Assay Detail
Binding
CHEMBL5146493
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DAPT from human 5-HT1A receptor expressed in CHO-K1 cells membrane by scintillation counter analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.33 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187742 | — | — | 1 | 8.79 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 8.30 |
| CHEMBL5185101 | — | — | 1 | 8.09 |
| CHEMBL5173329 | — | — | 1 | 7.97 |
| CHEMBL5209272 | — | — | 1 | 7.74 |
| CHEMBL5199182 | — | — | 1 | 7.68 |
| CHEMBL5182578 | — | — | 1 | 7.52 |
| CHEMBL5190746 | — | — | 1 | 7.49 |
| CHEMBL5195574 | — | — | 1 | 7.08 |
| CHEMBL5197186 | — | — | 1 | 7.06 |
| CHEMBL5209283 | — | — | 1 | 6.94 |
| CHEMBL5197377 | — | — | 1 | 6.61 |
| CHEMBL5208347 | — | — | 1 | 6.61 |
| CHEMBL5179632 | — | — | 1 | 6.60 |
| CHEMBL5189417 | — | — | 1 | 6.44 |
| CHEMBL5176063 | — | — | 1 | 6.33 |
| CHEMBL5194148 | — | — | 1 | - |
| CHEMBL5175846 | — | — | 1 | - |
| CHEMBL5178019 | — | — | 1 | - |
| CHEMBL5179661 | — | — | 1 | - |
| CHEMBL5189541 | — | — | 1 | - |
| CHEMBL5193064 | — | — | 1 | - |
| CHEMBL5198889 | — | — | 1 | - |
| CHEMBL5193580 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187742 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL49 | BUSPIRONE | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL5185101 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL5173329 | — | Ki | = | 10.72 | nM | 7.97 |
| CHEMBL5209272 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL5199182 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL5182578 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5190746 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL5195574 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL5197186 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL5209283 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL5197377 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL5208347 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL5179632 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL5189417 | — | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL5176063 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL5194148 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5175846 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5178019 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5179661 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5189541 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5193064 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5198889 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5193580 | — | Ki | > | 1000.0 | nM | - |