Assay Detail
Functional
CHEMBL3369685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Target occupancy of PDE10A in Sprague-Dawley rat striatum measured 1 hr post dosing and 10 mins post iv dosing of tracer by LC-MS/MS method
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Occ | 3 | - | - |
| EC50 | 3 | 6.36 | 6.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3319207 | — | — | 2 | 6.93 |
| CHEMBL3319209 | — | — | 2 | 6.15 |
| CHEMBL3319210 | — | — | 2 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3319207 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL3319209 | — | EC50 | = | 711.0 | nM | 6.15 |
| CHEMBL3319210 | — | EC50 | = | 965.0 | nM | 6.01 |
| CHEMBL3319210 | — | Occ | - | — | - | |
| CHEMBL3319209 | — | Occ | - | — | - | |
| CHEMBL3319207 | — | Occ | - | — | - |