Assay Detail
Functional
CHEMBL4627005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 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
34
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 34 | 6.31 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206440 | — | — | 2 | 7.45 |
| CHEMBL4646835 | — | — | 2 | 6.80 |
| CHEMBL4643961 | — | — | 2 | 6.68 |
| CHEMBL4635729 | — | — | 2 | 6.64 |
| CHEMBL4645305 | — | — | 2 | 6.54 |
| CHEMBL4632373 | — | — | 2 | 6.52 |
| CHEMBL4646555 | — | — | 2 | 6.36 |
| CHEMBL4639821 | — | — | 2 | 6.26 |
| CHEMBL4642761 | — | — | 2 | 6.05 |
| CHEMBL4638687 | — | — | 2 | 5.92 |
| CHEMBL4641860 | — | — | 2 | 5.92 |
| CHEMBL4645193 | — | — | 2 | 5.81 |
| CHEMBL4635373 | — | — | 2 | 5.81 |
| CHEMBL4635960 | — | — | 2 | 5.61 |
| CHEMBL4638006 | — | — | 2 | - |
| CHEMBL489624 | — | — | 2 | - |
| CHEMBL4636980 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206440 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL2206440 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4646835 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4646835 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4643961 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4643961 | — | EC50 | = | 213.8 | nM | 6.67 |
| CHEMBL4635729 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4635729 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL4645305 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4645305 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL4632373 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4632373 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4646555 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4646555 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4639821 | — | EC50 | = | 549.54 | nM | 6.26 |
| CHEMBL4639821 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4642761 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4642761 | — | EC50 | = | 912.01 | nM | 6.04 |
| CHEMBL4641860 | — | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL4641860 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4638687 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4638687 | — | EC50 | = | 1230.27 | nM | 5.91 |
| CHEMBL4645193 | — | EC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL4635373 | — | EC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL4635373 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4645193 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4635960 | — | EC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL4635960 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL489624 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL489624 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50118.72 | nM | - |