Assay Detail
Binding
CHEMBL805830
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In vitro binding affinity towards serotonin 5-HT2A receptor in rat cortical membranes using [3H]ketanserin as radioligand
20
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.91 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337226 | — | — | 1 | 9.05 |
| CHEMBL133104 | — | — | 1 | 9.00 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 8.77 |
| CHEMBL134423 | — | — | 4 | 8.70 |
| CHEMBL135898 | — | — | 1 | 8.47 |
| CHEMBL134351 | — | — | 1 | 8.00 |
| CHEMBL134502 | — | — | 1 | 7.85 |
| CHEMBL134964 | — | — | 1 | 7.75 |
| CHEMBL134394 | — | — | 2 | 7.70 |
| CHEMBL335615 | — | — | 1 | 7.60 |
| CHEMBL134804 | — | — | 1 | 7.54 |
| CHEMBL335616 | — | — | 1 | 7.48 |
| CHEMBL133430 | — | — | 1 | 7.34 |
| CHEMBL335029 | — | — | 1 | 7.28 |
| CHEMBL134065 | — | — | 1 | 7.10 |
| CHEMBL336401 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337226 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL133104 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL267777 | RITANSERIN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL134423 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL134423 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL135898 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL134351 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL134502 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL134423 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL134964 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL134394 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL335615 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL134423 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL134394 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL134804 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL335616 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL133430 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL335029 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL134065 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL336401 | — | IC50 | = | 100.0 | nM | 7.00 |