Assay Detail
Binding
CHEMBL5164653
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-FAM labeled PDI peptide from MDM2 (1 to 118 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant incubated for 1.5 hrs by fluorescence polarization competition assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| Ki | 46 | 8.29 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171665 | — | — | 1 | 9.30 |
| CHEMBL5197279 | — | — | 1 | 9.10 |
| CHEMBL5181559 | — | — | 1 | 8.96 |
| CHEMBL5173513 | — | — | 1 | 8.89 |
| CHEMBL5169689 | — | — | 1 | 8.85 |
| CHEMBL5196857 | — | — | 1 | 8.80 |
| CHEMBL5196069 | — | — | 1 | 8.80 |
| CHEMBL5205792 | — | — | 1 | 8.80 |
| CHEMBL5181296 | — | — | 1 | 8.80 |
| CHEMBL5207803 | — | — | 1 | 8.77 |
| CHEMBL5179430 | — | — | 1 | 8.74 |
| CHEMBL5173985 | — | — | 1 | 8.70 |
| CHEMBL5185334 | — | — | 1 | 8.70 |
| CHEMBL5185988 | — | — | 1 | 8.68 |
| CHEMBL5176086 | — | — | 1 | 8.66 |
| CHEMBL5195734 | — | — | 1 | 8.64 |
| CHEMBL5199459 | — | — | 1 | 8.64 |
| CHEMBL5183808 | — | — | 1 | 8.62 |
| CHEMBL5200925 | — | — | 1 | 8.60 |
| CHEMBL5190459 | — | — | 1 | 8.60 |
| CHEMBL5186698 | — | — | 1 | 8.59 |
| CHEMBL5188708 | — | — | 1 | 8.57 |
| CHEMBL5194615 | — | — | 1 | 8.57 |
| CHEMBL5191798 | — | — | 1 | 8.54 |
| CHEMBL5196353 | — | — | 1 | 8.51 |
| CHEMBL5186741 | — | — | 1 | 8.47 |
| CHEMBL5184577 | — | — | 1 | 8.44 |
| CHEMBL5204732 | — | — | 1 | 8.43 |
| CHEMBL5183859 | — | — | 1 | 8.42 |
| CHEMBL5181817 | — | — | 1 | 8.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171665 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL5197279 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL5181559 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL5173513 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5169689 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL5196857 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5196069 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5205792 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5181296 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5207803 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL5179430 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL5173985 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5185334 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5185988 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5176086 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL5195734 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5199459 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5183808 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL5200925 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL5190459 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL5186698 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL5188708 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5194615 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5191798 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL5196353 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL5186741 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL5184577 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL5204732 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL5183859 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL5181817 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL5170763 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL5179684 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL5194658 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL5203433 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5206418 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL5200857 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL5187542 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL5185313 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL5198421 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL5197590 | — | Ki | = | 34.1 | nM | 7.47 |
| CHEMBL191334 | NUTLIN-3 | Ki | = | 38.6 | nM | 7.41 |
| CHEMBL5206008 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL5180266 | — | Ki | = | 54.3 | nM | 7.26 |
| CHEMBL5180602 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL5201050 | — | Ki | = | 50200.0 | nM | 4.30 |
| CHEMBL5187340 | — | Ki | = | 0.0019 | nM | - |