Assay Detail
Binding
CHEMBL3584693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membranes by radioligand binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEKT |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.42 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.75 |
| CHEMBL3581255 | — | — | 1 | 6.67 |
| CHEMBL3580670 | — | — | 1 | 6.62 |
| CHEMBL3581250 | — | — | 1 | 6.61 |
| CHEMBL3581245 | — | — | 1 | 6.57 |
| CHEMBL3581254 | — | — | 1 | 6.42 |
| CHEMBL3581249 | — | — | 1 | 6.42 |
| CHEMBL3581256 | — | — | 1 | 6.38 |
| CHEMBL3581251 | — | — | 1 | 6.35 |
| CHEMBL3581246 | — | — | 1 | 6.24 |
| CHEMBL3581252 | — | — | 1 | 6.24 |
| CHEMBL3581253 | — | — | 1 | 6.24 |
| CHEMBL3581248 | — | — | 1 | 6.12 |
| CHEMBL3581244 | — | — | 1 | 6.09 |
| CHEMBL228082 | GLAUCINE | — | 1 | 6.01 |
| CHEMBL3581247 | — | — | 1 | 5.94 |
| CHEMBL464099 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3581255 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL3580670 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL3581250 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL3581245 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL3581254 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL3581249 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL3581256 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL3581251 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL3581246 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL3581252 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL3581253 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL3581248 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL3581244 | — | Ki | = | 818.0 | nM | 6.09 |
| CHEMBL228082 | GLAUCINE | Ki | = | 966.0 | nM | 6.01 |
| CHEMBL3581247 | — | Ki | = | 1156.0 | nM | 5.94 |
| CHEMBL464099 | — | Ki | - | — | - |