Assay Detail
Binding
CHEMBL5373316
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Inhibition of HDAC6 in human BEAS-2B cells assessed as deacetylation of acetylated alpha-tubulin level incubated for 24 hrs by Western blot analysis
20
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BEAS-2B |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.37 | 7.70 |
| IC50 | 2 | 7.35 | 8.00 |
| pEC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5435916 | — | — | 1 | 8.00 |
| CHEMBL4440341 | — | — | 1 | 7.70 |
| CHEMBL5410192 | — | — | 1 | 7.20 |
| CHEMBL3935992 | — | — | 1 | 7.10 |
| CHEMBL5438547 | — | — | 1 | 6.70 |
| CHEMBL5429808 | — | — | 1 | 6.60 |
| CHEMBL5408305 | — | — | 1 | 6.50 |
| CHEMBL5425061 | — | — | 1 | 6.50 |
| CHEMBL5408594 | — | — | 1 | 6.50 |
| CHEMBL5440081 | — | — | 1 | 6.40 |
| CHEMBL5425437 | — | — | 1 | 6.30 |
| CHEMBL5421243 | — | — | 1 | 6.20 |
| CHEMBL5440297 | — | — | 1 | 6.20 |
| CHEMBL5429654 | — | — | 1 | 6.00 |
| CHEMBL5403250 | — | — | 1 | 5.90 |
| CHEMBL5434758 | — | — | 1 | 5.80 |
| CHEMBL5417383 | — | — | 1 | 5.50 |
| CHEMBL5411782 | — | — | 1 | 5.50 |
| CHEMBL5429543 | — | — | 1 | - |
| CHEMBL5403435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5435916 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4440341 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5410192 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3935992 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5438547 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5429808 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL5408305 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5425061 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5408594 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5440081 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5425437 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL5421243 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5440297 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5429654 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5403250 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL5434758 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL5417383 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5411782 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5429543 | — | pEC50 | - | — | - | |
| CHEMBL5403435 | — | EC50 | > | 10000.0 | nM | - |