Assay Detail
Binding
CHEMBL4261268
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Inhibition of JAK1 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method
23
Total Activities
23
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
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.54 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290597 | — | — | 1 | 8.92 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.85 |
| CHEMBL4286762 | — | — | 1 | 8.72 |
| CHEMBL4286103 | — | — | 1 | 8.47 |
| CHEMBL4295151 | — | — | 1 | 8.37 |
| CHEMBL4287893 | — | — | 1 | 8.28 |
| CHEMBL4291720 | — | — | 1 | 8.18 |
| CHEMBL4278842 | — | — | 1 | 8.01 |
| CHEMBL4279991 | — | — | 1 | 7.97 |
| CHEMBL4291298 | — | — | 1 | 7.94 |
| CHEMBL4281080 | — | — | 1 | 7.75 |
| CHEMBL4289532 | — | — | 1 | 7.52 |
| CHEMBL4283458 | — | — | 1 | 7.43 |
| CHEMBL4278853 | — | — | 1 | 7.36 |
| CHEMBL4281492 | — | — | 1 | 7.24 |
| CHEMBL4280783 | — | — | 1 | 7.02 |
| CHEMBL4285332 | — | — | 1 | 6.99 |
| CHEMBL4284499 | — | — | 1 | 6.90 |
| CHEMBL4294002 | — | — | 1 | 6.86 |
| CHEMBL4289375 | — | — | 1 | 6.52 |
| CHEMBL4288673 | — | — | 1 | 6.37 |
| CHEMBL4282720 | — | — | 1 | 6.21 |
| CHEMBL4277379 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290597 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL4286762 | — | IC50 | = | 1.91 | nM | 8.72 |
| CHEMBL4286103 | — | IC50 | = | 3.37 | nM | 8.47 |
| CHEMBL4295151 | — | IC50 | = | 4.23 | nM | 8.37 |
| CHEMBL4287893 | — | IC50 | = | 5.28 | nM | 8.28 |
| CHEMBL4291720 | — | IC50 | = | 6.59 | nM | 8.18 |
| CHEMBL4278842 | — | IC50 | = | 9.89 | nM | 8.01 |
| CHEMBL4279991 | — | IC50 | = | 10.61 | nM | 7.97 |
| CHEMBL4291298 | — | IC50 | = | 11.48 | nM | 7.94 |
| CHEMBL4281080 | — | IC50 | = | 17.86 | nM | 7.75 |
| CHEMBL4289532 | — | IC50 | = | 30.17 | nM | 7.52 |
| CHEMBL4283458 | — | IC50 | = | 37.54 | nM | 7.43 |
| CHEMBL4278853 | — | IC50 | = | 43.78 | nM | 7.36 |
| CHEMBL4281492 | — | IC50 | = | 58.26 | nM | 7.24 |
| CHEMBL4280783 | — | IC50 | = | 95.62 | nM | 7.02 |
| CHEMBL4285332 | — | IC50 | = | 103.15 | nM | 6.99 |
| CHEMBL4284499 | — | IC50 | = | 125.1 | nM | 6.90 |
| CHEMBL4294002 | — | IC50 | = | 138.1 | nM | 6.86 |
| CHEMBL4289375 | — | IC50 | = | 304.45 | nM | 6.52 |
| CHEMBL4288673 | — | IC50 | = | 423.8 | nM | 6.37 |
| CHEMBL4282720 | — | IC50 | = | 616.3 | nM | 6.21 |
| CHEMBL4277379 | — | IC50 | = | 3334.0 | nM | 5.48 |