Assay Detail
Binding
CHEMBL2406002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to GST-tagged MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by HTRF assay
12
Total Activities
12
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 RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.53 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402737 | IDASANUTLIN | 3.0 | 1 | 8.22 |
| CHEMBL2386346 | RO-5045337 | 1.0 | 1 | 7.75 |
| CHEMBL2402734 | — | — | 1 | 7.70 |
| CHEMBL2402735 | — | — | 1 | 7.68 |
| CHEMBL2402733 | — | — | 1 | 7.66 |
| CHEMBL2402731 | — | — | 1 | 7.66 |
| CHEMBL2402732 | — | — | 1 | 7.64 |
| CHEMBL2402736 | — | — | 1 | 7.60 |
| CHEMBL2402730 | — | — | 1 | 7.38 |
| CHEMBL2402729 | — | — | 1 | 7.25 |
| CHEMBL2402574 | — | — | 1 | 7.13 |
| CHEMBL2402573 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402737 | IDASANUTLIN | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2386346 | RO-5045337 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2402734 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2402735 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2402733 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2402731 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2402732 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2402736 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2402730 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2402729 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2402574 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2402573 | — | IC50 | = | 196.0 | nM | 6.71 |