Assay Detail
Binding
CHEMBL5588481
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Inhibition of human recombinant HDAC4 using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate incubated for 24 hrs by fluorescence based Envision plate reader analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.64 | 5.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598054 | — | — | 1 | 5.97 |
| CHEMBL5598531 | — | — | 1 | 5.60 |
| CHEMBL5598550 | — | — | 1 | 5.36 |
| CHEMBL5597574 | — | — | 1 | - |
| CHEMBL5597266 | — | — | 1 | - |
| CHEMBL5597651 | — | — | 1 | - |
| CHEMBL5597702 | — | — | 1 | - |
| CHEMBL5597605 | — | — | 1 | - |
| CHEMBL5596044 | — | — | 1 | - |
| CHEMBL5598317 | — | — | 1 | - |
| CHEMBL5597396 | — | — | 1 | - |
| CHEMBL5597881 | — | — | 1 | - |
| CHEMBL5597417 | — | — | 1 | - |
| CHEMBL5598116 | — | — | 1 | - |
| CHEMBL5596602 | — | — | 1 | - |
| CHEMBL5598338 | — | — | 1 | - |
| CHEMBL3656841 | — | — | 1 | - |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598054 | — | IC50 | = | 1075.5 | nM | 5.97 |
| CHEMBL5598531 | — | IC50 | = | 2495.5 | nM | 5.60 |
| CHEMBL5598550 | — | IC50 | = | 4397.0 | nM | 5.36 |
| CHEMBL5597574 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5597266 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5597651 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597702 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597605 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5596044 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5598317 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597396 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597881 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5597417 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5598116 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5596602 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5598338 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3656841 | — | IC50 | - | — | - | |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - |