Assay Detail
Binding
CHEMBL5553737
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Inhibition of full length EPHA4 (unknown origin) expressed in HEK293T cells using NanoBRET NanoGlo substrate incubated for 2 hrs in presence of K4 tracer by NanoBRET assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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 |
|---|---|---|---|
| EC50 | 12 | 7.04 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566108 | — | — | 1 | 7.43 |
| CHEMBL5574808 | — | — | 1 | 7.43 |
| CHEMBL1198514 | — | — | 1 | 7.32 |
| CHEMBL5568747 | — | — | 1 | 7.24 |
| CHEMBL5566270 | — | — | 1 | 7.22 |
| CHEMBL5572722 | — | — | 1 | 7.08 |
| CHEMBL5571675 | — | — | 1 | 6.72 |
| CHEMBL5595264 | — | — | 1 | 6.60 |
| CHEMBL5565547 | — | — | 1 | 6.35 |
| CHEMBL5570805 | — | — | 1 | - |
| CHEMBL1235529 | — | — | 1 | - |
| CHEMBL5574265 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566108 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5574808 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1198514 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5568747 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5566270 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5572722 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5571675 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5595264 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5565547 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5570805 | — | EC50 | - | — | - | |
| CHEMBL1235529 | — | EC50 | - | — | - | |
| CHEMBL5574265 | — | EC50 | - | — | - |