Assay Detail
Binding
CHEMBL1007023
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Inhibition of Myc-His-tagged EphB4 expressed in CHOK1 cells assessed as phosphorylation by ELISA
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.21 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468970 | — | — | 1 | 7.77 |
| CHEMBL497198 | — | — | 1 | 7.50 |
| CHEMBL523744 | — | — | 1 | 6.77 |
| CHEMBL257553 | — | — | 1 | 6.76 |
| CHEMBL445162 | — | — | 1 | 6.72 |
| CHEMBL497194 | — | — | 1 | 6.68 |
| CHEMBL496574 | — | — | 1 | 6.13 |
| CHEMBL500724 | — | — | 1 | 6.05 |
| CHEMBL517720 | — | — | 1 | 6.05 |
| CHEMBL523088 | — | — | 1 | 5.69 |
| CHEMBL496968 | — | — | 1 | 5.14 |
| CHEMBL496760 | — | — | 1 | 4.85 |
| CHEMBL497195 | — | — | 1 | 4.65 |
| CHEMBL255874 | — | — | 1 | - |
| CHEMBL498404 | — | — | 1 | - |
| CHEMBL460600 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468970 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL497198 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL523744 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL257553 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL445162 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL497194 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL496574 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL500724 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL517720 | — | IC50 | = | 887.0 | nM | 6.05 |
| CHEMBL523088 | — | IC50 | = | 2054.0 | nM | 5.69 |
| CHEMBL496968 | — | IC50 | = | 7175.0 | nM | 5.14 |
| CHEMBL496760 | — | IC50 | = | 14117.0 | nM | 4.85 |
| CHEMBL497195 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL255874 | — | IC50 | - | — | - | |
| CHEMBL498404 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL460600 | — | IC50 | > | 30000.0 | nM | - |