Assay Detail
Functional
CHEMBL4222628
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Antagonist activity at human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium release preincubated for 15 mins followed by 5-HT addition measured every 1.7 secs for 60 secs by calcium 4 dye-based FLIPR assay
16
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HT2A receptor (5-HT2AR) antagonist M100907.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.55 | 8.32 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL74355 | VOLINANSERIN | 3.0 | 3 | 8.32 |
| CHEMBL4227912 | — | — | 2 | 7.53 |
| CHEMBL4227059 | — | — | 3 | 7.44 |
| CHEMBL4226407 | — | — | 2 | 7.40 |
| CHEMBL4228313 | — | — | 3 | 7.33 |
| CHEMBL4226858 | — | — | 3 | 7.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL74355 | VOLINANSERIN | IC50 | = | 4.786 | nM | 8.32 |
| CHEMBL74355 | VOLINANSERIN | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4227912 | — | IC50 | = | 29.51 | nM | 7.53 |
| CHEMBL4227912 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4227059 | — | IC50 | = | 36.31 | nM | 7.44 |
| CHEMBL4227059 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL4226407 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4226407 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4228313 | — | IC50 | = | 46.77 | nM | 7.33 |
| CHEMBL4228313 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL4226858 | — | IC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4226858 | — | IC50 | = | 56.6 | nM | 7.25 |
| CHEMBL74355 | VOLINANSERIN | Inhibition | - | % | - | |
| CHEMBL4228313 | — | Inhibition | - | % | - | |
| CHEMBL4226858 | — | Inhibition | - | % | - | |
| CHEMBL4227059 | — | Inhibition | - | % | - |