Assay Detail
Binding
CHEMBL4145343
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Binding affinity to DNA-tagged human GAK expressed in Escherichia coli BL21 using immobilised ligand incubated for 1 hr by quantitative PCR
22
Total Activities
22
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
Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 6.95 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.51 |
| CHEMBL3425867 | — | — | 1 | 8.05 |
| CHEMBL4165336 | — | — | 1 | 7.96 |
| CHEMBL4169166 | — | — | 1 | 7.75 |
| CHEMBL4163357 | — | — | 1 | 7.72 |
| CHEMBL4174075 | — | — | 1 | 7.58 |
| CHEMBL4177020 | — | — | 1 | 7.46 |
| CHEMBL4159994 | — | — | 1 | 7.34 |
| CHEMBL4171678 | — | — | 1 | 7.28 |
| CHEMBL4170643 | — | — | 1 | 7.21 |
| CHEMBL4163801 | — | — | 1 | 7.10 |
| CHEMBL4172550 | — | — | 1 | 7.05 |
| CHEMBL4160425 | — | — | 1 | 6.80 |
| CHEMBL4175117 | — | — | 1 | 6.77 |
| CHEMBL4167255 | — | — | 1 | 6.72 |
| CHEMBL4168337 | — | — | 1 | 6.68 |
| CHEMBL4159403 | — | — | 1 | 6.60 |
| CHEMBL4161901 | — | — | 1 | 6.10 |
| CHEMBL4166209 | — | — | 1 | 6.01 |
| CHEMBL4162766 | — | — | 1 | 5.80 |
| CHEMBL4170698 | — | — | 1 | 5.37 |
| CHEMBL4167311 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL3425867 | — | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL4165336 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL4169166 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL4163357 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL4174075 | — | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL4177020 | — | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL4159994 | — | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL4171678 | — | Kd | = | 52.0 | nM | 7.28 |
| CHEMBL4170643 | — | Kd | = | 61.0 | nM | 7.21 |
| CHEMBL4163801 | — | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL4172550 | — | Kd | = | 89.0 | nM | 7.05 |
| CHEMBL4160425 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL4175117 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL4167255 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL4168337 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL4159403 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL4161901 | — | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL4166209 | — | Kd | = | 970.0 | nM | 6.01 |
| CHEMBL4162766 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL4170698 | — | Kd | = | 4300.0 | nM | 5.37 |
| CHEMBL4167311 | — | Kd | = | 7200.0 | nM | 5.14 |