Assay Detail
Binding
CHEMBL3268063
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Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step radiometric assay
22
Total Activities
22
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
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.17 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562318 | MARDEPODECT | 2.0 | 1 | 9.43 |
| CHEMBL562513 | — | — | 1 | 8.85 |
| CHEMBL3262297 | — | — | 1 | 7.98 |
| CHEMBL3262293 | — | — | 1 | 7.95 |
| CHEMBL3262298 | — | — | 1 | 7.62 |
| CHEMBL3262303 | — | — | 1 | 7.48 |
| CHEMBL3262291 | — | — | 1 | 7.38 |
| CHEMBL3262294 | — | — | 1 | 7.17 |
| CHEMBL3262295 | — | — | 1 | 7.16 |
| CHEMBL3262290 | — | — | 1 | 6.91 |
| CHEMBL3262292 | — | — | 1 | 6.72 |
| CHEMBL3262296 | — | — | 1 | 6.23 |
| CHEMBL3262302 | — | — | 1 | 6.01 |
| CHEMBL3262300 | — | — | 1 | 5.49 |
| CHEMBL3262299 | — | — | 1 | 5.23 |
| CHEMBL3262285 | — | — | 1 | - |
| CHEMBL3262289 | — | — | 1 | - |
| CHEMBL3262286 | — | — | 1 | - |
| CHEMBL3262284 | — | — | 1 | - |
| CHEMBL3262288 | — | — | 1 | - |
| CHEMBL3262301 | — | — | 1 | - |
| CHEMBL3262287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562318 | MARDEPODECT | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL562513 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL3262297 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3262293 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL3262298 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL3262303 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL3262291 | — | IC50 | = | 41.5 | nM | 7.38 |
| CHEMBL3262294 | — | IC50 | = | 67.4 | nM | 7.17 |
| CHEMBL3262295 | — | IC50 | = | 68.5 | nM | 7.16 |
| CHEMBL3262290 | — | IC50 | = | 123.2 | nM | 6.91 |
| CHEMBL3262292 | — | IC50 | = | 188.2 | nM | 6.72 |
| CHEMBL3262296 | — | IC50 | = | 592.1 | nM | 6.23 |
| CHEMBL3262302 | — | IC50 | = | 971.2 | nM | 6.01 |
| CHEMBL3262300 | — | IC50 | = | 3217.2 | nM | 5.49 |
| CHEMBL3262299 | — | IC50 | = | 5936.8 | nM | 5.23 |
| CHEMBL3262285 | — | IC50 | - | — | - | |
| CHEMBL3262289 | — | IC50 | - | — | - | |
| CHEMBL3262286 | — | IC50 | - | — | - | |
| CHEMBL3262284 | — | IC50 | - | — | - | |
| CHEMBL3262288 | — | IC50 | - | — | - | |
| CHEMBL3262301 | — | IC50 | - | — | - | |
| CHEMBL3262287 | — | IC50 | - | — | - |