Assay Detail
Binding
CHEMBL4612627
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK1 in human STAT6-bla-RA1 cells assessed as reduction in IL4-induced STAT6-signalling pre-incubated for 1 hrs before human recombinant IL4 addition and further incubated for 4 hrs fluorescence based 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 | 5.86 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643061 | — | — | 1 | 7.11 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.06 |
| CHEMBL4639606 | — | — | 1 | 6.96 |
| CHEMBL4636507 | — | — | 1 | 6.96 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 6.75 |
| CHEMBL4649484 | — | — | 1 | 6.60 |
| CHEMBL4632766 | — | — | 1 | 6.38 |
| CHEMBL4647115 | — | — | 1 | 6.11 |
| CHEMBL4636220 | — | — | 1 | 6.07 |
| CHEMBL4648612 | — | — | 1 | 6.05 |
| CHEMBL4645613 | — | — | 1 | 6.00 |
| CHEMBL4634289 | — | — | 1 | 5.92 |
| CHEMBL4640029 | — | — | 1 | 5.92 |
| CHEMBL4645814 | — | — | 1 | 5.92 |
| CHEMBL4640521 | — | — | 1 | 5.89 |
| CHEMBL4639973 | — | — | 1 | 5.77 |
| CHEMBL4648246 | — | — | 1 | 5.75 |
| CHEMBL4647966 | — | — | 1 | 5.60 |
| CHEMBL4648820 | — | — | 1 | 5.57 |
| CHEMBL4639048 | — | — | 1 | 5.50 |
| CHEMBL4641076 | — | — | 1 | 5.47 |
| CHEMBL4636371 | — | — | 1 | 5.43 |
| CHEMBL4640335 | — | — | 1 | 5.37 |
| CHEMBL4638696 | — | — | 1 | 5.32 |
| CHEMBL4642546 | — | — | 1 | 5.07 |
| CHEMBL4632897 | — | — | 1 | 5.04 |
| CHEMBL4638030 | — | — | 1 | 4.85 |
| CHEMBL4647506 | — | — | 1 | 4.70 |
| CHEMBL4632980 | — | — | 1 | 4.70 |
| CHEMBL4638953 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643061 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4636507 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4639606 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4649484 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4632766 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4647115 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4636220 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4648612 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4645613 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4634289 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4645814 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4640029 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4640521 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4639973 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4648246 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4647966 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4648820 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4639048 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4641076 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4636371 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4640335 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4638696 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4642546 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4632897 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4638030 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4647506 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4632980 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4635464 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4645113 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4637596 | — | IC50 | - | — | - | |
| CHEMBL4633028 | — | IC50 | > | 14000.0 | nM | - |
| CHEMBL4647276 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4636368 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4649054 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4638808 | — | IC50 | - | — | - | |
| CHEMBL4638953 | — | IC50 | > | 40000.0 | nM | - |