Assay Detail
Functional
CHEMBL5164634
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Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.54 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5179430 | — | — | 1 | 7.36 |
| CHEMBL5181559 | — | — | 1 | 7.29 |
| CHEMBL5196857 | — | — | 1 | 7.22 |
| CHEMBL5205792 | — | — | 1 | 6.83 |
| CHEMBL5176086 | — | — | 1 | 6.82 |
| CHEMBL5188708 | — | — | 1 | 6.65 |
| CHEMBL5169689 | — | — | 1 | 6.57 |
| CHEMBL5199459 | — | — | 1 | 6.51 |
| CHEMBL5173513 | — | — | 1 | 6.48 |
| CHEMBL5197279 | — | — | 1 | 6.31 |
| CHEMBL5200857 | — | — | 1 | 6.20 |
| CHEMBL5195734 | — | — | 1 | 6.14 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 5.87 |
| CHEMBL5190459 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5179430 | — | IC50 | = | 43.3 | nM | 7.36 |
| CHEMBL5181559 | — | IC50 | = | 50.7 | nM | 7.29 |
| CHEMBL5196857 | — | IC50 | = | 60.1 | nM | 7.22 |
| CHEMBL5205792 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5176086 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL5188708 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL5169689 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL5199459 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL5173513 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL5197279 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL5200857 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL5195734 | — | IC50 | = | 719.0 | nM | 6.14 |
| CHEMBL191334 | NUTLIN-3 | IC50 | = | 1366.0 | nM | 5.87 |
| CHEMBL5190459 | — | IC50 | = | 4665.0 | nM | 5.33 |