Assay Detail
Binding
CHEMBL4124177
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Inhibition of recombinant human JAK3 (781 to 1124 residues) expressed in baculovirus expression system assessed as reduction in polypeptide substrate phosphorylation in presence of ATP by ELISA
30
Total Activities
30
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
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 | 30 | 7.00 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.46 |
| CHEMBL4125719 | — | — | 1 | 8.40 |
| CHEMBL4128181 | — | — | 1 | 8.05 |
| CHEMBL1650951 | — | — | 1 | 7.96 |
| CHEMBL4127091 | — | — | 1 | 7.96 |
| CHEMBL4125861 | — | — | 1 | 7.85 |
| CHEMBL4128324 | — | — | 1 | 7.64 |
| CHEMBL4128266 | — | — | 1 | 7.57 |
| CHEMBL4126944 | — | — | 1 | 7.52 |
| CHEMBL4128410 | — | — | 1 | 7.29 |
| CHEMBL4126097 | — | — | 1 | 7.23 |
| CHEMBL4129249 | — | — | 1 | 6.89 |
| CHEMBL4127590 | — | — | 1 | 6.89 |
| CHEMBL4129641 | — | — | 1 | 6.87 |
| CHEMBL4126514 | — | — | 1 | 6.74 |
| CHEMBL4129559 | — | — | 1 | 6.69 |
| CHEMBL4127174 | — | — | 1 | 6.65 |
| CHEMBL4129159 | — | — | 1 | 6.43 |
| CHEMBL4127032 | — | — | 1 | 6.41 |
| CHEMBL4128579 | — | — | 1 | 6.36 |
| CHEMBL4125935 | — | — | 1 | 6.33 |
| CHEMBL4128719 | — | — | 1 | 6.31 |
| CHEMBL4129943 | — | — | 1 | 6.30 |
| CHEMBL4127332 | — | — | 1 | 6.30 |
| CHEMBL4125798 | — | — | 1 | 6.26 |
| CHEMBL4128988 | — | — | 1 | 6.24 |
| CHEMBL4127480 | — | — | 1 | 6.19 |
| CHEMBL4129794 | — | — | 1 | 6.17 |
| CHEMBL4128005 | — | — | 1 | - |
| CHEMBL4129808 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4125719 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4128181 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1650951 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4127091 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4125861 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4128324 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4128266 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4126944 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4128410 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4126097 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4129249 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4127590 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4129641 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4126514 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4129559 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4127174 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4129159 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4127032 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4128579 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL4125935 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4128719 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4129943 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL4127332 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL4125798 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL4128988 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL4127480 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL4129794 | — | IC50 | = | 678.0 | nM | 6.17 |
| CHEMBL4128005 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4129808 | — | IC50 | > | 10000.0 | nM | - |