Assay Detail
Binding
CHEMBL5503692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to recombinant human TYK2 kinase domain by fluorescence polarization 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 |
|---|---|---|---|
| Kd | 10 | 7.67 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.96 |
| CHEMBL4116008 | CERDULATINIB | 2.0 | 1 | 8.16 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.14 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 8.04 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.92 |
| CHEMBL2107823 | GANDOTINIB | 2.0 | 1 | 7.80 |
| CHEMBL4303389 | NS-018 | 2.0 | 1 | 7.68 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.90 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.66 |
| CHEMBL3622820 | ITACITINIB | 3.0 | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4116008 | CERDULATINIB | Kd | = | 6.9 | nM | 8.16 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.3 | nM | 8.14 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 9.2 | nM | 8.04 |
| CHEMBL495727 | AT-9283 | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL2107823 | GANDOTINIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL4303389 | NS-018 | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 125.0 | nM | 6.90 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 217.0 | nM | 6.66 |
| CHEMBL3622820 | ITACITINIB | Kd | = | 385.0 | nM | 6.42 |