Assay Detail
Functional
CHEMBL4627014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-expressing Gqo5 assessed as inhibition of glutamate-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay 5HT2A_HUMAN/GRM2_HUMAN P28223/Q14416
27
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 27 | 6.41 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489624 | — | — | 2 | 7.64 |
| CHEMBL4638006 | — | — | 2 | 7.62 |
| CHEMBL4636980 | — | — | 2 | 7.54 |
| CHEMBL4645193 | — | — | 2 | 6.18 |
| CHEMBL4635960 | — | — | 2 | 6.16 |
| CHEMBL4638687 | — | — | 2 | 6.05 |
| CHEMBL4639821 | — | — | 2 | 6.00 |
| CHEMBL4641860 | — | — | 2 | 5.93 |
| CHEMBL4635373 | — | — | 2 | 5.72 |
| CHEMBL4642761 | — | — | 2 | 5.28 |
| CHEMBL4632373 | — | — | 1 | - |
| CHEMBL4643961 | — | — | 1 | - |
| CHEMBL4635729 | — | — | 1 | - |
| CHEMBL4645305 | — | — | 1 | - |
| CHEMBL4646555 | — | — | 1 | - |
| CHEMBL4646835 | — | — | 1 | - |
| CHEMBL2206440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489624 | — | IC50 | = | 22.91 | nM | 7.64 |
| CHEMBL489624 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4638006 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4638006 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL4636980 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4636980 | — | IC50 | = | 28.84 | nM | 7.54 |
| CHEMBL4645193 | — | IC50 | = | 660.69 | nM | 6.18 |
| CHEMBL4645193 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4635960 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4635960 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4638687 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4638687 | — | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL4639821 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4639821 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4641860 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL4641860 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4635373 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4635373 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL4642761 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4642761 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL2206440 | — | IC50 | - | — | - | |
| CHEMBL4646835 | — | IC50 | - | — | - | |
| CHEMBL4632373 | — | IC50 | - | — | - | |
| CHEMBL4643961 | — | IC50 | - | — | - | |
| CHEMBL4635729 | — | IC50 | - | — | - | |
| CHEMBL4645305 | — | IC50 | - | — | - | |
| CHEMBL4646555 | — | IC50 | - | — | - |