Assay Detail
ADMET
CHEMBL4140833
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate preincubated for 15 mins followed by NADPH addition measured after 8 mins by LC-MS/MS analysis
5
Total Activities
5
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 VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.75 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4165248 | — | — | 1 | 6.48 |
| CHEMBL2361777 | — | — | 1 | 6.16 |
| CHEMBL4172016 | — | — | 1 | 5.53 |
| CHEMBL4160748 | — | — | 1 | 5.51 |
| CHEMBL4168668 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4165248 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2361777 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4172016 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL4160748 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL4168668 | — | IC50 | = | 8670.0 | nM | 5.06 |