Assay Detail
Functional
CHEMBL4627010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-expressing Gqo5 assessed as increase in intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
26
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 |
|---|---|---|---|
| EC50 | 26 | 6.02 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643961 | — | — | 2 | 6.92 |
| CHEMBL4646835 | — | — | 2 | 6.77 |
| CHEMBL2206440 | — | — | 2 | 6.68 |
| CHEMBL4632373 | — | — | 2 | 6.68 |
| CHEMBL4645305 | — | — | 2 | 6.58 |
| CHEMBL4635729 | — | — | 2 | 6.55 |
| CHEMBL4645193 | — | — | 1 | 5.00 |
| CHEMBL4646555 | — | — | 1 | 5.00 |
| CHEMBL4642761 | — | — | 1 | 5.00 |
| CHEMBL4639821 | — | — | 1 | 5.00 |
| CHEMBL4635373 | — | — | 1 | 5.00 |
| CHEMBL4638687 | — | — | 1 | 5.00 |
| CHEMBL4641860 | — | — | 1 | 5.00 |
| CHEMBL4635960 | — | — | 1 | 5.00 |
| CHEMBL4636980 | — | — | 2 | - |
| CHEMBL4638006 | — | — | 2 | - |
| CHEMBL489624 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643961 | — | EC50 | = | 120.23 | nM | 6.92 |
| CHEMBL4643961 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4646835 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4646835 | — | EC50 | = | 173.78 | nM | 6.76 |
| CHEMBL2206440 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4632373 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4632373 | — | EC50 | = | 208.93 | nM | 6.68 |
| CHEMBL2206440 | — | EC50 | = | 208.93 | nM | 6.68 |
| CHEMBL4645305 | — | EC50 | = | 263.03 | nM | 6.58 |
| CHEMBL4645305 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4635729 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL4635729 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4635960 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4646555 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4642761 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4639821 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4635373 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4645193 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4641860 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4638687 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL489624 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL489624 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50000.0 | nM | - |