Assay Detail
Functional
CHEMBL4729690
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Antiproliferative activity against human U251 cells overexpressing EPHA2 assessed as reduction in cell viability incubated for 48 hrs by MTT assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Dimeric small molecule agonists of EphA2 receptor inhibit glioblastoma cell growth.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.10 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800258 | — | — | 1 | 5.80 |
| CHEMBL4743476 | — | — | 1 | 5.72 |
| CHEMBL4170029 | — | — | 1 | 5.68 |
| CHEMBL4760980 | — | — | 1 | 5.61 |
| CHEMBL4795916 | — | — | 1 | 5.57 |
| CHEMBL4791067 | — | — | 1 | 5.52 |
| CHEMBL4763314 | — | — | 1 | 5.50 |
| CHEMBL4796707 | — | — | 1 | 5.47 |
| CHEMBL4763068 | — | — | 1 | 5.36 |
| CHEMBL4797934 | — | — | 1 | 5.30 |
| CHEMBL4743448 | — | — | 1 | 5.29 |
| CHEMBL4785494 | — | — | 1 | 5.25 |
| CHEMBL4757701 | — | — | 1 | 5.17 |
| CHEMBL4782528 | — | — | 1 | 5.13 |
| CHEMBL4784904 | — | — | 1 | 5.13 |
| CHEMBL4780785 | — | — | 1 | 5.00 |
| CHEMBL188679 | — | — | 1 | 4.95 |
| CHEMBL4168909 | — | — | 1 | 4.92 |
| CHEMBL366103 | — | — | 1 | 4.90 |
| CHEMBL4759706 | — | — | 1 | 4.84 |
| CHEMBL4764123 | — | — | 1 | 4.78 |
| CHEMBL4788507 | — | — | 1 | 4.58 |
| CHEMBL4800241 | — | — | 1 | 4.56 |
| CHEMBL4788996 | — | — | 1 | 4.55 |
| CHEMBL4778844 | — | — | 1 | 4.52 |
| CHEMBL4752577 | — | — | 1 | 4.38 |
| CHEMBL4758346 | — | — | 1 | 4.29 |
| CHEMBL4758535 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800258 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4743476 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4170029 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4760980 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL4795916 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4791067 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4763314 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL4796707 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL4763068 | — | IC50 | = | 4410.0 | nM | 5.36 |
| CHEMBL4797934 | — | IC50 | = | 4990.0 | nM | 5.30 |
| CHEMBL4743448 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL4785494 | — | IC50 | = | 5660.0 | nM | 5.25 |
| CHEMBL4757701 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL4782528 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL4784904 | — | IC50 | = | 7410.0 | nM | 5.13 |
| CHEMBL4780785 | — | IC50 | = | 9920.0 | nM | 5.00 |
| CHEMBL188679 | — | IC50 | = | 11140.0 | nM | 4.95 |
| CHEMBL4168909 | — | IC50 | = | 12060.0 | nM | 4.92 |
| CHEMBL366103 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4759706 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL4764123 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL4788507 | — | IC50 | = | 26430.0 | nM | 4.58 |
| CHEMBL4800241 | — | IC50 | = | 27410.0 | nM | 4.56 |
| CHEMBL4788996 | — | IC50 | = | 27990.0 | nM | 4.55 |
| CHEMBL4778844 | — | IC50 | = | 30440.0 | nM | 4.52 |
| CHEMBL4752577 | — | IC50 | = | 41410.0 | nM | 4.38 |
| CHEMBL4758346 | — | IC50 | = | 51860.0 | nM | 4.29 |
| CHEMBL4758535 | — | IC50 | = | 122300.0 | nM | - |