Assay Detail
Binding
CHEMBL2390026
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TYK2 (unknown origin)
37
Total Activities
37
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 |
|---|---|---|---|
| Ki | 37 | 8.22 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.30 |
| CHEMBL2387225 | — | — | 1 | 9.00 |
| CHEMBL2387219 | — | — | 1 | 8.89 |
| CHEMBL2387221 | — | — | 1 | 8.85 |
| CHEMBL2387222 | — | — | 1 | 8.80 |
| CHEMBL2387223 | — | — | 1 | 8.80 |
| CHEMBL2387124 | — | — | 1 | 8.74 |
| CHEMBL2387127 | — | — | 1 | 8.60 |
| CHEMBL2387110 | — | — | 1 | 8.52 |
| CHEMBL2387112 | — | — | 1 | 8.51 |
| CHEMBL2387218 | — | — | 1 | 8.49 |
| CHEMBL2387119 | — | — | 1 | 8.48 |
| CHEMBL2387126 | — | — | 1 | 8.47 |
| CHEMBL2387118 | — | — | 1 | 8.36 |
| CHEMBL2387224 | — | — | 1 | 8.32 |
| CHEMBL2387131 | — | — | 1 | 8.29 |
| CHEMBL2387114 | — | — | 1 | 8.27 |
| CHEMBL2387128 | — | — | 1 | 8.15 |
| CHEMBL2387115 | — | — | 1 | 8.12 |
| CHEMBL2387122 | — | — | 1 | 8.11 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.11 |
| CHEMBL2387113 | — | — | 1 | 8.11 |
| CHEMBL2387132 | — | — | 1 | 8.07 |
| CHEMBL2387134 | — | — | 1 | 8.04 |
| CHEMBL2387125 | — | — | 1 | 8.02 |
| CHEMBL2387117 | — | — | 1 | 7.99 |
| CHEMBL2385101 | — | — | 1 | 7.96 |
| CHEMBL2387217 | — | — | 1 | 7.96 |
| CHEMBL2387129 | — | — | 1 | 7.94 |
| CHEMBL2387111 | — | — | 1 | 7.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2387225 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2387219 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2387221 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2387222 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2387223 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2387124 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2387127 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2387110 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2387112 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2387218 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2387119 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2387126 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL2387118 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2387224 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL2387131 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL2387114 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2387128 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL2387115 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL221959 | TOFACITINIB | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL2387113 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL2387122 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL2387132 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL2387134 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2387125 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL2387117 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL2385101 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL2387217 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL2387129 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL2387111 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2387133 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL2387220 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2387116 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL2387130 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL2387123 | — | Ki | = | 30.1 | nM | 7.52 |
| CHEMBL2387121 | — | Ki | = | 35.1 | nM | 7.46 |
| CHEMBL2387120 | — | Ki | = | 60.8 | nM | 7.22 |