Assay Detail
Binding
CHEMBL5503696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TYK2 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase assay
10
Total Activities
10
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
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.75 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.82 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 7.58 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.44 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.22 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | 7.04 |
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 6.67 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.60 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.27 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.43 |
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4116008 | CERDULATINIB | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL495727 | AT-9283 | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2107823 | GANDOTINIB | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4303389 | NS-018 | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL1078178 | MOMELOTINIB | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL2035187 | PACRITINIB | IC50 | = | 536.0 | nM | 6.27 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 3714.0 | nM | 5.43 |
| CHEMBL3622820 | ITACITINIB | IC50 | = | 4095.0 | nM | 5.39 |