Assay Detail
Binding
CHEMBL4258464
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method
54
Total Activities
54
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
Design, synthesis and evaluation of (<i>R</i>)-3-(7-(methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 7.32 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4279526 | — | — | 1 | 8.85 |
| CHEMBL4289789 | — | — | 1 | 8.55 |
| CHEMBL4293578 | — | — | 1 | 8.24 |
| CHEMBL4276966 | — | — | 1 | 8.20 |
| CHEMBL4285473 | — | — | 1 | 8.16 |
| CHEMBL4283965 | — | — | 1 | 8.14 |
| CHEMBL4279819 | — | — | 1 | 8.07 |
| CHEMBL4283883 | — | — | 1 | 8.05 |
| CHEMBL4283964 | — | — | 1 | 8.03 |
| CHEMBL4278452 | — | — | 1 | 8.03 |
| CHEMBL4282998 | — | — | 1 | 8.01 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 8.00 |
| CHEMBL4284912 | — | — | 1 | 7.92 |
| CHEMBL4290931 | — | — | 1 | 7.92 |
| CHEMBL4281921 | — | — | 1 | 7.89 |
| CHEMBL4279402 | — | — | 1 | 7.82 |
| CHEMBL4294556 | — | — | 1 | 7.80 |
| CHEMBL4287327 | — | — | 1 | 7.77 |
| CHEMBL4291829 | — | — | 1 | 7.70 |
| CHEMBL4284136 | — | — | 1 | 7.70 |
| CHEMBL4292871 | — | — | 1 | 7.68 |
| CHEMBL4293482 | — | — | 1 | 7.64 |
| CHEMBL4290189 | — | — | 1 | 7.58 |
| CHEMBL4284023 | — | — | 1 | 7.54 |
| CHEMBL4277098 | — | — | 1 | 7.51 |
| CHEMBL4276863 | — | — | 1 | 7.47 |
| CHEMBL4280523 | — | — | 1 | 7.40 |
| CHEMBL4286370 | — | — | 1 | 7.30 |
| CHEMBL4295175 | — | — | 1 | 7.28 |
| CHEMBL4291528 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4279526 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4289789 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4293578 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4276966 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4285473 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4283965 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4279819 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4283883 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4283964 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4278452 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4282998 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4284912 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4290931 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4281921 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4279402 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4294556 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4287327 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4291829 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4284136 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4292871 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4293482 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4290189 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4284023 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4277098 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4276863 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4280523 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4286370 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4295175 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4291528 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4280297 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4277099 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4287505 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4285014 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4285042 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4293188 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4285642 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4279618 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4285366 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4290647 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4280010 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4288323 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4280418 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4287238 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4292627 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4287529 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4292011 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4276682 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4282330 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4283881 | — | IC50 | = | 520.0 | nM | 6.28 |