Assay Detail
Binding
CHEMBL3877344
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Inhibition of JAK2 (unknown origin) preincubated for 20 mins followed by [33P]ATP addition measured after 120 mins by Hotspot assay
16
Total Activities
16
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 Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.43 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3961053 | — | — | 1 | 9.01 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 9.00 |
| CHEMBL3924682 | — | — | 1 | 8.90 |
| CHEMBL3917405 | — | — | 1 | 8.85 |
| CHEMBL3915689 | — | — | 1 | 8.77 |
| CHEMBL3964125 | — | — | 1 | 8.64 |
| CHEMBL3980203 | — | — | 1 | 8.61 |
| CHEMBL3920872 | — | — | 1 | 8.59 |
| CHEMBL3951291 | — | — | 1 | 8.37 |
| CHEMBL3942555 | — | — | 1 | 8.33 |
| CHEMBL3945293 | — | — | 1 | 8.30 |
| CHEMBL3933593 | — | — | 1 | 8.16 |
| CHEMBL3952364 | — | — | 1 | 8.05 |
| CHEMBL3972157 | — | — | 1 | 7.52 |
| CHEMBL3981879 | — | — | 1 | 7.33 |
| CHEMBL3954183 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3961053 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL2035187 | PACRITINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3924682 | — | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL3917405 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3915689 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL3964125 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL3980203 | — | IC50 | = | 2.45 | nM | 8.61 |
| CHEMBL3920872 | — | IC50 | = | 2.57 | nM | 8.59 |
| CHEMBL3951291 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3942555 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3945293 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3933593 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3952364 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3972157 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3981879 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3954183 | — | IC50 | < | 39.0 | nM | - |