Assay Detail
ADMET
CHEMBL4124183
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Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate in presence of 10 uM [gamma33P]ATP by radiometric method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.95 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.70 |
| CHEMBL4127590 | — | — | 1 | 7.32 |
| CHEMBL4128266 | — | — | 1 | 7.28 |
| CHEMBL4128410 | — | — | 1 | 6.95 |
| CHEMBL4126514 | — | — | 1 | 6.74 |
| CHEMBL4125719 | — | — | 1 | 6.73 |
| CHEMBL4128181 | — | — | 1 | 6.46 |
| CHEMBL1650951 | — | — | 1 | 6.24 |
| CHEMBL4125861 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4127590 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4128266 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4128410 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4126514 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4125719 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL4128181 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL1650951 | — | IC50 | = | 578.0 | nM | 6.24 |
| CHEMBL4125861 | — | IC50 | = | 765.0 | nM | 6.12 |