Assay Detail
Binding
CHEMBL3614295
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293 cell membranes by radioligand competition binding assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.29 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3613880 | — | — | 1 | 9.19 |
| CHEMBL425285 | — | — | 1 | 8.60 |
| CHEMBL221866 | — | — | 1 | 8.49 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.40 |
| CHEMBL3613879 | — | — | 1 | 8.28 |
| CHEMBL3613874 | — | — | 1 | 8.16 |
| CHEMBL3613878 | — | — | 1 | 8.15 |
| CHEMBL139926 | — | — | 1 | 8.14 |
| CHEMBL373873 | — | — | 1 | 8.13 |
| CHEMBL3613875 | — | — | 1 | 7.82 |
| CHEMBL59725 | — | — | 1 | 7.77 |
| CHEMBL218351 | — | — | 1 | 7.54 |
| CHEMBL346692 | — | — | 1 | 7.51 |
| CHEMBL217981 | — | — | 1 | 7.39 |
| CHEMBL386986 | — | — | 1 | 7.36 |
| CHEMBL3613876 | — | — | 1 | 7.30 |
| CHEMBL221129 | — | — | 1 | 7.21 |
| CHEMBL3613873 | — | — | 1 | 7.08 |
| CHEMBL3613877 | — | — | 1 | 7.05 |
| CHEMBL220754 | — | — | 1 | 7.03 |
| CHEMBL143352 | — | — | 1 | 7.00 |
| CHEMBL218607 | — | — | 1 | 6.96 |
| CHEMBL424294 | — | — | 1 | 6.92 |
| CHEMBL139600 | — | — | 1 | 6.89 |
| CHEMBL437525 | — | — | 1 | 6.85 |
| CHEMBL221587 | — | — | 1 | 6.85 |
| CHEMBL385289 | — | — | 1 | 6.82 |
| CHEMBL140968 | — | — | 1 | 6.66 |
| CHEMBL342060 | — | — | 1 | 6.51 |
| CHEMBL142020 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3613880 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL425285 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL221866 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3613879 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3613874 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL3613878 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL139926 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL373873 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL3613875 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL59725 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL218351 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL346692 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL217981 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL386986 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3613876 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL221129 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3613873 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL3613877 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL220754 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL143352 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL218607 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL424294 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL139600 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL437525 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL221587 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL385289 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL140968 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL342060 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL142020 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL357684 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL141845 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL221843 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL344677 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL124444 | — | Ki | = | 1100.0 | nM | 5.96 |