Assay Detail
ADMET
CHEMBL5546192
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Inhibition of CYP3A4 in human liver microsomes using midazolam substrate incubated for 5 mins in presence of NADPH by UPLC-MS/MS analysis
8
Total Activities
8
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 HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.94 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571568 | — | — | 1 | 5.60 |
| CHEMBL5571377 | — | — | 1 | 5.60 |
| CHEMBL5579682 | — | — | 1 | 5.29 |
| CHEMBL5574976 | — | — | 1 | 4.92 |
| CHEMBL5591595 | — | — | 1 | 4.60 |
| CHEMBL5593998 | — | — | 1 | 4.57 |
| CHEMBL5593039 | — | — | 1 | 4.48 |
| CHEMBL5569981 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571568 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5571377 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5579682 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5574976 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5591595 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5593998 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL5593039 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5569981 | — | IC50 | = | 33000.0 | nM | 4.48 |