Assay Detail
Binding
CHEMBL980602
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Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy
16
Total Activities
16
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
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.85 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 8.77 |
| CHEMBL101008 | — | — | 1 | 7.75 |
| CHEMBL6616 | — | — | 1 | 7.72 |
| CHEMBL6607 | BROLAMFETAMINE | 2.0 | 1 | 7.66 |
| CHEMBL6620 | — | — | 1 | 7.48 |
| CHEMBL101189 | — | — | 1 | 7.47 |
| CHEMBL465866 | — | — | 1 | 7.23 |
| CHEMBL8600 | DOM | — | 1 | 7.00 |
| CHEMBL8224 | — | — | 1 | 7.00 |
| CHEMBL464850 | — | — | 1 | 6.75 |
| CHEMBL293399 | — | — | 1 | 6.46 |
| CHEMBL451156 | — | — | 1 | 6.38 |
| CHEMBL99846 | — | — | 1 | 5.70 |
| CHEMBL100626 | — | — | 1 | 5.64 |
| CHEMBL8642 | — | — | 1 | 5.28 |
| CHEMBL26687 | MESCALINE | 1.0 | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267777 | RITANSERIN | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL101008 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL6616 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL6607 | BROLAMFETAMINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL6620 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL101189 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL465866 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL8600 | DOM | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL8224 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL464850 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL293399 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL451156 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL99846 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL100626 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL8642 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL26687 | MESCALINE | Ki | = | 5500.0 | nM | 5.26 |