Assay Detail
Binding
CHEMBL4268222
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Inhibition of HDAC1 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate preincubated with enzyme followed by substrate addition for 2 hrs and measured for 1.5 hrs at 15 mins time interval by fluorescence assay
23
Total Activities
23
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
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.61 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4278951 | — | — | 1 | 8.42 |
| CHEMBL4282456 | — | — | 1 | 7.49 |
| CHEMBL4286867 | — | — | 1 | 7.25 |
| CHEMBL4292408 | — | — | 1 | 7.11 |
| CHEMBL4294153 | — | — | 1 | 7.08 |
| CHEMBL4290748 | — | — | 1 | 7.05 |
| CHEMBL4289006 | — | — | 1 | 6.86 |
| CHEMBL4283513 | — | — | 1 | 6.85 |
| CHEMBL4283921 | — | — | 1 | 6.84 |
| CHEMBL4295224 | — | — | 1 | 6.81 |
| CHEMBL4277267 | — | — | 1 | 6.75 |
| CHEMBL4280050 | — | — | 1 | 6.58 |
| CHEMBL4281785 | — | — | 1 | 6.54 |
| CHEMBL4294092 | — | — | 1 | 6.46 |
| CHEMBL4284388 | — | — | 1 | 6.42 |
| CHEMBL4280540 | — | — | 1 | 6.20 |
| CHEMBL4290831 | — | — | 1 | 6.11 |
| CHEMBL4285223 | — | — | 1 | 6.03 |
| CHEMBL4278591 | — | — | 1 | 5.98 |
| CHEMBL4291781 | — | — | 1 | 5.77 |
| CHEMBL4282471 | — | — | 1 | 5.47 |
| CHEMBL4290689 | — | — | 1 | 5.34 |
| CHEMBL4282877 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4278951 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4282456 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL4286867 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4292408 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4294153 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4290748 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4289006 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4283513 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4283921 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4295224 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4277267 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4280050 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4281785 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL4294092 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4284388 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL4280540 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL4290831 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL4285223 | — | IC50 | = | 934.0 | nM | 6.03 |
| CHEMBL4278591 | — | IC50 | = | 1043.0 | nM | 5.98 |
| CHEMBL4291781 | — | IC50 | = | 1701.0 | nM | 5.77 |
| CHEMBL4282471 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL4290689 | — | IC50 | = | 4581.0 | nM | 5.34 |
| CHEMBL4282877 | — | IC50 | > | 10000.0 | nM | - |