Assay Detail
Binding
CHEMBL3430283
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Binding affinity to human GAK fused to T7 bacteriophage expressed in Escherichia coli BL21 after 1 hr by qPCR analysis
30
Total Activities
30
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 |
Publication
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 30 | 7.17 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.59 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 8.19 |
| CHEMBL3425865 | — | — | 1 | 8.08 |
| CHEMBL3425867 | — | — | 1 | 8.05 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.89 |
| CHEMBL3425868 | — | — | 1 | 7.75 |
| CHEMBL3425866 | — | — | 1 | 7.75 |
| CHEMBL3425873 | — | — | 1 | 7.57 |
| CHEMBL3425847 | — | — | 1 | 7.38 |
| CHEMBL3425859 | — | — | 1 | 7.33 |
| CHEMBL3425846 | — | — | 1 | 7.28 |
| CHEMBL3425877 | — | — | 1 | 7.20 |
| CHEMBL3425863 | — | — | 1 | 7.14 |
| CHEMBL3425878 | — | — | 1 | 7.06 |
| CHEMBL3425872 | — | — | 1 | 7.00 |
| CHEMBL3425876 | — | — | 1 | 6.96 |
| CHEMBL3425841 | — | — | 1 | 6.92 |
| CHEMBL3425862 | — | — | 1 | 6.89 |
| CHEMBL3425870 | — | — | 1 | 6.85 |
| CHEMBL3425869 | — | — | 1 | 6.72 |
| CHEMBL3425860 | — | — | 1 | 6.70 |
| CHEMBL3425875 | — | — | 1 | 6.64 |
| CHEMBL3425874 | — | — | 1 | 6.57 |
| CHEMBL3425842 | — | — | 1 | 6.52 |
| CHEMBL3425871 | — | — | 1 | 6.50 |
| CHEMBL3425844 | — | — | 1 | 6.30 |
| CHEMBL3425880 | — | — | 1 | 5.70 |
| CHEMBL3425879 | — | — | 1 | - |
| CHEMBL3425864 | — | — | 1 | - |
| CHEMBL3425861 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL607707 | PELITINIB | Kd | = | 6.4 | nM | 8.19 |
| CHEMBL3425865 | — | Kd | = | 8.3 | nM | 8.08 |
| CHEMBL3425867 | — | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL939 | GEFITINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL3425868 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL3425866 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL3425873 | — | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL3425847 | — | Kd | = | 42.0 | nM | 7.38 |
| CHEMBL3425859 | — | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL3425846 | — | Kd | = | 52.0 | nM | 7.28 |
| CHEMBL3425877 | — | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL3425863 | — | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL3425878 | — | Kd | = | 88.0 | nM | 7.06 |
| CHEMBL3425872 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL3425876 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL3425841 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL3425862 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL3425870 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL3425869 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL3425860 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL3425875 | — | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL3425874 | — | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL3425842 | — | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL3425871 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL3425844 | — | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL3425880 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL3425879 | — | Kd | - | — | - | |
| CHEMBL3425864 | — | Kd | - | — | - | |
| CHEMBL3425861 | — | Kd | - | — | - |