Assay Detail
Binding
CHEMBL4481498
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to biotinylated human GAK (13 to 338 residues) expressed in Escherichia coli incubated for 1.5 hrs by fluorescent tracer dependent TR-FRET based competitive ligand binding displacement assay
11
Total Activities
11
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
SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 7.98 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4443342 | — | — | 1 | 8.72 |
| CHEMBL311959 | — | — | 1 | 8.54 |
| CHEMBL4585158 | — | — | 1 | 8.41 |
| CHEMBL4556662 | — | — | 1 | 8.17 |
| CHEMBL4517424 | — | — | 1 | 8.10 |
| CHEMBL4575895 | — | — | 1 | 8.01 |
| CHEMBL4586530 | — | — | 1 | 7.77 |
| CHEMBL4592501 | — | — | 1 | 7.68 |
| CHEMBL530635 | — | — | 1 | 7.60 |
| CHEMBL535429 | — | — | 1 | 7.51 |
| CHEMBL4586588 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4443342 | — | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL311959 | — | Kd | = | 2.9 | nM | 8.54 |
| CHEMBL4585158 | — | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL4556662 | — | Kd | = | 6.7 | nM | 8.17 |
| CHEMBL4517424 | — | Kd | = | 7.9 | nM | 8.10 |
| CHEMBL4575895 | — | Kd | = | 9.7 | nM | 8.01 |
| CHEMBL4586530 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL4592501 | — | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL530635 | — | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL535429 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL4586588 | — | Kd | = | 59.0 | nM | 7.23 |