Assay Detail
Binding
CHEMBL3243058
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to GST-thrombin-tagged human MDM2 (1 to 188) expressed in Escherichia coli assessed as inhibition of interaction with p53 in serum free buffer incubated for 20 mins prior to p53 addition measured after 60 mins by HTRF assay
22
Total Activities
22
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
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 9.09 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125537 | — | — | 1 | 10.00 |
| CHEMBL3233123 | — | — | 1 | 9.52 |
| CHEMBL3233126 | — | — | 1 | 9.52 |
| CHEMBL3233127 | — | — | 1 | 9.40 |
| CHEMBL3233140 | — | — | 1 | 9.40 |
| CHEMBL3233137 | — | — | 1 | 9.40 |
| CHEMBL3233125 | — | — | 1 | 9.30 |
| CHEMBL3233139 | — | — | 1 | 9.30 |
| CHEMBL3233130 | — | — | 1 | 9.30 |
| CHEMBL3233124 | — | — | 1 | 9.22 |
| CHEMBL3233122 | — | — | 1 | 9.10 |
| CHEMBL3233133 | — | — | 1 | 9.05 |
| CHEMBL3233134 | — | — | 1 | 9.05 |
| CHEMBL3233131 | — | — | 1 | 9.00 |
| CHEMBL3233136 | — | — | 1 | 8.96 |
| CHEMBL3233121 | — | — | 1 | 8.96 |
| CHEMBL3233129 | — | — | 1 | 8.89 |
| CHEMBL3233138 | — | — | 1 | 8.70 |
| CHEMBL3233141 | — | — | 1 | 8.70 |
| CHEMBL3233128 | — | — | 1 | 8.52 |
| CHEMBL3233132 | — | — | 1 | 8.30 |
| CHEMBL3233135 | — | — | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125537 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3233123 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3233126 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3233127 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3233140 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3233137 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3233125 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3233139 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3233130 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3233124 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3233122 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3233133 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3233134 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3233131 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3233136 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3233121 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3233129 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3233138 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3233141 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3233128 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3233132 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3233135 | — | IC50 | = | 5.0 | nM | 8.30 |