Assay Detail
Binding
CHEMBL5731350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro JAK Kinase Inhibition Test: Kinases used were human-derived JAK1, JAK2, JAK3, and TYK2 (Millipore, Germany). Each of these kinases was diluted with a suitable buffer solution as described below, and then mixed with reagents. Kinase-activity inhibitory effects of some of the compounds of Examples 1 to 73 (for example, Examples 5, 55, and 66) for JAK1, JAK2, JAK3, and TYK2 were measured at various concentrations by the above-described method, and IC50 values were determined. The IC50 values of the test compounds were calculated from % inhibition values of the compounds, by the Cheng-Prusoff method (Biochem. Pharmacol. (1973) 22, 3099-3108).
15
Total Activities
5
Compounds Tested
3
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
Substituted N-(pyrrolidine-3-yl)-7H-pyrrolo[2,3-D]pyrimidine-4-amine as janus kinase inhibitor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.08 | 7.61 |
| kon | 5 | - | - |
| k_off | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4293578 | — | — | 3 | 7.61 |
| CHEMBL4284023 | — | — | 3 | 7.39 |
| CHEMBL5889676 | — | — | 3 | 6.70 |
| CHEMBL4279819 | — | — | 3 | 6.60 |
| CHEMBL4290957 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4293578 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4284023 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL5889676 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL4279819 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4279819 | — | kon | = | - | — | - |
| CHEMBL4279819 | — | k_off | = | - | s-1 | - |
| CHEMBL4284023 | — | kon | = | - | — | - |
| CHEMBL4284023 | — | k_off | = | - | s-1 | - |
| CHEMBL4290957 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4290957 | — | kon | = | - | — | - |
| CHEMBL4290957 | — | k_off | = | - | s-1 | - |
| CHEMBL4293578 | — | kon | = | - | — | - |
| CHEMBL4293578 | — | k_off | = | - | s-1 | - |
| CHEMBL5889676 | — | kon | = | - | — | - |
| CHEMBL5889676 | — | k_off | = | - | s-1 | - |