Assay Detail
Binding
CHEMBL4201979
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human MDM2 (1 to 125 residues) and p53 (unknown origin) interaction pre-incubated for 20 mins before peptide-2-biot addition and measured after 3 hrs by HTRF assay
19
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Target
Tumour suppressor p53/oncoprotein Mdm2 (CHEMBL1907611) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.51 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4203529 | — | — | 2 | 8.51 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 8.46 |
| CHEMBL4218748 | — | — | 1 | 8.00 |
| CHEMBL4207959 | — | — | 2 | 7.62 |
| CHEMBL4217905 | — | — | 1 | 7.48 |
| CHEMBL4209483 | — | — | 2 | 6.52 |
| CHEMBL4211645 | — | — | 1 | 6.46 |
| CHEMBL4212066 | — | — | 1 | 6.21 |
| CHEMBL4203887 | — | — | 2 | 6.18 |
| CHEMBL4206333 | — | — | 2 | 6.15 |
| CHEMBL4210216 | — | — | 1 | 6.13 |
| CHEMBL4212404 | — | — | 1 | 5.90 |
| CHEMBL4205549 | — | — | 1 | 5.47 |
| CHEMBL4214609 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4203529 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL191334 | NUTLIN-3 | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4218748 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4207959 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL4217905 | — | IC50 | = | 33.03 | nM | 7.48 |
| CHEMBL4209483 | — | IC50 | = | 303.5 | nM | 6.52 |
| CHEMBL4211645 | — | IC50 | = | 349.5 | nM | 6.46 |
| CHEMBL4203529 | — | IC50 | = | 538.2 | nM | 6.27 |
| CHEMBL4212066 | — | IC50 | = | 619.0 | nM | 6.21 |
| CHEMBL4203887 | — | IC50 | = | 654.8 | nM | 6.18 |
| CHEMBL4206333 | — | IC50 | = | 712.2 | nM | 6.15 |
| CHEMBL4210216 | — | IC50 | = | 738.8 | nM | 6.13 |
| CHEMBL4203887 | — | IC50 | = | 1039.0 | nM | 5.98 |
| CHEMBL4207959 | — | IC50 | = | 1144.0 | nM | 5.94 |
| CHEMBL4212404 | — | IC50 | = | 1257.0 | nM | 5.90 |
| CHEMBL4206333 | — | IC50 | = | 3032.5 | nM | 5.52 |
| CHEMBL4205549 | — | IC50 | = | 3384.5 | nM | 5.47 |
| CHEMBL4209483 | — | IC50 | = | 3724.7 | nM | 5.43 |
| CHEMBL4214609 | — | IC50 | = | 3680.0 | nM | 5.43 |