Assay Detail
Binding
CHEMBL4684873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of biotinylated ephrin-A1-Fc from recombinant mouse c-terminal His6-tagged EphA2 Fc (Ala22 to Ala535 residues) preincubated for 1 hr followed by ephrin-A1-FC addition and measured after 4 hrs by ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3α-carbamoyloxy derivative with antiangiogenetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.31 | 6.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761556 | — | — | 1 | 6.02 |
| CHEMBL4780052 | — | — | 1 | 5.96 |
| CHEMBL4761852 | — | — | 1 | 5.92 |
| CHEMBL4078429 | — | — | 1 | 5.92 |
| CHEMBL4756215 | — | — | 1 | 5.82 |
| CHEMBL4783384 | — | — | 1 | 5.57 |
| CHEMBL4795158 | — | — | 1 | 5.48 |
| CHEMBL4763613 | — | — | 1 | 5.43 |
| CHEMBL4776034 | — | — | 1 | 5.35 |
| CHEMBL4746495 | — | — | 1 | 5.28 |
| CHEMBL4742817 | — | — | 1 | 5.26 |
| CHEMBL4776886 | — | — | 1 | 5.15 |
| CHEMBL4796089 | — | — | 1 | 5.04 |
| CHEMBL4750207 | — | — | 1 | 4.92 |
| CHEMBL4762494 | — | — | 1 | 4.82 |
| CHEMBL4744026 | — | — | 1 | 4.77 |
| CHEMBL4791118 | — | — | 1 | 4.52 |
| CHEMBL4794685 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761556 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4780052 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4761852 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4078429 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4756215 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4783384 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4795158 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4763613 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4776034 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4746495 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4742817 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4776886 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4796089 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4750207 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4762494 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4744026 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4791118 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4794685 | — | IC50 | = | 38000.0 | nM | 4.42 |