Assay Detail
Functional
CHEMBL4627009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2A 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
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 |
|---|---|---|---|
| IC50 | 34 | 6.51 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638006 | — | — | 2 | 9.09 |
| CHEMBL4636980 | — | — | 2 | 8.03 |
| CHEMBL489624 | — | — | 2 | 7.96 |
| CHEMBL4638687 | — | — | 2 | 6.57 |
| CHEMBL4639821 | — | — | 2 | 6.55 |
| CHEMBL4641860 | — | — | 2 | 6.52 |
| CHEMBL4645193 | — | — | 2 | 6.39 |
| CHEMBL4635373 | — | — | 2 | 6.35 |
| CHEMBL4635960 | — | — | 2 | 6.29 |
| CHEMBL4646555 | — | — | 2 | 6.14 |
| CHEMBL4642761 | — | — | 2 | 5.92 |
| CHEMBL2206440 | — | — | 2 | 5.89 |
| CHEMBL4643961 | — | — | 2 | 5.41 |
| CHEMBL4646835 | — | — | 2 | 5.39 |
| CHEMBL4635729 | — | — | 2 | 5.22 |
| CHEMBL4645305 | — | — | 2 | - |
| CHEMBL4632373 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638006 | — | IC50 | = | 0.8128 | nM | 9.09 |
| CHEMBL4638006 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4636980 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4636980 | — | IC50 | = | 9.333 | nM | 8.03 |
| CHEMBL489624 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL489624 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4638687 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4638687 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL4639821 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4639821 | — | IC50 | = | 288.4 | nM | 6.54 |
| CHEMBL4641860 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4641860 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4645193 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4645193 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL4635373 | — | IC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4635373 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4635960 | — | IC50 | = | 512.86 | nM | 6.29 |
| CHEMBL4635960 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4646555 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4646555 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL4642761 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4642761 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL2206440 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL2206440 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4643961 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4643961 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4646835 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4646835 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL4635729 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL4635729 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4645305 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4632373 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4632373 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4645305 | — | IC50 | > | 50000.0 | nM | - |