Assay Detail
Binding
CHEMBL3742723
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Inhibition of human recombinant PDE10A1 expressed in baculovirus infected insect SF21 cells using [3H]cAMP as substrate after 30 mins by scintillation proximity assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.95 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3741573 | — | — | 1 | 10.43 |
| CHEMBL3741841 | — | — | 1 | 10.32 |
| CHEMBL3742354 | — | — | 1 | 9.96 |
| CHEMBL3741950 | — | — | 1 | 9.92 |
| CHEMBL3739783 | — | — | 1 | 9.48 |
| CHEMBL3741781 | — | — | 1 | 9.39 |
| CHEMBL3741660 | — | — | 1 | 9.34 |
| CHEMBL3741492 | — | — | 1 | 9.06 |
| CHEMBL3741207 | — | — | 1 | 9.00 |
| CHEMBL3741064 | — | — | 1 | 8.80 |
| CHEMBL3741518 | — | — | 1 | 8.77 |
| CHEMBL3739662 | — | — | 1 | 8.53 |
| CHEMBL3741528 | — | — | 1 | 8.50 |
| CHEMBL3741850 | — | — | 1 | 8.48 |
| CHEMBL3741836 | — | — | 1 | 7.99 |
| CHEMBL219445 | — | — | 1 | 7.80 |
| CHEMBL3742381 | — | — | 1 | 7.69 |
| CHEMBL3741213 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3741573 | — | IC50 | = | 0.037 | nM | 10.43 |
| CHEMBL3741841 | — | IC50 | = | 0.048 | nM | 10.32 |
| CHEMBL3742354 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3741950 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3739783 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3741781 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL3741660 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL3741492 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL3741207 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL3741064 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL3741518 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL3739662 | — | IC50 | = | 2.95 | nM | 8.53 |
| CHEMBL3741528 | — | IC50 | = | 3.18 | nM | 8.50 |
| CHEMBL3741850 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3741836 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL219445 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3742381 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL3741213 | — | IC50 | = | 26.3 | nM | 7.58 |