Assay Detail
Binding
CHEMBL2182644
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Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SJSA-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.42 | 6.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2059435 | — | — | 1 | 6.12 |
| CHEMBL2177191 | — | — | 1 | 5.82 |
| CHEMBL2177189 | — | — | 1 | 5.80 |
| CHEMBL2059300 | — | — | 1 | 5.72 |
| CHEMBL2177188 | — | — | 1 | 5.51 |
| CHEMBL2177187 | — | — | 1 | 5.37 |
| CHEMBL2177190 | — | — | 1 | 5.26 |
| CHEMBL191334 | NUTLIN-3 | — | 1 | 5.15 |
| CHEMBL2177186 | — | — | 1 | 4.97 |
| CHEMBL2177813 | — | — | 1 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2059435 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2177191 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2177189 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2059300 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2177188 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2177187 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2177190 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL191334 | NUTLIN-3 | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2177186 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL2177813 | — | IC50 | = | 34400.0 | nM | 4.46 |