Assay Detail
Binding
CHEMBL5506671
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Inhibition of C-terminal 6XHis-tagged full length human recombinant HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis
25
Total Activities
25
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
HDAC/NAMPT dual inhibitors overcome initial drug-resistance in p53-null leukemia cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.98 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5083249 | — | — | 1 | 7.82 |
| CHEMBL5087431 | — | — | 1 | 7.77 |
| CHEMBL5078985 | — | — | 1 | 7.73 |
| CHEMBL5561596 | — | — | 1 | 7.71 |
| CHEMBL5532146 | — | — | 1 | 7.42 |
| CHEMBL5561465 | — | — | 1 | 7.31 |
| CHEMBL5559648 | — | — | 1 | 7.29 |
| CHEMBL5556752 | — | — | 1 | 7.22 |
| CHEMBL5565699 | — | — | 1 | 7.10 |
| CHEMBL5555272 | — | — | 1 | 7.08 |
| CHEMBL5558823 | — | — | 1 | 7.05 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.02 |
| CHEMBL5568033 | — | — | 1 | 6.95 |
| CHEMBL5557716 | — | — | 1 | 6.91 |
| CHEMBL5559070 | — | — | 1 | 6.85 |
| CHEMBL5532078 | — | — | 1 | 6.82 |
| CHEMBL5560853 | — | — | 1 | 6.73 |
| CHEMBL5550071 | — | — | 1 | 6.47 |
| CHEMBL5563379 | — | — | 1 | 6.30 |
| CHEMBL5532409 | — | — | 1 | 6.27 |
| CHEMBL5557041 | — | — | 1 | 5.93 |
| CHEMBL5560674 | — | — | 1 | 5.70 |
| CHEMBL5560296 | — | — | 1 | - |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | - |
| CHEMBL5558311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5083249 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5087431 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL5078985 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL5561596 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL5532146 | — | IC50 | = | 37.81 | nM | 7.42 |
| CHEMBL5561465 | — | IC50 | = | 49.2 | nM | 7.31 |
| CHEMBL5559648 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL5556752 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5565699 | — | IC50 | = | 78.7 | nM | 7.10 |
| CHEMBL5555272 | — | IC50 | = | 84.1 | nM | 7.08 |
| CHEMBL5558823 | — | IC50 | = | 88.5 | nM | 7.05 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL5568033 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5557716 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5559070 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5532078 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5560853 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL5550071 | — | IC50 | = | 338.7 | nM | 6.47 |
| CHEMBL5563379 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL5532409 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL5557041 | — | IC50 | = | 1176.0 | nM | 5.93 |
| CHEMBL5560674 | — | IC50 | = | 2002.0 | nM | 5.70 |
| CHEMBL5560296 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL566757 | DAPORINAD | IC50 | > | 10000.0 | nM | - |
| CHEMBL5558311 | — | IC50 | > | 10000.0 | nM | - |