Assay Detail
Functional
CHEMBL4627016
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 assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay 5HT2A_HUMAN/GRM2_HUMAN P28223/Q14416
34
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 | 34 | 6.01 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638006 | — | — | 2 | 8.21 |
| CHEMBL489624 | — | — | 2 | 8.04 |
| CHEMBL4636980 | — | — | 2 | 7.80 |
| CHEMBL4645193 | — | — | 2 | 6.57 |
| CHEMBL4641860 | — | — | 2 | 6.52 |
| CHEMBL4638687 | — | — | 2 | 6.29 |
| CHEMBL4635373 | — | — | 2 | 6.00 |
| CHEMBL4639821 | — | — | 2 | 5.81 |
| CHEMBL4635960 | — | — | 2 | 5.80 |
| CHEMBL4642761 | — | — | 2 | 5.10 |
| CHEMBL4645305 | — | — | 2 | 5.00 |
| CHEMBL4635729 | — | — | 2 | 5.00 |
| CHEMBL4643961 | — | — | 2 | 5.00 |
| CHEMBL4632373 | — | — | 2 | 5.00 |
| CHEMBL4646835 | — | — | 2 | 5.00 |
| CHEMBL2206440 | — | — | 2 | 5.00 |
| CHEMBL4646555 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638006 | — | IC50 | = | 6.166 | nM | 8.21 |
| CHEMBL4638006 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL489624 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL489624 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4636980 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4636980 | — | IC50 | = | 16.22 | nM | 7.79 |
| CHEMBL4645193 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL4645193 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4641860 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4641860 | — | IC50 | = | 309.03 | nM | 6.51 |
| CHEMBL4638687 | — | IC50 | = | 512.86 | nM | 6.29 |
| CHEMBL4638687 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4635373 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4635373 | — | IC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL4639821 | — | IC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL4635960 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4635960 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4639821 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4642761 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4642761 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4645305 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4646835 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4632373 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4643961 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4635729 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4645305 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4635729 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4643961 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4632373 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4646835 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2206440 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2206440 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4646555 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4646555 | — | IC50 | > | 50000.0 | nM | - |