Assay Detail
Binding
CHEMBL4768535
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Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in sf9 insect cells using Boc-Lys(TFA)-AM as substrate incubated for 60 mins by fluorescence assay
23
Total Activities
23
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
Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.05 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4786031 | — | — | 1 | 8.62 |
| CHEMBL4790137 | — | — | 1 | 8.52 |
| CHEMBL4793650 | — | — | 1 | 8.49 |
| CHEMBL4777182 | — | — | 1 | 8.48 |
| CHEMBL4786350 | — | — | 1 | 8.48 |
| CHEMBL4776328 | — | — | 1 | 8.47 |
| CHEMBL4788954 | — | — | 1 | 8.44 |
| CHEMBL4792980 | — | — | 1 | 8.42 |
| CHEMBL4792567 | — | — | 1 | 8.40 |
| CHEMBL4782066 | — | — | 1 | 8.39 |
| CHEMBL4786063 | — | — | 1 | 8.38 |
| CHEMBL4776974 | — | — | 1 | 8.36 |
| CHEMBL4788942 | — | — | 1 | 8.36 |
| CHEMBL4782988 | — | — | 1 | 8.35 |
| CHEMBL4799886 | — | — | 1 | 8.31 |
| CHEMBL4776599 | — | — | 1 | 8.14 |
| CHEMBL4782327 | — | — | 1 | 7.90 |
| CHEMBL4792025 | — | — | 1 | 7.61 |
| CHEMBL4792705 | — | — | 1 | 7.49 |
| CHEMBL4797623 | — | — | 1 | 7.39 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.36 |
| CHEMBL4779831 | — | — | 1 | 7.27 |
| CHEMBL4784481 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4786031 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4790137 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4793650 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4777182 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4786350 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4776328 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4788954 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4792980 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4792567 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4782066 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4786063 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4776974 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4788942 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4782988 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4799886 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4776599 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4782327 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4792025 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL4792705 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL4797623 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4779831 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4784481 | — | IC50 | = | 3340.0 | nM | 5.48 |