Assay Detail
Binding
CHEMBL3132469
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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
19
Total Activities
19
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
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.40 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125527 | — | — | 1 | 8.96 |
| CHEMBL3125529 | — | — | 1 | 8.96 |
| CHEMBL3125531 | — | — | 1 | 8.89 |
| CHEMBL3125526 | — | — | 1 | 8.85 |
| CHEMBL3125530 | — | — | 1 | 8.80 |
| CHEMBL3125524 | — | — | 1 | 8.80 |
| CHEMBL3125522 | — | — | 1 | 8.80 |
| CHEMBL3125525 | — | — | 1 | 8.77 |
| CHEMBL3125528 | — | — | 1 | 8.74 |
| CHEMBL3125523 | — | — | 1 | 8.47 |
| CHEMBL3125532 | — | — | 1 | 8.42 |
| CHEMBL2059435 | — | — | 1 | 8.39 |
| CHEMBL3125705 | — | — | 1 | 8.33 |
| CHEMBL3125706 | — | — | 1 | 8.25 |
| CHEMBL3125707 | — | — | 1 | 8.19 |
| CHEMBL3125709 | — | — | 1 | 7.66 |
| CHEMBL3125708 | — | — | 1 | 7.66 |
| CHEMBL3125703 | — | — | 1 | 7.50 |
| CHEMBL3125704 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125527 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3125529 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3125531 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3125526 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3125530 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3125524 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3125522 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3125525 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3125528 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3125523 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3125532 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2059435 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3125705 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3125706 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3125707 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3125709 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3125708 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3125703 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3125704 | — | IC50 | = | 62.4 | nM | 7.21 |