Assay Detail
Binding
CHEMBL1919970
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Inhibition of rat recombinant PDE10A expressed in baculovirus infected insect Sf9 cells using [3H]cAMP as substrate after 60 mins by scintillation counting
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL6140) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.02 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562318 | MARDEPODECT | 2.0 | 1 | 9.30 |
| CHEMBL1915747 | — | — | 1 | 9.30 |
| CHEMBL1915725 | — | — | 1 | 8.80 |
| CHEMBL1915727 | — | — | 1 | 8.60 |
| CHEMBL1915726 | — | — | 1 | 8.50 |
| CHEMBL1915742 | — | — | 1 | 8.50 |
| CHEMBL1915746 | — | — | 1 | 8.40 |
| CHEMBL1915736 | — | — | 1 | 8.40 |
| CHEMBL1915729 | — | — | 1 | 8.30 |
| CHEMBL1915733 | — | — | 1 | 8.30 |
| CHEMBL1915730 | — | — | 1 | 8.00 |
| CHEMBL1915738 | — | — | 1 | 8.00 |
| CHEMBL1915734 | — | — | 1 | 7.90 |
| CHEMBL1915737 | — | — | 1 | 7.80 |
| CHEMBL1915735 | — | — | 1 | 7.80 |
| CHEMBL1915743 | — | — | 1 | 7.70 |
| CHEMBL1915728 | — | — | 1 | 7.70 |
| CHEMBL1915741 | — | — | 1 | 7.50 |
| CHEMBL1915732 | — | — | 1 | 7.50 |
| CHEMBL1915744 | — | — | 1 | 7.50 |
| CHEMBL1915745 | — | — | 1 | 7.50 |
| CHEMBL1915739 | — | — | 1 | 7.10 |
| CHEMBL1915740 | — | — | 1 | 7.00 |
| CHEMBL1915731 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562318 | MARDEPODECT | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL1915747 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL1915725 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL1915727 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL1915726 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL1915742 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL1915746 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL1915736 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL1915729 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1915733 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1915730 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1915738 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1915734 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL1915737 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1915735 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL1915743 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1915728 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1915741 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1915732 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1915744 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1915745 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1915739 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1915740 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1915731 | — | IC50 | = | 100.0 | nM | 7.00 |