Assay Detail
Binding
CHEMBL3888199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
HDAC inhibitors and therapeutic methods using the same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.98 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3927240 | — | — | 1 | 6.76 |
| CHEMBL3944582 | — | — | 1 | 6.76 |
| CHEMBL3973046 | — | — | 1 | 6.49 |
| CHEMBL3948680 | — | — | 1 | 6.49 |
| CHEMBL3951328 | — | — | 1 | 6.40 |
| CHEMBL3893799 | — | — | 1 | 6.40 |
| CHEMBL3902014 | — | — | 1 | 6.38 |
| CHEMBL3907295 | — | — | 1 | 6.38 |
| CHEMBL3923615 | — | — | 1 | 6.38 |
| CHEMBL3958794 | — | — | 1 | 6.38 |
| CHEMBL356769 | TUBACIN | — | 1 | 6.07 |
| CHEMBL3910971 | — | — | 1 | 6.04 |
| CHEMBL3979548 | — | — | 1 | 6.04 |
| CHEMBL3918458 | — | — | 1 | 5.92 |
| CHEMBL3921742 | — | — | 1 | 5.92 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.90 |
| CHEMBL3940062 | — | — | 1 | 5.74 |
| CHEMBL3938052 | — | — | 1 | 5.74 |
| CHEMBL3953441 | — | — | 1 | 5.72 |
| CHEMBL3899275 | — | — | 1 | 5.72 |
| CHEMBL3908319 | — | — | 1 | 5.62 |
| CHEMBL3922129 | — | — | 1 | 5.62 |
| CHEMBL4107832 | — | — | 1 | 5.25 |
| CHEMBL4109326 | — | — | 1 | 5.25 |
| CHEMBL3893169 | — | — | 1 | 5.03 |
| CHEMBL3893905 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3927240 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3944582 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3973046 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL3948680 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL3951328 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL3893799 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL3902014 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL3907295 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL3923615 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL3958794 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL356769 | TUBACIN | IC50 | = | 854.0 | nM | 6.07 |
| CHEMBL3910971 | — | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL3979548 | — | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL3918458 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3921742 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL3940062 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL3938052 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL3953441 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL3899275 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL3908319 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL3922129 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL4107832 | — | IC50 | = | 5590.0 | nM | 5.25 |
| CHEMBL4109326 | — | IC50 | = | 5590.0 | nM | 5.25 |
| CHEMBL3893169 | — | IC50 | = | 9430.0 | nM | 5.03 |
| CHEMBL3893905 | — | IC50 | = | 9430.0 | nM | 5.03 |