Assay Detail
Binding
CHEMBL5553735
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Binding affinity to recombinant his tagged GAK (unknown origin) assessed as dissociation constant by surface plasmon resonance method
6
Total Activities
6
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
Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 7.81 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566270 | — | — | 1 | 8.30 |
| CHEMBL5574808 | — | — | 1 | 8.21 |
| CHEMBL5565547 | — | — | 1 | 8.13 |
| CHEMBL5568747 | — | — | 1 | 7.85 |
| CHEMBL5574265 | — | — | 1 | 7.44 |
| CHEMBL1235529 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566270 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL5574808 | — | Kd | = | 6.2 | nM | 8.21 |
| CHEMBL5565547 | — | Kd | = | 7.4 | nM | 8.13 |
| CHEMBL5568747 | — | Kd | = | 14.1 | nM | 7.85 |
| CHEMBL5574265 | — | Kd | = | 36.6 | nM | 7.44 |
| CHEMBL1235529 | — | Kd | = | 112.4 | nM | 6.95 |