Assay Detail
Binding
CHEMBL4627017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human HT2A receptor expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting method
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT<sub>2A</sub>/mGlu<sub>2</sub> Receptor Complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.37 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638006 | — | — | 2 | 9.28 |
| CHEMBL4636980 | — | — | 2 | 8.53 |
| CHEMBL4639821 | — | — | 2 | 7.48 |
| CHEMBL4641860 | — | — | 2 | 7.10 |
| CHEMBL4638687 | — | — | 2 | 7.00 |
| CHEMBL4645193 | — | — | 2 | 6.96 |
| CHEMBL4635373 | — | — | 2 | 6.89 |
| CHEMBL4635960 | — | — | 2 | 6.70 |
| CHEMBL4642761 | — | — | 2 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638006 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL4638006 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL4636980 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL4636980 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4639821 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4639821 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL4641860 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL4641860 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL4638687 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4638687 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4645193 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4645193 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL4635373 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4635373 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL4635960 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4635960 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4642761 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL4642761 | — | Ki | = | 363.08 | nM | 6.44 |