Assay Detail
Binding
CHEMBL3374010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2 (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 | 7.17 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.40 |
| CHEMBL3335678 | — | — | 1 | 8.15 |
| CHEMBL3335691 | — | — | 1 | 8.05 |
| CHEMBL3335686 | — | — | 1 | 7.80 |
| CHEMBL3335690 | — | — | 1 | 7.62 |
| CHEMBL3357978 | — | — | 1 | 7.44 |
| CHEMBL3335699 | — | — | 1 | 7.35 |
| CHEMBL3335685 | — | — | 1 | 7.33 |
| CHEMBL3335676 | — | — | 1 | 7.33 |
| CHEMBL3335682 | — | — | 1 | 7.32 |
| CHEMBL3335692 | — | — | 1 | 7.29 |
| CHEMBL3335687 | — | — | 1 | 7.25 |
| CHEMBL3335694 | — | — | 1 | 7.15 |
| CHEMBL3335684 | — | — | 1 | 7.11 |
| CHEMBL3335688 | — | — | 1 | 7.09 |
| CHEMBL3335680 | — | — | 1 | 7.04 |
| CHEMBL3335683 | — | — | 1 | 7.00 |
| CHEMBL3335698 | — | — | 1 | 6.99 |
| CHEMBL3335689 | — | — | 1 | 6.97 |
| CHEMBL3335695 | — | — | 1 | 6.89 |
| CHEMBL3335697 | — | — | 1 | 6.75 |
| CHEMBL3335681 | — | — | 1 | 6.74 |
| CHEMBL3335693 | — | — | 1 | 6.74 |
| CHEMBL3335677 | — | — | 1 | 6.65 |
| CHEMBL3335679 | — | — | 1 | 6.63 |
| CHEMBL3357977 | — | — | 1 | 5.36 |
| CHEMBL3335696 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3335678 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3335691 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3335686 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3335690 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3357978 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3335699 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3335685 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3335676 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3335682 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3335692 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3335687 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3335694 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3335684 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3335688 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3335680 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3335683 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3335698 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3335689 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3335695 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL3335697 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3335681 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3335693 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3335677 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3335679 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL3357977 | — | IC50 | = | 4410.0 | nM | 5.36 |
| CHEMBL3335696 | — | IC50 | = | 54.0 | nM | - |