Assay Detail
Binding
CHEMBL5136187
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Binding affinity to JAK2 JH2 V617F mutant (unknown origin) expressed in baculovirus infected Sf9 cells assessed as dissociation constant measured upto 30 mins in presence of tracer by competitive fluorescence polarization assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 7.09 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191140 | — | — | 1 | 7.48 |
| CHEMBL5192135 | — | — | 1 | 7.37 |
| CHEMBL5184259 | — | — | 1 | 7.30 |
| CHEMBL5196073 | — | — | 1 | 7.21 |
| CHEMBL5176386 | — | — | 1 | 6.88 |
| CHEMBL4449644 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191140 | — | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL5192135 | — | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL5184259 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL5196073 | — | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL5176386 | — | Kd | = | 131.0 | nM | 6.88 |
| CHEMBL4449644 | — | Kd | = | 478.0 | nM | 6.32 |