Assay Detail
Binding
CHEMBL4612622
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Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay
38
Total Activities
38
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
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.26 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.57 |
| CHEMBL4643061 | — | — | 1 | 7.92 |
| CHEMBL4649484 | — | — | 1 | 7.82 |
| CHEMBL4639606 | — | — | 1 | 7.72 |
| CHEMBL4636507 | — | — | 1 | 7.50 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 7.44 |
| CHEMBL4647276 | — | — | 1 | 7.19 |
| CHEMBL4638030 | — | — | 1 | 7.05 |
| CHEMBL4647115 | — | — | 1 | 7.03 |
| CHEMBL4632766 | — | — | 1 | 6.92 |
| CHEMBL4639973 | — | — | 1 | 6.92 |
| CHEMBL4634289 | — | — | 1 | 6.82 |
| CHEMBL4640029 | — | — | 1 | 6.80 |
| CHEMBL4648612 | — | — | 1 | 6.48 |
| CHEMBL4640521 | — | — | 1 | 6.47 |
| CHEMBL4648820 | — | — | 1 | 6.44 |
| CHEMBL4645814 | — | — | 1 | 6.44 |
| CHEMBL4645613 | — | — | 1 | 6.42 |
| CHEMBL4636220 | — | — | 1 | 6.37 |
| CHEMBL4641076 | — | — | 1 | 6.24 |
| CHEMBL4639048 | — | — | 1 | 6.24 |
| CHEMBL4636371 | — | — | 1 | 5.89 |
| CHEMBL4648246 | — | — | 1 | 5.89 |
| CHEMBL4632897 | — | — | 1 | 5.80 |
| CHEMBL4638953 | — | — | 1 | 5.77 |
| CHEMBL4633028 | — | — | 1 | 5.68 |
| CHEMBL4638808 | — | — | 1 | 5.60 |
| CHEMBL4647966 | — | — | 1 | 5.57 |
| CHEMBL4638696 | — | — | 1 | 5.55 |
| CHEMBL4642546 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4643061 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4649484 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4639606 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4636507 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4647276 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4638030 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4647115 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4632766 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4639973 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4634289 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4640029 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4648612 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4640521 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4648820 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4645814 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4645613 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4636220 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4641076 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4639048 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4636371 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4648246 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4632897 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4638953 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4633028 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4638808 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4647966 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4638696 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4642546 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4635464 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4647506 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4637596 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4649054 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4640335 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4632980 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4636368 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4645113 | — | IC50 | = | 35000.0 | nM | 4.46 |