Assay Detail
Functional
CHEMBL4627007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive modulator activity at human mGlu2 receptor expressed in HEK293 cells co-expressing Gqo5 assessed as increase in intracellular Ca2+ mobilization incubated for 1 hr in presence of EC20 glutamate 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 | 7.16 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206440 | — | — | 2 | 8.28 |
| CHEMBL4632373 | — | — | 2 | 8.10 |
| CHEMBL4645305 | — | — | 2 | 8.06 |
| CHEMBL4643961 | — | — | 2 | 8.05 |
| CHEMBL4646835 | — | — | 2 | 8.00 |
| CHEMBL4635729 | — | — | 2 | 7.94 |
| CHEMBL4646555 | — | — | 2 | 7.10 |
| CHEMBL4642761 | — | — | 2 | 6.50 |
| CHEMBL4641860 | — | — | 2 | 6.50 |
| CHEMBL4639821 | — | — | 2 | 6.49 |
| CHEMBL4635960 | — | — | 2 | 6.32 |
| CHEMBL4635373 | — | — | 2 | 6.29 |
| CHEMBL4645193 | — | — | 2 | 6.29 |
| CHEMBL4638687 | — | — | 2 | 6.28 |
| CHEMBL4636980 | — | — | 2 | - |
| CHEMBL4638006 | — | — | 2 | - |
| CHEMBL489624 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206440 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL2206440 | — | EC50 | = | 5.248 | nM | 8.28 |
| CHEMBL4632373 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4632373 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4645305 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4645305 | — | EC50 | = | 8.71 | nM | 8.06 |
| CHEMBL4643961 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4643961 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL4646835 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4646835 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4635729 | — | EC50 | = | 11.48 | nM | 7.94 |
| CHEMBL4635729 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4646555 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4646555 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4642761 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4641860 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4642761 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4641860 | — | EC50 | = | 323.59 | nM | 6.49 |
| CHEMBL4639821 | — | EC50 | = | 323.59 | nM | 6.49 |
| CHEMBL4639821 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4635960 | — | EC50 | = | 478.63 | nM | 6.32 |
| CHEMBL4635960 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4635373 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL4645193 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL4645193 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4635373 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4638687 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4638687 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL489624 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50118.72 | nM | - |
| CHEMBL489624 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4636980 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4638006 | — | EC50 | > | 50000.0 | nM | - |