Assay Detail
Binding
CHEMBL3370341
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Binding affinity to human GST-thrombin-tagged MDM2 assessed as inhibition of interaction with human p53 after 1 hr by HTRF assay in presence of 15% human serum
33
Total Activities
33
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
Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 9.75 | 10.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318783 | — | — | 1 | 10.23 |
| CHEMBL3318761 | — | — | 1 | 10.23 |
| CHEMBL3318768 | — | — | 1 | 10.15 |
| CHEMBL3318781 | — | — | 1 | 10.13 |
| CHEMBL3318771 | — | — | 1 | 10.12 |
| CHEMBL3318756 | — | — | 1 | 10.10 |
| CHEMBL3318758 | — | — | 1 | 10.09 |
| CHEMBL3318762 | — | — | 1 | 10.07 |
| CHEMBL3318782 | — | — | 1 | 10.06 |
| CHEMBL3318764 | — | — | 1 | 10.04 |
| CHEMBL3318767 | — | — | 1 | 10.02 |
| CHEMBL3318760 | — | — | 1 | 10.01 |
| CHEMBL3318757 | — | — | 1 | 9.96 |
| CHEMBL3318769 | — | — | 1 | 9.92 |
| CHEMBL3318786 | — | — | 1 | 9.92 |
| CHEMBL3318763 | — | — | 1 | 9.92 |
| CHEMBL3318779 | — | — | 1 | 9.82 |
| CHEMBL3318765 | — | — | 1 | 9.82 |
| CHEMBL3318770 | — | — | 1 | 9.80 |
| CHEMBL3318759 | — | — | 1 | 9.77 |
| CHEMBL3318787 | — | — | 1 | 9.66 |
| CHEMBL3318775 | — | — | 1 | 9.62 |
| CHEMBL3318773 | — | — | 1 | 9.52 |
| CHEMBL3318774 | — | — | 1 | 9.51 |
| CHEMBL3318784 | — | — | 1 | 9.43 |
| CHEMBL3318777 | — | — | 1 | 9.42 |
| CHEMBL3318776 | — | — | 1 | 9.40 |
| CHEMBL3318785 | — | — | 1 | 9.38 |
| CHEMBL3318778 | — | — | 1 | 9.33 |
| CHEMBL3318772 | — | — | 1 | 9.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318783 | — | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL3318761 | — | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL3318768 | — | IC50 | = | 0.071 | nM | 10.15 |
| CHEMBL3318781 | — | IC50 | = | 0.074 | nM | 10.13 |
| CHEMBL3318771 | — | IC50 | = | 0.075 | nM | 10.12 |
| CHEMBL3318756 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL3318758 | — | IC50 | = | 0.081 | nM | 10.09 |
| CHEMBL3318762 | — | IC50 | = | 0.086 | nM | 10.07 |
| CHEMBL3318782 | — | IC50 | = | 0.088 | nM | 10.06 |
| CHEMBL3318764 | — | IC50 | = | 0.091 | nM | 10.04 |
| CHEMBL3318767 | — | IC50 | = | 0.096 | nM | 10.02 |
| CHEMBL3318760 | — | IC50 | = | 0.098 | nM | 10.01 |
| CHEMBL3318757 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3318763 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3318786 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3318769 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3318779 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3318765 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3318770 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3318759 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3318787 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3318775 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3318773 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3318774 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3318784 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL3318777 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL3318776 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3318785 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL3318778 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL3318772 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL3318766 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL3318755 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3318780 | — | IC50 | = | 1.1 | nM | 8.96 |