Assay Detail
Binding
CHEMBL3369961
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE10A (amino acids 14 to 779) using [3H]-labelled cyclic nucleotide as substrate after 1 hr b beta counting
13
Total Activities
13
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 SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.97 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562513 | — | — | 1 | 9.52 |
| CHEMBL3317682 | — | — | 1 | 7.40 |
| CHEMBL3317688 | — | — | 1 | 7.40 |
| CHEMBL3317687 | — | — | 1 | 7.38 |
| CHEMBL1642578 | — | — | 1 | 7.30 |
| CHEMBL3317689 | — | — | 1 | 7.26 |
| CHEMBL3317683 | — | — | 1 | 6.77 |
| CHEMBL3317686 | — | — | 1 | 6.72 |
| CHEMBL3317684 | — | — | 1 | 6.66 |
| CHEMBL3317690 | — | — | 1 | 6.32 |
| CHEMBL3317691 | — | — | 1 | 6.05 |
| CHEMBL3317692 | — | — | 1 | 6.00 |
| CHEMBL3317685 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562513 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3317682 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3317688 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3317687 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1642578 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3317689 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3317683 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3317686 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3317684 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3317690 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3317691 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3317692 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3317685 | — | IC50 | = | 1300.0 | nM | 5.89 |