Assay Detail
Binding
CHEMBL4627018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human 5HT2A/mGlu2 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 | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 (CHEMBL4630758) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 7.15 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638006 | — | — | 2 | 8.52 |
| CHEMBL4636980 | — | — | 2 | 8.19 |
| CHEMBL4641860 | — | — | 2 | 7.16 |
| CHEMBL4639821 | — | — | 2 | 7.00 |
| CHEMBL4645193 | — | — | 2 | 6.94 |
| CHEMBL4638687 | — | — | 2 | 6.93 |
| CHEMBL4635960 | — | — | 2 | 6.78 |
| CHEMBL4635373 | — | — | 2 | 6.75 |
| CHEMBL4642761 | — | — | 2 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638006 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL4638006 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4636980 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4636980 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL4641860 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4641860 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL4639821 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4639821 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL4645193 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL4638687 | — | Ki | = | 117.49 | nM | 6.93 |
| CHEMBL4638687 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4645193 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4635960 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL4635960 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4635373 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL4635373 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL4642761 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL4642761 | — | Ki | = | 831.76 | nM | 6.08 |