Assay Detail
Binding
CHEMBL4359660
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Binding affinity to wild type human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain (536 to 812 residues) expressed in baculovirus infected sf9 insect cells measured for 1 hr in presence of fluorescein conjugate tracer by competitive fluorescence polarization assay
15
Total Activities
15
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
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 5.59 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449644 | — | — | 1 | 6.46 |
| CHEMBL4525245 | — | — | 1 | 6.43 |
| CHEMBL4440610 | — | — | 1 | 6.36 |
| CHEMBL191003 | JNJ-7706621 | — | 1 | 6.34 |
| CHEMBL4476380 | — | — | 1 | 6.24 |
| CHEMBL4539227 | — | — | 1 | 6.19 |
| CHEMBL4519945 | — | — | 1 | 5.72 |
| CHEMBL573107 | — | — | 1 | 5.70 |
| CHEMBL4437716 | — | — | 1 | 5.40 |
| CHEMBL4475907 | — | — | 1 | 5.33 |
| CHEMBL4560164 | — | — | 1 | 5.16 |
| CHEMBL4453849 | — | — | 1 | 4.91 |
| CHEMBL187345 | — | — | 1 | 4.78 |
| CHEMBL4455581 | — | — | 1 | 4.52 |
| CHEMBL4582077 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449644 | — | Kd | = | 346.0 | nM | 6.46 |
| CHEMBL4525245 | — | Kd | = | 374.0 | nM | 6.43 |
| CHEMBL4440610 | — | Kd | = | 439.0 | nM | 6.36 |
| CHEMBL191003 | JNJ-7706621 | Kd | = | 456.0 | nM | 6.34 |
| CHEMBL4476380 | — | Kd | = | 571.0 | nM | 6.24 |
| CHEMBL4539227 | — | Kd | = | 643.0 | nM | 6.19 |
| CHEMBL4519945 | — | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL573107 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL4437716 | — | Kd | = | 4000.0 | nM | 5.40 |
| CHEMBL4475907 | — | Kd | = | 4700.0 | nM | 5.33 |
| CHEMBL4560164 | — | Kd | = | 7000.0 | nM | 5.16 |
| CHEMBL4453849 | — | Kd | = | 12300.0 | nM | 4.91 |
| CHEMBL187345 | — | Kd | = | 16700.0 | nM | 4.78 |
| CHEMBL4455581 | — | Kd | = | 30500.0 | nM | 4.52 |
| CHEMBL4582077 | — | Kd | = | 47800.0 | nM | 4.32 |