Assay Detail
Binding
CHEMBL4359667
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Inhibition of full length human C-terminal FLAG-tagged JAK2 V617F mutant (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 2 | 4.48 | 4.96 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191003 | JNJ-7706621 | — | 2 | 4.96 |
| CHEMBL4476380 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191003 | JNJ-7706621 | IC50 | = | 11050.0 | nM | 4.96 |
| CHEMBL4476380 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL191003 | JNJ-7706621 | Inhibition | - | % | - |