Assay Detail
Binding
CHEMBL5553734
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Binding affinity to recombinant his tagged EPHA2 (D596 to G900 residues) (unknown origin) expressed in Escherichia coli rosetta BL21(D3)-R3-pRARE2 competent cells 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 | 6.85 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5574808 | — | — | 1 | 7.02 |
| CHEMBL5565547 | — | — | 1 | 7.01 |
| CHEMBL5566270 | — | — | 1 | 6.90 |
| CHEMBL5568747 | — | — | 1 | 6.83 |
| CHEMBL1235529 | — | — | 1 | 6.51 |
| CHEMBL5574265 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5574808 | — | Kd | = | 95.3 | nM | 7.02 |
| CHEMBL5565547 | — | Kd | = | 97.4 | nM | 7.01 |
| CHEMBL5566270 | — | Kd | = | 126.1 | nM | 6.90 |
| CHEMBL5568747 | — | Kd | = | 148.0 | nM | 6.83 |
| CHEMBL1235529 | — | Kd | = | 307.0 | nM | 6.51 |
| CHEMBL5574265 | — | Kd | - | — | - |