 | — | — | 1 | 6.66 |
| CHEMBL3235352 | — | — | 1 | 6.65 |
| CHEMBL3235360 | — | — | 1 | 6.64 |
| CHEMBL3235363 | — | — | 1 | 6.55 |
| CHEMBL3235340 | — | — | 1 | 6.38 |
| CHEMBL3235342 | — | — | 1 | 6.35 |
| CHEMBL3235359 | — | — | 1 | 6.32 |
| CHEMBL3235351 | — | — | 1 | 6.28 |
| CHEMBL3235337 | — | — | 1 | 6.14 |
| CHEMBL3235344 | — | — | 1 | 6.03 |
| CHEMBL3235357 | — | — | 1 | 6.00 |
| CHEMBL3235358 | — | — | 1 | 5.77 |
| CHEMBL3235349 | — | — | 1 | 5.44 |
| CHEMBL3235347 | — | — | 1 | 5.07 |
| CHEMBL3235348 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3235355 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3235353 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3235354 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3235345 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3235361 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3235362 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3235338 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3235335 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3235334 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3235333 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3235343 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3235350 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL3235339 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3235336 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3235356 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3235341 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3235352 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3235360 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3235363 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3235340 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3235342 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3235359 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3235351 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3235337 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3235344 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3235357 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3235358 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3235349 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3235347 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL3235348 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3235346 | — | IC50 | > | 10000.0 | nM | - |