Assay Detail
Binding
CHEMBL5739017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Histone Deacetylase Enzymatic Activity Assay: HDAC3: The following trypsin-coupled protocol and Caliper protocol described Herein was used to assay the compounds of the invention. HDAC3-Kinetic IC50 3Hr PreIncubation. Working Stocks: 1xHDAC Assay Buffer: 50 mM HEPES (GIBCO 15630-114), 100mM KCl, 0.001% Tween-20 (Zymed 00-3005), -0.05% BSA (Invitrogen, P2489), pH 7.4, 1.5xHDAC: 0.1 ug/ml HDAC3 (BPS Inc) in assay buffer 3x Substrate+3x Trpsin: 28.5 uM Substrate + 450nM Trpsin in assay buffer 300x Trypsin stock is made up in HDAC Assay Buffer, aliquoted and stored at -802C. BPS Enzyme and Substrate amounts (per well).
516
Total Activities
171
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibitors of histone deacetylase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 172 | 5.17 | 6.26 |
| kon | 172 | - | - |
| k_off | 172 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5814768 | — | — | 3 | 6.26 |
| CHEMBL5981441 | — | — | 3 | 6.26 |
| CHEMBL5913418 | — | — | 3 | 6.26 |
| CHEMBL5847851 | — | — | 3 | 6.26 |
| CHEMBL5850813 | — | — | 3 | 6.26 |
| CHEMBL5896877 | — | — | 3 | 6.26 |
| CHEMBL5848875 | — | — | 3 | 6.26 |
| CHEMBL6027603 | — | — | 3 | 6.26 |
| CHEMBL5176393 | — | — | 3 | 5.52 |
| CHEMBL3828396 | — | — | 3 | 5.52 |
| CHEMBL5989744 | — | — | 3 | 5.52 |
| CHEMBL5755237 | — | — | 3 | 5.52 |
| CHEMBL6025201 | — | — | 3 | 5.52 |
| CHEMBL5876772 | — | — | 3 | 5.52 |
| CHEMBL5933518 | — | — | 3 | 5.52 |
| CHEMBL5754429 | — | — | 3 | 5.52 |
| CHEMBL5974061 | — | — | 3 | 5.52 |
| CHEMBL5812090 | — | — | 3 | 5.52 |
| CHEMBL5892854 | — | — | 3 | 5.52 |
| CHEMBL5962972 | — | — | 3 | 5.52 |
| CHEMBL5900933 | — | — | 3 | 5.52 |
| CHEMBL5784501 | — | — | 3 | 5.52 |
| CHEMBL5897740 | — | — | 3 | 5.52 |
| CHEMBL5971852 | — | — | 3 | 5.52 |
| CHEMBL6029999 | — | — | 3 | 5.52 |
| CHEMBL6002677 | — | — | 3 | 5.52 |
| CHEMBL5796634 | — | — | 3 | 5.52 |
| CHEMBL6001399 | — | — | 3 | 5.52 |
| CHEMBL5873964 | — | — | 3 | 5.52 |
| CHEMBL5929946 | — | — | 3 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5847851 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5850813 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5896877 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL6027603 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5814768 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5913418 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5848875 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5981441 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL5817463 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5962972 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5971959 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6025201 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5902890 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5784501 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5874378 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5900933 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5837624 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5856390 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6002677 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5876772 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL3828396 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5979351 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5925056 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6001399 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5754429 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5796634 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6029999 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5978579 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5974061 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5906784 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5897740 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5989744 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5916619 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6064722 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5755237 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5793327 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5757591 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5860094 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5866801 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6049685 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5983339 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5944351 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5741285 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6013755 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5923575 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5809219 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5176393 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5928087 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL5857161 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL6015573 | — | IC50 | = | 3050.0 | nM | 5.52 |