Assay Detail
Functional
CHEMBL5362135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCT-116 cells overexpressing MDM2 assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
39
Total Activities
39
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 novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 4.97 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5418298 | — | — | 1 | 6.17 |
| CHEMBL5426939 | — | — | 1 | 6.14 |
| CHEMBL5416654 | — | — | 1 | 5.65 |
| CHEMBL5422731 | — | — | 1 | 5.40 |
| CHEMBL5430787 | — | — | 1 | 5.38 |
| CHEMBL5437839 | — | — | 1 | 5.21 |
| CHEMBL5417713 | — | — | 1 | 5.11 |
| CHEMBL5400761 | — | — | 1 | 5.05 |
| CHEMBL5400500 | — | — | 1 | 5.00 |
| CHEMBL5409375 | — | — | 1 | 4.99 |
| CHEMBL5428948 | — | — | 1 | 4.98 |
| CHEMBL5413374 | — | — | 1 | 4.96 |
| CHEMBL2152332 | — | — | 1 | 4.95 |
| CHEMBL5422030 | — | — | 1 | 4.93 |
| CHEMBL5433819 | — | — | 1 | 4.92 |
| CHEMBL5422264 | — | — | 1 | 4.91 |
| CHEMBL5403978 | — | — | 1 | 4.88 |
| CHEMBL5439731 | — | — | 1 | 4.87 |
| CHEMBL5395339 | — | — | 1 | 4.85 |
| CHEMBL5394884 | — | — | 1 | 4.85 |
| CHEMBL5396791 | — | — | 1 | 4.85 |
| CHEMBL5403300 | — | — | 1 | 4.81 |
| CHEMBL5418384 | — | — | 1 | 4.81 |
| CHEMBL5439641 | — | — | 1 | 4.79 |
| CHEMBL5416279 | — | — | 1 | 4.78 |
| CHEMBL5426013 | — | — | 1 | 4.78 |
| CHEMBL5419081 | — | — | 1 | 4.73 |
| CHEMBL5420518 | — | — | 1 | 4.73 |
| CHEMBL5413250 | — | — | 1 | 4.72 |
| CHEMBL5407048 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5418298 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5426939 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5416654 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL5422731 | — | IC50 | = | 3970.0 | nM | 5.40 |
| CHEMBL5430787 | — | IC50 | = | 4210.0 | nM | 5.38 |
| CHEMBL5437839 | — | IC50 | = | 6240.0 | nM | 5.21 |
| CHEMBL5417713 | — | IC50 | = | 7690.0 | nM | 5.11 |
| CHEMBL5400761 | — | IC50 | = | 8860.0 | nM | 5.05 |
| CHEMBL5400500 | — | IC50 | = | 9980.0 | nM | 5.00 |
| CHEMBL5409375 | — | IC50 | = | 10140.0 | nM | 4.99 |
| CHEMBL5428948 | — | IC50 | = | 10410.0 | nM | 4.98 |
| CHEMBL5413374 | — | IC50 | = | 11050.0 | nM | 4.96 |
| CHEMBL2152332 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL5422030 | — | IC50 | = | 11690.0 | nM | 4.93 |
| CHEMBL5433819 | — | IC50 | = | 12040.0 | nM | 4.92 |
| CHEMBL5422264 | — | IC50 | = | 12350.0 | nM | 4.91 |
| CHEMBL5403978 | — | IC50 | = | 13270.0 | nM | 4.88 |
| CHEMBL5439731 | — | IC50 | = | 13540.0 | nM | 4.87 |
| CHEMBL5396791 | — | IC50 | = | 14020.0 | nM | 4.85 |
| CHEMBL5394884 | — | IC50 | = | 14220.0 | nM | 4.85 |
| CHEMBL5395339 | — | IC50 | = | 14130.0 | nM | 4.85 |
| CHEMBL5403300 | — | IC50 | = | 15580.0 | nM | 4.81 |
| CHEMBL5418384 | — | IC50 | = | 15420.0 | nM | 4.81 |
| CHEMBL5439641 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL5416279 | — | IC50 | = | 16620.0 | nM | 4.78 |
| CHEMBL5426013 | — | IC50 | = | 16430.0 | nM | 4.78 |
| CHEMBL5419081 | — | IC50 | = | 18530.0 | nM | 4.73 |
| CHEMBL5420518 | — | IC50 | = | 18780.0 | nM | 4.73 |
| CHEMBL5413250 | — | IC50 | = | 18930.0 | nM | 4.72 |
| CHEMBL5407048 | — | IC50 | = | 19550.0 | nM | 4.71 |
| CHEMBL5394970 | — | IC50 | = | 21530.0 | nM | 4.67 |
| CHEMBL5408349 | — | IC50 | = | 21930.0 | nM | 4.66 |
| CHEMBL5408490 | — | IC50 | = | 29180.0 | nM | 4.54 |
| CHEMBL5422314 | — | IC50 | = | 30110.0 | nM | 4.52 |
| CHEMBL5406435 | — | IC50 | = | 33010.0 | nM | 4.48 |
| CHEMBL5433851 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5403465 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5434849 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5406939 | — | IC50 | > | 40000.0 | nM | - |