Assay Detail
Binding
CHEMBL3738294
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Displacement of biotinylated-ephrin-A1-Fc from EphA2-Fc receptor (unknown origin) preincubated for 1 hr followed by biotinylated-ephrin-A1-Fc addition measured after 4 hrs by ELISA
15
Total Activities
15
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
Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.89 | 5.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3734863 | — | — | 1 | 5.45 |
| CHEMBL3736250 | — | — | 1 | 5.39 |
| CHEMBL3735992 | — | — | 1 | 5.37 |
| CHEMBL3734937 | — | — | 1 | 5.30 |
| CHEMBL3735509 | — | — | 1 | 5.22 |
| CHEMBL3736171 | — | — | 1 | 5.20 |
| CHEMBL3736070 | — | — | 1 | 5.05 |
| CHEMBL3736176 | — | — | 1 | 4.65 |
| CHEMBL169264 | — | — | 1 | 4.40 |
| CHEMBL3736217 | — | — | 1 | 4.32 |
| CHEMBL3735472 | — | — | 1 | 4.30 |
| CHEMBL3736006 | — | — | 1 | 4.05 |
| CHEMBL3736288 | — | — | 1 | - |
| CHEMBL3735198 | — | — | 1 | - |
| CHEMBL3734875 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3734863 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL3736250 | — | IC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL3735992 | — | IC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL3734937 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3735509 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL3736171 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3736070 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL3736176 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL169264 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3736217 | — | IC50 | = | 47863.01 | nM | 4.32 |
| CHEMBL3735472 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3736006 | — | IC50 | = | 89125.09 | nM | 4.05 |
| CHEMBL3736288 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3735198 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3734875 | — | IC50 | > | 100000.0 | nM | - |