Assay Detail
Binding
CHEMBL4332969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 1 mM ATP by HTRF assay
35
Total Activities
35
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
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.34 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.30 |
| CHEMBL4450627 | — | — | 1 | 7.10 |
| CHEMBL4473956 | — | — | 1 | 7.05 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 6.70 |
| CHEMBL4541648 | — | — | 1 | 6.68 |
| CHEMBL4463109 | — | — | 1 | 6.68 |
| CHEMBL4543011 | — | — | 1 | 6.67 |
| CHEMBL4464668 | — | — | 1 | 6.48 |
| CHEMBL4470305 | — | — | 1 | 6.35 |
| CHEMBL4435664 | — | — | 1 | 6.28 |
| CHEMBL4461890 | — | — | 1 | 6.23 |
| CHEMBL4459688 | — | — | 1 | 6.19 |
| CHEMBL1650951 | — | — | 1 | 6.16 |
| CHEMBL4439785 | — | — | 1 | 6.15 |
| CHEMBL4522075 | — | — | 1 | 6.12 |
| CHEMBL4444087 | — | — | 1 | 6.09 |
| CHEMBL4441142 | — | — | 1 | 6.05 |
| CHEMBL4554336 | — | — | 1 | 6.00 |
| CHEMBL4578121 | — | — | 1 | 5.89 |
| CHEMBL4533508 | — | — | 1 | 5.46 |
| CHEMBL4444559 | — | — | 1 | 5.43 |
| CHEMBL4461593 | — | — | 1 | - |
| CHEMBL4526325 | — | — | 1 | - |
| CHEMBL4513304 | — | — | 1 | - |
| CHEMBL4464446 | — | — | 1 | - |
| CHEMBL4463237 | — | — | 1 | - |
| CHEMBL4445411 | — | — | 1 | - |
| CHEMBL4463762 | — | — | 1 | - |
| CHEMBL4557507 | — | — | 1 | - |
| CHEMBL4537868 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4450627 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4473956 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4541648 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4463109 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4543011 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4464668 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL4470305 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4435664 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4461890 | — | IC50 | = | 584.0 | nM | 6.23 |
| CHEMBL4459688 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1650951 | — | IC50 | = | 685.0 | nM | 6.16 |
| CHEMBL4439785 | — | IC50 | = | 709.0 | nM | 6.15 |
| CHEMBL4522075 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4444087 | — | IC50 | = | 817.0 | nM | 6.09 |
| CHEMBL4441142 | — | IC50 | = | 895.0 | nM | 6.05 |
| CHEMBL4554336 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4578121 | — | IC50 | = | 1276.0 | nM | 5.89 |
| CHEMBL4533508 | — | IC50 | = | 3456.0 | nM | 5.46 |
| CHEMBL4444559 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL4520141 | — | IC50 | - | — | - | |
| CHEMBL4544861 | — | IC50 | - | — | - | |
| CHEMBL4454565 | — | IC50 | - | — | - | |
| CHEMBL4457521 | — | IC50 | - | — | - | |
| CHEMBL4461660 | — | IC50 | - | — | - | |
| CHEMBL4537868 | — | IC50 | - | — | - | |
| CHEMBL4557507 | — | IC50 | - | — | - | |
| CHEMBL4463762 | — | IC50 | - | — | - | |
| CHEMBL4445411 | — | IC50 | - | — | - | |
| CHEMBL4463237 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4464446 | — | IC50 | - | — | - | |
| CHEMBL4513304 | — | IC50 | - | — | - | |
| CHEMBL4526325 | — | IC50 | - | — | - | |
| CHEMBL4461593 | — | IC50 | - | — | - |