Assay Detail
Binding
CHEMBL4010158
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.72 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069091 | — | — | 1 | 8.59 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.43 |
| CHEMBL4091155 | — | — | 1 | 8.31 |
| CHEMBL4091064 | — | — | 1 | 8.25 |
| CHEMBL4060403 | — | — | 1 | 8.20 |
| CHEMBL4072821 | — | — | 1 | 7.11 |
| CHEMBL4060461 | — | — | 2 | 7.04 |
| CHEMBL4105030 | — | — | 1 | 7.03 |
| CHEMBL4069145 | — | — | 1 | 7.00 |
| CHEMBL4063235 | — | — | 1 | 6.96 |
| CHEMBL4096353 | — | — | 1 | 6.92 |
| CHEMBL4087187 | — | — | 1 | 6.75 |
| CHEMBL4098803 | — | — | 1 | 6.68 |
| CHEMBL4099711 | — | — | 1 | 6.60 |
| CHEMBL4088639 | — | — | 1 | 6.52 |
| CHEMBL4063282 | — | — | 1 | 6.51 |
| CHEMBL4098236 | — | — | 1 | 6.46 |
| CHEMBL4070091 | — | — | 1 | 6.42 |
| CHEMBL4079301 | — | — | 1 | 6.39 |
| CHEMBL4071868 | — | — | 1 | 6.06 |
| CHEMBL4102616 | — | — | 1 | 5.96 |
| CHEMBL4080762 | — | — | 1 | 5.96 |
| CHEMBL4078348 | — | — | 1 | 5.92 |
| CHEMBL4067439 | — | — | 1 | 5.82 |
| CHEMBL4094869 | — | — | 1 | 5.80 |
| CHEMBL4098859 | — | — | 1 | 5.80 |
| CHEMBL4097330 | — | — | 1 | 5.70 |
| CHEMBL4090208 | — | — | 1 | 5.66 |
| CHEMBL4071185 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069091 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4091155 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4091064 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL4060403 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4072821 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4060461 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL4105030 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL4060461 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4069145 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4063235 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4096353 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4087187 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL4098803 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4099711 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4088639 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL4063282 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4098236 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL4070091 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL4079301 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL4071868 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL4102616 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4080762 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4078348 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL4067439 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4094869 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4098859 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4097330 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4090208 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4071185 | — | Ki | = | 2300.0 | nM | 5.64 |