Assay Detail
Binding
CHEMBL2091389
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Inhibition of MDM2 binding domain assessed as inhibition of p53 binding to MDM2 after 1 hr by fluorescence polarization assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.82 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2089208 | — | — | 1 | 7.05 |
| CHEMBL2089203 | — | — | 1 | 7.04 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 6.92 |
| CHEMBL2089201 | — | — | 1 | 6.50 |
| CHEMBL2089211 | — | — | 1 | 6.29 |
| CHEMBL2089152 | — | — | 1 | 6.15 |
| CHEMBL2089151 | — | — | 1 | 6.14 |
| CHEMBL2089209 | — | — | 1 | 5.98 |
| CHEMBL2089149 | — | — | 1 | 5.86 |
| CHEMBL2089200 | — | — | 1 | 5.76 |
| CHEMBL2089204 | — | — | 1 | 5.52 |
| CHEMBL2089210 | — | — | 1 | 5.40 |
| CHEMBL1909836 | — | — | 1 | 5.17 |
| CHEMBL2089202 | — | — | 1 | 5.09 |
| CHEMBL2089320 | — | — | 1 | 4.92 |
| CHEMBL2089322 | — | — | 1 | 4.68 |
| CHEMBL2089207 | — | — | 1 | 4.42 |
| CHEMBL2089206 | — | — | 1 | - |
| CHEMBL2089321 | — | — | 1 | - |
| CHEMBL2089205 | — | — | 1 | - |
| CHEMBL2089153 | — | — | 1 | - |
| CHEMBL2089150 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2089208 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL2089203 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL191334 | NUTLIN-3 | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL2089201 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL2089211 | — | Ki | = | 518.0 | nM | 6.29 |
| CHEMBL2089152 | — | Ki | = | 707.0 | nM | 6.15 |
| CHEMBL2089151 | — | Ki | = | 721.0 | nM | 6.14 |
| CHEMBL2089209 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL2089149 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL2089200 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL2089204 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL2089210 | — | Ki | = | 3980.0 | nM | 5.40 |
| CHEMBL1909836 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL2089202 | — | Ki | = | 8180.0 | nM | 5.09 |
| CHEMBL2089320 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL2089322 | — | Ki | = | 21100.0 | nM | 4.68 |
| CHEMBL2089207 | — | Ki | = | 37700.0 | nM | 4.42 |
| CHEMBL2089206 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2089321 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2089205 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2089153 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2089150 | — | Ki | > | 100000.0 | nM | - |