Assay Detail
Binding
CHEMBL3828935
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay
39
Total Activities
39
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
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 8.40 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828518 | — | — | 1 | 9.35 |
| CHEMBL3828636 | — | — | 1 | 9.31 |
| CHEMBL3828492 | — | — | 1 | 9.26 |
| CHEMBL3827517 | — | — | 1 | 9.26 |
| CHEMBL3827814 | — | — | 1 | 9.19 |
| CHEMBL3827296 | — | — | 1 | 9.09 |
| CHEMBL3827865 | — | — | 1 | 9.07 |
| CHEMBL3828180 | — | — | 1 | 9.01 |
| CHEMBL3827281 | — | — | 1 | 9.00 |
| CHEMBL3828408 | — | — | 1 | 9.00 |
| CHEMBL3827650 | — | — | 1 | 9.00 |
| CHEMBL3827738 | — | — | 1 | 9.00 |
| CHEMBL3827794 | — | — | 1 | 8.99 |
| CHEMBL3827894 | — | — | 1 | 8.98 |
| CHEMBL3826997 | — | — | 1 | 8.96 |
| CHEMBL3828747 | — | — | 1 | 8.96 |
| CHEMBL3827660 | — | — | 1 | 8.96 |
| CHEMBL3827004 | — | — | 1 | 8.94 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 8.90 |
| CHEMBL3827612 | — | — | 1 | 8.86 |
| CHEMBL3828628 | — | — | 1 | 8.80 |
| CHEMBL3827317 | — | — | 1 | 8.80 |
| CHEMBL3828289 | — | — | 1 | 8.80 |
| CHEMBL3827780 | — | — | 1 | 8.70 |
| CHEMBL3828482 | — | — | 1 | 8.58 |
| CHEMBL3828486 | — | — | 1 | 8.29 |
| CHEMBL3827489 | — | — | 1 | 8.21 |
| CHEMBL3827398 | — | — | 1 | 8.00 |
| CHEMBL3828070 | — | — | 1 | 8.00 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828518 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL3828636 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3827517 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL3828492 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL3827814 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL3827296 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL3827865 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL3828180 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL3827738 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3827650 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3828408 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL3827281 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3827794 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL3827894 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL3827660 | — | IC50 | = | 1.11 | nM | 8.96 |
| CHEMBL3826997 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3828747 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3827004 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL3827612 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL3827317 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3828289 | — | IC50 | = | 1.59 | nM | 8.80 |
| CHEMBL3828628 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3827780 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL3828482 | — | IC50 | = | 2.62 | nM | 8.58 |
| CHEMBL3828486 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3827489 | — | IC50 | = | 6.15 | nM | 8.21 |
| CHEMBL3827398 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3828070 | — | IC50 | = | 10.01 | nM | 8.00 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3827056 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL3828337 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3828188 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3827477 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3828135 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3827881 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3828218 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3827548 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3828164 | — | IC50 | = | 300.0 | nM | 6.52 |