Assay Detail
Binding
CHEMBL4377381
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TYK2 in human whole blood assessed as decrease in IFNalpha-induced STAT5 phosphorylation preincubated for 1 hr followed by stimulation with IFN-alpha for 15 mins by fluorescence analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.00 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4557190 | — | — | 1 | 7.92 |
| CHEMBL4435170 | DEUCRAVACITINIB | 4.0 | 1 | 7.89 |
| CHEMBL4571117 | — | — | 1 | 7.89 |
| CHEMBL4469750 | — | — | 1 | 7.82 |
| CHEMBL4476261 | — | — | 1 | 7.80 |
| CHEMBL4580625 | — | — | 1 | 7.72 |
| CHEMBL4572855 | — | — | 1 | 7.64 |
| CHEMBL4457060 | — | — | 1 | 7.40 |
| CHEMBL4537259 | — | — | 1 | 7.21 |
| CHEMBL4559585 | — | — | 1 | 7.16 |
| CHEMBL4566158 | — | — | 1 | 7.10 |
| CHEMBL4565054 | — | — | 1 | 7.06 |
| CHEMBL4443834 | — | — | 1 | 7.00 |
| CHEMBL4582205 | — | — | 1 | 6.92 |
| CHEMBL4468025 | — | — | 1 | 6.85 |
| CHEMBL4435079 | — | — | 1 | 6.82 |
| CHEMBL4578980 | — | — | 1 | 6.80 |
| CHEMBL4543984 | — | — | 1 | 6.77 |
| CHEMBL4474729 | — | — | 1 | 6.75 |
| CHEMBL4524832 | — | — | 1 | 6.64 |
| CHEMBL4439617 | — | — | 1 | 6.57 |
| CHEMBL4441840 | — | — | 1 | 6.55 |
| CHEMBL4572426 | — | — | 1 | 6.52 |
| CHEMBL4581296 | — | — | 1 | 6.41 |
| CHEMBL4534832 | — | — | 1 | 6.28 |
| CHEMBL4587924 | — | — | 1 | 6.24 |
| CHEMBL4577224 | — | — | 1 | 6.12 |
| CHEMBL4527672 | — | — | 1 | 6.06 |
| CHEMBL4543090 | — | — | 1 | - |
| CHEMBL4530035 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4557190 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4435170 | DEUCRAVACITINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4571117 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4469750 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4476261 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4580625 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4572855 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4457060 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4537259 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4559585 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4566158 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4565054 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4443834 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4582205 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4468025 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4435079 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4578980 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4543984 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4474729 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4524832 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4439617 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4441840 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4572426 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4581296 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4534832 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4587924 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4577224 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4527672 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4543090 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4530035 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4471908 | — | IC50 | > | 10000.0 | nM | - |