Assay Detail
Binding
CHEMBL4268221
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Inhibition of human JAK2 using poly(Glu:Tyr)(4:1) as substrate preincubated for 20 mins followed by [gamma33P]ATP addition measured after 120 mins by ion exchange filter paper method
29
Total Activities
29
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 | 29 | 7.92 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290831 | — | — | 1 | 9.05 |
| CHEMBL4281785 | — | — | 1 | 8.74 |
| CHEMBL4284388 | — | — | 1 | 8.59 |
| CHEMBL4279986 | — | — | 1 | 8.54 |
| CHEMBL4290689 | — | — | 1 | 8.53 |
| CHEMBL4286867 | — | — | 1 | 8.51 |
| CHEMBL4280540 | — | — | 1 | 8.47 |
| CHEMBL4294153 | — | — | 1 | 8.44 |
| CHEMBL4295224 | — | — | 1 | 8.41 |
| CHEMBL4289006 | — | — | 1 | 8.37 |
| CHEMBL4292408 | — | — | 1 | 8.34 |
| CHEMBL4277267 | — | — | 1 | 8.18 |
| CHEMBL4290297 | — | — | 1 | 8.10 |
| CHEMBL4282456 | — | — | 1 | 8.04 |
| CHEMBL2208024 | — | — | 1 | 7.86 |
| CHEMBL4278591 | — | — | 1 | 7.77 |
| CHEMBL4285223 | — | — | 1 | 7.75 |
| CHEMBL2208025 | — | — | 1 | 7.71 |
| CHEMBL4283921 | — | — | 1 | 7.64 |
| CHEMBL4280050 | — | — | 1 | 7.59 |
| CHEMBL2208023 | — | — | 1 | 7.56 |
| CHEMBL2208028 | — | — | 1 | 7.54 |
| CHEMBL4290748 | — | — | 1 | 7.48 |
| CHEMBL4278951 | — | — | 1 | 7.38 |
| CHEMBL4291781 | — | — | 1 | 7.34 |
| CHEMBL4282471 | — | — | 1 | 7.23 |
| CHEMBL4283513 | — | — | 1 | 7.02 |
| CHEMBL4294092 | — | — | 1 | 6.96 |
| CHEMBL4282877 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290831 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4281785 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4284388 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4279986 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4290689 | — | IC50 | = | 2.93 | nM | 8.53 |
| CHEMBL4286867 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4280540 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4294153 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4295224 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4289006 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4292408 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4277267 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4290297 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4282456 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL2208024 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4278591 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4285223 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2208025 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL4283921 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4280050 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL2208023 | — | IC50 | = | 27.4 | nM | 7.56 |
| CHEMBL2208028 | — | IC50 | = | 28.7 | nM | 7.54 |
| CHEMBL4290748 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4278951 | — | IC50 | = | 41.3 | nM | 7.38 |
| CHEMBL4291781 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4282471 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL4283513 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL4294092 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4282877 | — | IC50 | = | 239.0 | nM | 6.62 |