Assay Detail
Binding
CHEMBL4667704
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Binding affinity to human wild type partial length GAK (G13 to Y338 residues) expressed in bacterial expression system by KinomeScan method
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
Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 7.52 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4443342 | — | — | 1 | 8.39 |
| CHEMBL4781252 | — | — | 1 | 8.31 |
| CHEMBL4585158 | — | — | 1 | 8.31 |
| CHEMBL4556662 | — | — | 1 | 8.20 |
| CHEMBL4740155 | — | — | 1 | 8.12 |
| CHEMBL4517424 | — | — | 1 | 8.07 |
| CHEMBL4782290 | — | — | 1 | 8.07 |
| CHEMBL535429 | — | — | 1 | 8.00 |
| CHEMBL311959 | — | — | 1 | 7.96 |
| CHEMBL3925728 | — | — | 1 | 7.89 |
| CHEMBL4746133 | — | — | 1 | 7.64 |
| CHEMBL530635 | — | — | 1 | 7.47 |
| CHEMBL4586530 | — | — | 1 | 7.46 |
| CHEMBL4575895 | — | — | 1 | 7.37 |
| CHEMBL4592501 | — | — | 1 | 7.32 |
| CHEMBL4744568 | — | — | 1 | 7.24 |
| CHEMBL4752943 | — | — | 1 | 7.12 |
| CHEMBL4446630 | — | — | 1 | 6.89 |
| CHEMBL4586588 | — | — | 1 | 6.77 |
| CHEMBL4746235 | — | — | 1 | 6.35 |
| CHEMBL4462395 | — | — | 1 | 5.00 |
| CHEMBL4518437 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4443342 | — | Kd | = | 4.1 | nM | 8.39 |
| CHEMBL4781252 | — | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL4585158 | — | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL4556662 | — | Kd | = | 6.3 | nM | 8.20 |
| CHEMBL4740155 | — | Kd | = | 7.6 | nM | 8.12 |
| CHEMBL4517424 | — | Kd | = | 8.6 | nM | 8.07 |
| CHEMBL4782290 | — | Kd | = | 8.6 | nM | 8.07 |
| CHEMBL535429 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL311959 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL3925728 | — | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL4746133 | — | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL530635 | — | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL4586530 | — | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL4575895 | — | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL4592501 | — | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL4744568 | — | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL4752943 | — | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL4446630 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL4586588 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL4746235 | — | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL4462395 | — | Kd | = | 9900.0 | nM | 5.00 |
| CHEMBL4518437 | — | Kd | > | 30000.0 | nM | - |