Assay Detail
Binding
CHEMBL4610789
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay
9
Total Activities
9
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 boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.47 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.84 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 6.27 |
| CHEMBL4642642 | — | — | 1 | 6.18 |
| CHEMBL4640647 | — | — | 1 | 6.05 |
| CHEMBL4648837 | — | — | 1 | 6.01 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | - |
| CHEMBL4649397 | — | — | 1 | - |
| CHEMBL4645290 | — | — | 1 | - |
| CHEMBL4648104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 533.7 | nM | 6.27 |
| CHEMBL4642642 | — | IC50 | = | 657.9 | nM | 6.18 |
| CHEMBL4640647 | — | IC50 | = | 891.5 | nM | 6.05 |
| CHEMBL4648837 | — | IC50 | = | 971.6 | nM | 6.01 |
| CHEMBL1873475 | IBRUTINIB | IC50 | > | 1000.0 | nM | - |
| CHEMBL4649397 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4645290 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4648104 | — | IC50 | > | 1000.0 | nM | - |