Assay Detail
Binding
CHEMBL3243059
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Binding affinity to GST-thrombin-tagged human MDM2 (1 to 188) expressed in Escherichia coli assessed as inhibition of interaction with p53 in buffer containing 15% human serum 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 | 8.31 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233141 | — | — | 1 | 9.30 |
| CHEMBL3125537 | — | — | 1 | 8.96 |
| CHEMBL3233140 | — | — | 1 | 8.74 |
| CHEMBL3233125 | — | — | 1 | 8.70 |
| CHEMBL3233130 | — | — | 1 | 8.70 |
| CHEMBL3233137 | — | — | 1 | 8.68 |
| CHEMBL3233123 | — | — | 1 | 8.64 |
| CHEMBL3233126 | — | — | 1 | 8.62 |
| CHEMBL3233138 | — | — | 1 | 8.60 |
| CHEMBL3233122 | — | — | 1 | 8.43 |
| CHEMBL3233127 | — | — | 1 | 8.40 |
| CHEMBL3233139 | — | — | 1 | 8.29 |
| CHEMBL3233124 | — | — | 1 | 8.22 |
| CHEMBL3233136 | — | — | 1 | 8.16 |
| CHEMBL3233134 | — | — | 1 | 8.00 |
| CHEMBL3233129 | — | — | 1 | 8.00 |
| CHEMBL3233121 | — | — | 1 | 7.96 |
| CHEMBL3233133 | — | — | 1 | 7.77 |
| CHEMBL3233131 | — | — | 1 | 7.75 |
| CHEMBL3233132 | — | — | 1 | 7.70 |
| CHEMBL3233135 | — | — | 1 | 7.64 |
| CHEMBL3233128 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233141 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3125537 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3233140 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3233125 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3233130 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3233137 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3233123 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3233126 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3233138 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3233122 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3233127 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3233139 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3233124 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3233136 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3233134 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3233129 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL3233121 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3233133 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3233131 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3233132 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3233135 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3233128 | — | IC50 | = | 26.0 | nM | 7.58 |