Assay Detail
Binding
CHEMBL5611201
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Inhibition of C-terminal 6His/FLAG tagged full length human recombinant HDAC1 (1 to 482 residues) extracted from Sf9 cells using Z-Lys(Ac)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by fluorescence based microplate reader analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with <i>In Vitro</i> and <i>In Vivo</i> Activity in Neurodegenerative Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.65 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5614364 | — | — | 1 | 7.06 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.00 |
| CHEMBL5612956 | — | — | 1 | 6.95 |
| CHEMBL5613964 | — | — | 1 | 6.86 |
| CHEMBL5612700 | — | — | 1 | 6.85 |
| CHEMBL5614345 | — | — | 1 | 6.61 |
| CHEMBL5613087 | — | — | 1 | 6.38 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.50 |
| CHEMBL5613368 | — | — | 1 | - |
| CHEMBL4173258 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5614364 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5612956 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5613964 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5612700 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5614345 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL5613087 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL5613368 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4173258 | — | IC50 | > | 10000.0 | nM | - |