Assay Detail
Functional
CHEMBL5334710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human 5-HT2A receptor expressed in cell membrane assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT<sub>2A</sub> Receptor Inverse Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.30 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 7.90 |
| CHEMBL5414080 | — | — | 1 | 7.10 |
| CHEMBL5414859 | — | — | 1 | 7.10 |
| CHEMBL5403965 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5414080 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5414859 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5403965 | — | IC50 | = | 79.4 | nM | 7.10 |