Assay Detail
ADMET
CHEMBL4675900
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP2C19 in human liver microsomes using probe substrate and in presence of co-factor preincubated for 20 mins followed by substrate addition by LC-MS/MS analysis
2
Total Activities
2
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 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 4.74 | 4.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3717363 | — | — | 1 | 4.74 |
| CHEMBL3716365 | GLPG-1205 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3717363 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL3716365 | GLPG-1205 | IC50 | > | 100000.0 | nM | - |