Assay Detail
Binding
CHEMBL2344643
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Inhibition of human myc-tagged full length EphB4 expressed in MEF cells assessed as inhibition of ephrinB2-Fc-induced autophosphorylation incubated for 90 mins prior to ephrinB2-Fc-induction measured after 2 hrs by sandwich ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MEF |
| 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 | 12 | 6.72 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2333603 | — | — | 1 | 7.30 |
| CHEMBL2333595 | — | — | 1 | 7.17 |
| CHEMBL566515 | — | — | 1 | 6.89 |
| CHEMBL2333602 | — | — | 1 | 6.82 |
| CHEMBL2333593 | — | — | 1 | 6.64 |
| CHEMBL2333597 | — | — | 1 | 6.57 |
| CHEMBL2333600 | — | — | 1 | 5.66 |
| CHEMBL2333594 | — | — | 1 | - |
| CHEMBL2333596 | — | — | 1 | - |
| CHEMBL2333598 | — | — | 1 | - |
| CHEMBL2333599 | — | — | 1 | - |
| CHEMBL2333601 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2333603 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2333595 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL566515 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2333602 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2333593 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2333597 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2333600 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2333594 | — | IC50 | - | — | - | |
| CHEMBL2333596 | — | IC50 | - | — | - | |
| CHEMBL2333598 | — | IC50 | - | — | - | |
| CHEMBL2333599 | — | IC50 | - | — | - | |
| CHEMBL2333601 | — | IC50 | - | — | - |