Assay Detail
Binding
CHEMBL1827309
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE10A assessed as reduction in hydrolysis of [3H]cAMP by scintillation proximity assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.85 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 7.68 |
| CHEMBL1821790 | — | — | 1 | 7.55 |
| CHEMBL1821791 | — | — | 1 | 7.31 |
| CHEMBL1821774 | — | — | 1 | 7.31 |
| CHEMBL1821787 | — | — | 1 | 7.26 |
| CHEMBL1821789 | — | — | 1 | 7.26 |
| CHEMBL1821775 | — | — | 1 | 7.23 |
| CHEMBL1821776 | — | — | 1 | 6.95 |
| CHEMBL1821777 | — | — | 1 | 6.70 |
| CHEMBL1821784 | — | — | 1 | 6.70 |
| CHEMBL1821779 | — | — | 1 | 6.62 |
| CHEMBL1821778 | — | — | 1 | 6.61 |
| CHEMBL1821788 | — | — | 1 | 6.61 |
| CHEMBL1821782 | — | — | 1 | 6.61 |
| CHEMBL1821785 | — | — | 1 | 6.58 |
| CHEMBL1821786 | — | — | 1 | 6.52 |
| CHEMBL1821783 | — | — | 1 | 6.33 |
| CHEMBL1821780 | — | — | 1 | 6.30 |
| CHEMBL1821781 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19224 | PAPAVERINE | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1821790 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1821791 | — | IC50 | = | 48.8 | nM | 7.31 |
| CHEMBL1821774 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1821787 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1821789 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1821775 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL1821776 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL1821777 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL1821784 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1821779 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL1821778 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL1821788 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL1821782 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL1821785 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL1821786 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL1821783 | — | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL1821780 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1821781 | — | IC50 | = | 872.0 | nM | 6.06 |