Assay Detail
Binding
CHEMBL3602283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MDM2/p53 interaction (unknown origin) using biotinylated MDM2 and Cy5-p53 (18 to 26 amino acids) by TR-FRET assay
18
Total Activities
18
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 a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.35 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3601323 | — | — | 1 | 8.96 |
| CHEMBL3601399 | — | — | 1 | 8.80 |
| CHEMBL3601397 | — | — | 1 | 8.80 |
| CHEMBL3601398 | CGM-097 | 1.0 | 1 | 8.77 |
| CHEMBL3601396 | — | — | 1 | 8.77 |
| CHEMBL3601322 | — | — | 1 | 8.72 |
| CHEMBL3601402 | — | — | 1 | 8.70 |
| CHEMBL3601317 | — | — | 1 | 8.64 |
| CHEMBL3601401 | — | — | 1 | 8.60 |
| CHEMBL3601321 | — | — | 1 | 8.52 |
| CHEMBL3601320 | — | — | 1 | 8.52 |
| CHEMBL3601319 | — | — | 1 | 8.40 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 8.39 |
| CHEMBL3601403 | — | — | 1 | 8.12 |
| CHEMBL3601316 | — | — | 1 | 8.10 |
| CHEMBL3601400 | — | — | 1 | 7.94 |
| CHEMBL3601324 | — | — | 1 | 7.70 |
| CHEMBL3601318 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3601323 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3601399 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3601397 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3601398 | CGM-097 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3601396 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3601322 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3601402 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3601317 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3601401 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3601321 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3601320 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3601319 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL191334 | NUTLIN-3 | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3601403 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3601316 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3601400 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL3601324 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3601318 | — | IC50 | = | 1171.0 | nM | 5.93 |