Assay Detail
Binding
CHEMBL3766477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay
20
Total Activities
20
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
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.84 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3763213 | — | — | 1 | 9.26 |
| CHEMBL3763991 | — | — | 1 | 9.04 |
| CHEMBL3764277 | — | — | 1 | 9.01 |
| CHEMBL3765517 | — | — | 1 | 8.92 |
| CHEMBL3763252 | — | — | 1 | 8.82 |
| CHEMBL3765822 | — | — | 1 | 8.68 |
| CHEMBL3764030 | — | — | 1 | 8.26 |
| CHEMBL3764637 | — | — | 1 | 8.20 |
| CHEMBL3764463 | — | — | 1 | 8.17 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 8.06 |
| CHEMBL3764383 | — | — | 1 | 8.01 |
| CHEMBL3765131 | — | — | 1 | 8.00 |
| CHEMBL3763864 | — | — | 1 | 7.52 |
| CHEMBL3764167 | — | — | 1 | 7.48 |
| CHEMBL3763697 | — | — | 1 | 7.14 |
| CHEMBL3763184 | — | — | 1 | 7.04 |
| CHEMBL498859 | — | — | 1 | 6.55 |
| CHEMBL3763289 | — | — | 1 | 6.43 |
| CHEMBL3763310 | — | — | 1 | 6.19 |
| CHEMBL3763833 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3763213 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL3763991 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL3764277 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3765517 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3763252 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3765822 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3764030 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3764637 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3764463 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2105759 | BARICITINIB | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3764383 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3765131 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3763864 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3764167 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3763697 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3763184 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL498859 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3763289 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3763310 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3763833 | — | IC50 | = | 770.0 | nM | 6.11 |