Assay Detail
ADMET
CHEMBL2444388
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Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 5 to 60 mins by LC-MS/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.89 | 5.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171124 | — | — | 1 | 5.35 |
| CHEMBL2441342 | — | — | 1 | 4.72 |
| CHEMBL2441340 | — | — | 1 | 4.61 |
| CHEMBL2441346 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171124 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2441342 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL2441340 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL2441346 | — | IC50 | > | 25000.0 | nM | - |