Assay Detail
Binding
CHEMBL1287100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.13 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276948 | — | — | 1 | 7.48 |
| CHEMBL1277312 | — | — | 1 | 7.47 |
| CHEMBL1277770 | — | — | 1 | 7.47 |
| CHEMBL1276947 | — | — | 1 | 7.16 |
| CHEMBL1277126 | — | — | 1 | 6.98 |
| CHEMBL1277935 | — | — | 1 | 6.93 |
| CHEMBL1277678 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276948 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL1277312 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL1277770 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL1276947 | — | Ki | = | 69.18 | nM | 7.16 |
| CHEMBL1277126 | — | Ki | = | 104.71 | nM | 6.98 |
| CHEMBL1277935 | — | Ki | = | 117.49 | nM | 6.93 |
| CHEMBL1277678 | — | Ki | = | 354.81 | nM | 6.45 |