Assay Detail
ADMET
CHEMBL2443949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP3A4 in human liver microsomes using nifedipine 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 | 4.88 | 5.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441342 | — | — | 1 | 5.13 |
| CHEMBL2171124 | — | — | 1 | 5.00 |
| CHEMBL2441340 | — | — | 1 | 4.71 |
| CHEMBL2441346 | — | — | 1 | 4.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441342 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2171124 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2441340 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL2441346 | — | IC50 | = | 20500.0 | nM | 4.69 |