Assay Detail
Binding
CHEMBL2389438
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Inhibition of TYK2 (unknown origin) assessed as inhibition of STAT4 phosphorylation by cell-based assay
16
Total Activities
16
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
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.66 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.00 |
| CHEMBL2387221 | — | — | 1 | 6.84 |
| CHEMBL2387124 | — | — | 1 | 6.80 |
| CHEMBL2387127 | — | — | 1 | 6.71 |
| CHEMBL2387126 | — | — | 1 | 6.70 |
| CHEMBL2387222 | — | — | 1 | 6.68 |
| CHEMBL2387223 | — | — | 1 | 6.65 |
| CHEMBL2387225 | — | — | 1 | 6.61 |
| CHEMBL2387119 | — | — | 1 | 6.56 |
| CHEMBL2387224 | — | — | 1 | 6.42 |
| CHEMBL2387110 | — | — | 1 | 6.41 |
| CHEMBL2387112 | — | — | 1 | 6.36 |
| CHEMBL2387118 | — | — | 1 | 6.34 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.20 |
| CHEMBL2387219 | — | — | 1 | - |
| CHEMBL2387218 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2387221 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL2387124 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL2387127 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL2387126 | — | EC50 | = | 198.0 | nM | 6.70 |
| CHEMBL2387222 | — | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL2387223 | — | EC50 | = | 224.0 | nM | 6.65 |
| CHEMBL2387225 | — | EC50 | = | 248.0 | nM | 6.61 |
| CHEMBL2387119 | — | EC50 | = | 273.0 | nM | 6.56 |
| CHEMBL2387224 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2387110 | — | EC50 | = | 393.0 | nM | 6.41 |
| CHEMBL2387112 | — | EC50 | = | 436.0 | nM | 6.36 |
| CHEMBL2387118 | — | EC50 | = | 452.0 | nM | 6.34 |
| CHEMBL221959 | TOFACITINIB | EC50 | = | 625.0 | nM | 6.20 |
| CHEMBL2387219 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2387218 | — | EC50 | > | 5000.0 | nM | - |