Assay Detail
Binding
CHEMBL4332968
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Inhibition of human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system in presence of 6 uM ATP by HTRF assay
43
Total Activities
35
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
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.00 | 9.40 |
| Ki | 8 | 7.91 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464668 | — | — | 1 | 9.40 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 9.40 |
| CHEMBL4450627 | — | — | 2 | 9.40 |
| CHEMBL4463109 | — | — | 1 | 9.40 |
| CHEMBL4578121 | — | — | 1 | 9.22 |
| CHEMBL4454565 | — | — | 2 | 9.22 |
| CHEMBL4543011 | — | — | 2 | 9.10 |
| CHEMBL4435664 | — | — | 2 | 9.00 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.77 |
| CHEMBL1650951 | — | — | 1 | 8.70 |
| CHEMBL4461890 | — | — | 1 | 8.70 |
| CHEMBL4444087 | — | — | 1 | 8.55 |
| CHEMBL4470305 | — | — | 2 | 8.48 |
| CHEMBL4522075 | — | — | 1 | 8.40 |
| CHEMBL4464446 | — | — | 1 | 8.36 |
| CHEMBL4441142 | — | — | 1 | 8.27 |
| CHEMBL4541648 | — | — | 1 | 8.22 |
| CHEMBL4533508 | — | — | 2 | 8.19 |
| CHEMBL4459688 | — | — | 1 | 8.12 |
| CHEMBL4461660 | — | — | 1 | 7.80 |
| CHEMBL4439785 | — | — | 1 | 7.72 |
| CHEMBL4444559 | — | — | 2 | 7.68 |
| CHEMBL4445411 | — | — | 2 | 7.68 |
| CHEMBL4463237 | — | — | 1 | 7.68 |
| CHEMBL4520141 | — | — | 1 | 7.68 |
| CHEMBL4554336 | — | — | 1 | 7.57 |
| CHEMBL4513304 | — | — | 1 | 7.39 |
| CHEMBL4463762 | — | — | 1 | 7.28 |
| CHEMBL4544861 | — | — | 1 | 6.98 |
| CHEMBL4557507 | — | — | 1 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4450627 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4463109 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4464668 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4578121 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4454565 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4543011 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4435664 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4450627 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4435664 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4461890 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1650951 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4444087 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4470305 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4522075 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4470305 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4464446 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4441142 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4541648 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4533508 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4459688 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4454565 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL4461660 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4439785 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4445411 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4520141 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4444559 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4463237 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4554336 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4533508 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4513304 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4445411 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4463762 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4543011 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4544861 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4444559 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL4557507 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4537868 | — | IC50 | = | 873.0 | nM | 6.06 |
| CHEMBL4461593 | — | IC50 | = | 894.0 | nM | 6.05 |
| CHEMBL4526325 | — | IC50 | = | 1777.0 | nM | 5.75 |
| CHEMBL4457521 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4473956 | — | IC50 | < | 0.1 | nM | - |