Assay Detail
ADMET
CHEMBL3602291
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Time dependent inhibition of CYP3A4 in human liver microsomes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 8 | 4.99 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3601399 | — | — | 1 | 5.30 |
| CHEMBL3601323 | — | — | 1 | 5.03 |
| CHEMBL3601397 | — | — | 1 | 4.95 |
| CHEMBL3601400 | — | — | 1 | 4.88 |
| CHEMBL3601398 | CGM-097 | 1.0 | 1 | 4.77 |
| CHEMBL3601401 | — | — | 1 | - |
| CHEMBL3601402 | — | — | 1 | - |
| CHEMBL3601403 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3601399 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3601323 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3601397 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL3601400 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL3601398 | CGM-097 | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3601401 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3601402 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3601403 | — | IC50 | > | 20000.0 | nM | - |