Assay Detail
Binding
CHEMBL4261269
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Inhibition of TYK2 (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 |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.03 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4295151 | — | — | 1 | 8.71 |
| CHEMBL4291720 | — | — | 1 | 8.65 |
| CHEMBL4290597 | — | — | 1 | 8.36 |
| CHEMBL4281080 | — | — | 1 | 8.08 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.98 |
| CHEMBL4286762 | — | — | 1 | 7.76 |
| CHEMBL4278842 | — | — | 1 | 7.74 |
| CHEMBL4291298 | — | — | 1 | 7.49 |
| CHEMBL4284499 | — | — | 1 | 7.40 |
| CHEMBL4287893 | — | — | 1 | 7.35 |
| CHEMBL4286103 | — | — | 1 | 7.13 |
| CHEMBL4283458 | — | — | 1 | 6.78 |
| CHEMBL4279991 | — | — | 1 | 6.75 |
| CHEMBL4281492 | — | — | 1 | 6.59 |
| CHEMBL4289532 | — | — | 1 | 6.56 |
| CHEMBL4278853 | — | — | 1 | 6.47 |
| CHEMBL4280783 | — | — | 1 | 6.37 |
| CHEMBL4288673 | — | — | 1 | 6.15 |
| CHEMBL4294002 | — | — | 1 | 5.93 |
| CHEMBL4289375 | — | — | 1 | 5.82 |
| CHEMBL4277379 | — | — | 1 | 5.32 |
| CHEMBL4282720 | — | — | 1 | 5.24 |
| CHEMBL4285332 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4295151 | — | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL4291720 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL4290597 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL4281080 | — | IC50 | = | 8.38 | nM | 8.08 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 10.38 | nM | 7.98 |
| CHEMBL4286762 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4278842 | — | IC50 | = | 18.42 | nM | 7.74 |
| CHEMBL4291298 | — | IC50 | = | 32.39 | nM | 7.49 |
| CHEMBL4284499 | — | IC50 | = | 39.43 | nM | 7.40 |
| CHEMBL4287893 | — | IC50 | = | 45.1 | nM | 7.35 |
| CHEMBL4286103 | — | IC50 | = | 73.66 | nM | 7.13 |
| CHEMBL4283458 | — | IC50 | = | 166.85 | nM | 6.78 |
| CHEMBL4279991 | — | IC50 | = | 176.3 | nM | 6.75 |
| CHEMBL4281492 | — | IC50 | = | 256.5 | nM | 6.59 |
| CHEMBL4289532 | — | IC50 | = | 273.4 | nM | 6.56 |
| CHEMBL4278853 | — | IC50 | = | 336.3 | nM | 6.47 |
| CHEMBL4280783 | — | IC50 | = | 427.45 | nM | 6.37 |
| CHEMBL4288673 | — | IC50 | = | 708.65 | nM | 6.15 |
| CHEMBL4294002 | — | IC50 | = | 1163.5 | nM | 5.93 |
| CHEMBL4289375 | — | IC50 | = | 1502.0 | nM | 5.82 |
| CHEMBL4277379 | — | IC50 | = | 4766.0 | nM | 5.32 |
| CHEMBL4282720 | — | IC50 | = | 5730.0 | nM | 5.24 |
| CHEMBL4285332 | — | IC50 | > | 1000.0 | nM | - |