Assay Detail
Binding
CHEMBL1646316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE10A expressed in Sf9 cells using [3H]cAMP by scintillation proximity assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL4409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.38 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642569 | — | — | 1 | 9.74 |
| CHEMBL1641615 | — | — | 1 | 7.92 |
| CHEMBL1642568 | — | — | 1 | 7.80 |
| CHEMBL1642581 | — | — | 1 | 7.80 |
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 7.77 |
| CHEMBL1642583 | — | — | 1 | 7.51 |
| CHEMBL1642582 | — | — | 1 | 7.43 |
| CHEMBL1642570 | — | — | 1 | 7.32 |
| CHEMBL1642578 | — | — | 1 | 7.30 |
| CHEMBL1642580 | — | — | 1 | 7.30 |
| CHEMBL1642579 | — | — | 1 | 7.28 |
| CHEMBL1642571 | — | — | 1 | 7.14 |
| CHEMBL1642577 | — | — | 1 | 7.12 |
| CHEMBL1642585 | — | — | 1 | 7.11 |
| CHEMBL1642574 | — | — | 1 | 7.08 |
| CHEMBL1642575 | — | — | 1 | 7.00 |
| CHEMBL1642573 | — | — | 1 | 6.96 |
| CHEMBL1642572 | — | — | 1 | 6.89 |
| CHEMBL1642576 | — | — | 1 | 6.80 |
| CHEMBL1642584 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642569 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL1641615 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1642568 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1642581 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL19224 | PAPAVERINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1642583 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1642582 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1642570 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1642578 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1642580 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1642579 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1642571 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1642577 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1642585 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1642574 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1642575 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1642573 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1642572 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1642576 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1642584 | — | IC50 | = | 430.0 | nM | 6.37 |