Assay Detail
Binding
CHEMBL3607773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of p53-MDM2 interaction (unknown origin) by TR-FRET assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Tumour suppressor p53/oncoprotein Mdm2 (CHEMBL1907611) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.97 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3601317 | — | — | 1 | 8.64 |
| CHEMBL3601316 | — | — | 1 | 8.10 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 8.00 |
| CHEMBL3604664 | — | — | 1 | 7.82 |
| CHEMBL3604663 | — | — | 1 | 6.92 |
| CHEMBL3604661 | — | — | 1 | 6.92 |
| CHEMBL3604662 | — | — | 1 | 6.77 |
| CHEMBL3604660 | — | — | 1 | 6.42 |
| CHEMBL3604658 | — | — | 1 | 6.27 |
| CHEMBL3604659 | — | — | 1 | 6.00 |
| CHEMBL3601318 | — | — | 1 | 5.92 |
| CHEMBL3603849 | — | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3601317 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3601316 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL191334 | NUTLIN-3 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3604664 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3604663 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3604661 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3604662 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3604660 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3604658 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3604659 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3601318 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3603849 | — | IC50 | = | 1400.0 | nM | 5.85 |