Assay Detail
Binding
CHEMBL5588474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant HDAC1 using Ac-Lys-Tyr-Lys(eta-acetyl)-AMC as substrate incubated for 24 hrs by fluorescence based Envision plate reader analysis
35
Total Activities
35
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 | 35 | 6.10 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598116 | — | — | 1 | 7.28 |
| CHEMBL5596602 | — | — | 1 | 6.96 |
| CHEMBL5598317 | — | — | 1 | 6.88 |
| CHEMBL5597266 | — | — | 1 | 6.77 |
| CHEMBL5597881 | — | — | 1 | 6.46 |
| CHEMBL5597396 | — | — | 1 | 6.38 |
| CHEMBL5597605 | — | — | 1 | 6.32 |
| CHEMBL5598390 | — | — | 1 | 6.29 |
| CHEMBL5598338 | — | — | 1 | 6.28 |
| CHEMBL5596479 | — | — | 1 | 6.26 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.26 |
| CHEMBL5598168 | — | — | 1 | 6.25 |
| CHEMBL5597417 | — | — | 1 | 6.17 |
| CHEMBL5597636 | — | — | 1 | 6.14 |
| CHEMBL5589771 | — | — | 1 | 6.05 |
| CHEMBL5598071 | — | — | 1 | 6.03 |
| CHEMBL5597381 | — | — | 1 | 6.01 |
| CHEMBL5598054 | — | — | 1 | 6.01 |
| CHEMBL5598550 | — | — | 1 | 5.94 |
| CHEMBL5597651 | — | — | 1 | 5.93 |
| CHEMBL5596683 | — | — | 1 | 5.92 |
| CHEMBL5589751 | — | — | 1 | 5.83 |
| CHEMBL5596740 | — | — | 1 | 5.82 |
| CHEMBL5598531 | — | — | 1 | 5.78 |
| CHEMBL5598107 | — | — | 1 | 5.77 |
| CHEMBL5598136 | — | — | 1 | 5.76 |
| CHEMBL5596717 | — | — | 1 | 5.71 |
| CHEMBL5598502 | — | — | 1 | 5.59 |
| CHEMBL5597702 | — | — | 1 | 5.54 |
| CHEMBL5597775 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598116 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL5596602 | — | IC50 | = | 108.3 | nM | 6.96 |
| CHEMBL5598317 | — | IC50 | = | 133.5 | nM | 6.88 |
| CHEMBL5597266 | — | IC50 | = | 168.9 | nM | 6.77 |
| CHEMBL5597881 | — | IC50 | = | 346.9 | nM | 6.46 |
| CHEMBL5597396 | — | IC50 | = | 418.2 | nM | 6.38 |
| CHEMBL5597605 | — | IC50 | = | 483.5 | nM | 6.32 |
| CHEMBL5598390 | — | IC50 | = | 517.6 | nM | 6.29 |
| CHEMBL5598338 | — | IC50 | = | 530.6 | nM | 6.28 |
| CHEMBL5596479 | — | IC50 | = | 548.2 | nM | 6.26 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 542.8 | nM | 6.26 |
| CHEMBL5598168 | — | IC50 | = | 557.7 | nM | 6.25 |
| CHEMBL5597417 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL5597636 | — | IC50 | = | 727.7 | nM | 6.14 |
| CHEMBL5589771 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL5598071 | — | IC50 | = | 945.1 | nM | 6.03 |
| CHEMBL5598054 | — | IC50 | = | 981.0 | nM | 6.01 |
| CHEMBL5597381 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL5598550 | — | IC50 | = | 1152.0 | nM | 5.94 |
| CHEMBL5597651 | — | IC50 | = | 1187.0 | nM | 5.93 |
| CHEMBL5596683 | — | IC50 | = | 1206.0 | nM | 5.92 |
| CHEMBL5589751 | — | IC50 | = | 1494.0 | nM | 5.83 |
| CHEMBL5596740 | — | IC50 | = | 1502.0 | nM | 5.82 |
| CHEMBL5598531 | — | IC50 | = | 1664.0 | nM | 5.78 |
| CHEMBL5598107 | — | IC50 | = | 1704.0 | nM | 5.77 |
| CHEMBL5598136 | — | IC50 | = | 1722.0 | nM | 5.76 |
| CHEMBL5596717 | — | IC50 | = | 1932.0 | nM | 5.71 |
| CHEMBL5598502 | — | IC50 | = | 2562.0 | nM | 5.59 |
| CHEMBL5597702 | — | IC50 | = | 2891.0 | nM | 5.54 |
| CHEMBL5597775 | — | IC50 | = | 4880.0 | nM | 5.31 |
| CHEMBL5597574 | — | IC50 | = | 4999.0 | nM | 5.30 |
| CHEMBL3656841 | — | IC50 | - | — | - | |
| CHEMBL5596044 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5596921 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5596733 | — | IC50 | > | 10000.0 | nM | - |