Assay Detail
Binding
CHEMBL2344645
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Inhibition of EphB4 (unknown origin) transfected in CHO cells using Z'-LYTE TYR-1 peptide as substrate after 2 hrs by FRET assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.58 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2333602 | — | — | 1 | 7.85 |
| CHEMBL2333603 | — | — | 1 | 7.25 |
| CHEMBL2333595 | — | — | 1 | 7.04 |
| CHEMBL2333593 | — | — | 1 | 6.75 |
| CHEMBL2333597 | — | — | 1 | 6.74 |
| CHEMBL2333600 | — | — | 1 | 6.52 |
| CHEMBL2333594 | — | — | 1 | 5.89 |
| CHEMBL271967 | — | — | 1 | 5.72 |
| CHEMBL577156 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2333602 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2333603 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2333595 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2333593 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL2333597 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL2333600 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2333594 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL271967 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL577156 | — | IC50 | = | 3300.0 | nM | 5.48 |