Assay Detail
Binding
CHEMBL4612624
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human TYK2 catalytic domain (871 to 1187 residues) incubated for 40 mins in presence of TK substrate-biotin by TR-FRET assay
33
Total Activities
33
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
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.04 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643061 | — | — | 1 | 7.70 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.14 |
| CHEMBL4645814 | — | — | 1 | 6.89 |
| CHEMBL4645613 | — | — | 1 | 6.82 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 6.80 |
| CHEMBL4647115 | — | — | 1 | 6.75 |
| CHEMBL4634289 | — | — | 1 | 6.66 |
| CHEMBL4648612 | — | — | 1 | 6.66 |
| CHEMBL4639973 | — | — | 1 | 6.66 |
| CHEMBL4648820 | — | — | 1 | 6.48 |
| CHEMBL4636220 | — | — | 1 | 6.37 |
| CHEMBL4638696 | — | — | 1 | 6.19 |
| CHEMBL4636371 | — | — | 1 | 6.17 |
| CHEMBL4640521 | — | — | 1 | 6.16 |
| CHEMBL4640335 | — | — | 1 | 6.08 |
| CHEMBL4641076 | — | — | 1 | 5.96 |
| CHEMBL4648246 | — | — | 1 | 5.80 |
| CHEMBL4638953 | — | — | 1 | 5.57 |
| CHEMBL4633028 | — | — | 1 | 5.55 |
| CHEMBL4642546 | — | — | 1 | 5.47 |
| CHEMBL4635464 | — | — | 1 | 5.41 |
| CHEMBL4647506 | — | — | 1 | 5.38 |
| CHEMBL4632897 | — | — | 1 | 5.17 |
| CHEMBL4632980 | — | — | 1 | 4.96 |
| CHEMBL4649054 | — | — | 1 | 4.85 |
| CHEMBL4636368 | — | — | 1 | 4.80 |
| CHEMBL4645113 | — | — | 1 | 4.62 |
| CHEMBL4647966 | — | — | 1 | - |
| CHEMBL4632766 | — | — | 1 | - |
| CHEMBL4638808 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643061 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4645814 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4645613 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4647115 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4634289 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4648612 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4639973 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4648820 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4636220 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4638696 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4636371 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4640521 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4640335 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4641076 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4648246 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4638953 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4633028 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4642546 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4635464 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4647506 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4632897 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4632980 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4649054 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4636368 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4645113 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4647966 | — | IC50 | - | — | - | |
| CHEMBL4632766 | — | IC50 | - | — | - | |
| CHEMBL4638808 | — | IC50 | - | — | - | |
| CHEMBL4639048 | — | IC50 | - | — | - | |
| CHEMBL4637596 | — | IC50 | - | — | - | |
| CHEMBL4640029 | — | IC50 | - | — | - |