Assay Detail
ADMET
CHEMBL4140834
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Inhibition of CYP2C9 in human liver microsomes using diclofenac 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 | 4.59 | 4.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4160748 | — | — | 1 | 4.61 |
| CHEMBL4165248 | — | — | 1 | 4.57 |
| CHEMBL2361777 | — | — | 1 | - |
| CHEMBL4168668 | — | — | 1 | - |
| CHEMBL4172016 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4160748 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL4165248 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2361777 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4168668 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4172016 | — | IC50 | > | 30000.0 | nM | - |