Assay Detail
Binding
CHEMBL3374011
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK1 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr in presence of [gamma-33P]ATP by scintillation counting analysis
27
Total Activities
27
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
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.07 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.70 |
| CHEMBL3335691 | — | — | 1 | 7.82 |
| CHEMBL3335686 | — | — | 1 | 7.82 |
| CHEMBL3335684 | — | — | 1 | 7.58 |
| CHEMBL3335678 | — | — | 1 | 7.52 |
| CHEMBL3335685 | — | — | 1 | 7.46 |
| CHEMBL3335687 | — | — | 1 | 7.38 |
| CHEMBL3335694 | — | — | 1 | 7.28 |
| CHEMBL3335676 | — | — | 1 | 7.23 |
| CHEMBL3335692 | — | — | 1 | 7.15 |
| CHEMBL3335682 | — | — | 1 | 7.08 |
| CHEMBL3335683 | — | — | 1 | 7.04 |
| CHEMBL3335689 | — | — | 1 | 6.99 |
| CHEMBL3335688 | — | — | 1 | 6.95 |
| CHEMBL3357978 | — | — | 1 | 6.89 |
| CHEMBL3335699 | — | — | 1 | 6.72 |
| CHEMBL3335693 | — | — | 1 | 6.70 |
| CHEMBL3335698 | — | — | 1 | 6.64 |
| CHEMBL3335696 | — | — | 1 | 6.54 |
| CHEMBL3335695 | — | — | 1 | 6.29 |
| CHEMBL3335697 | — | — | 1 | 6.21 |
| CHEMBL3357977 | — | — | 1 | 5.65 |
| CHEMBL3335690 | — | — | 1 | - |
| CHEMBL3335681 | — | — | 1 | - |
| CHEMBL3335680 | — | — | 1 | - |
| CHEMBL3335679 | — | — | 1 | - |
| CHEMBL3335677 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3335691 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3335686 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3335684 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3335678 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3335685 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3335687 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3335694 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3335676 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3335692 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3335682 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3335683 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3335689 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL3335688 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3357978 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL3335699 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL3335693 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3335698 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL3335696 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL3335695 | — | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL3335697 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL3357977 | — | IC50 | = | 2225.0 | nM | 5.65 |
| CHEMBL3335690 | — | IC50 | - | — | - | |
| CHEMBL3335681 | — | IC50 | - | — | - | |
| CHEMBL3335680 | — | IC50 | - | — | - | |
| CHEMBL3335679 | — | IC50 | - | — | - | |
| CHEMBL3335677 | — | IC50 | - | — | - |