Assay Detail
Binding
CHEMBL3887673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Serotonin 5-HT2A Receptor Binding Assay: The assay was performed according to the method by Leysen J E et al. (Leysen J E, Niemegeers C J E, Van Nueten J M and Laduron P M. [3H] Ketanserin (R 41 468), a selective 3H-ligand for serotonin 2 receptor binding sites. Mol. Pharmacol., 1982, 21: 301-314). The binding assay was performed using 40 ul of the membrane specimen, 20 ul of [3H]-Ketanserin (final concentration 1 to 3 nM), 20 ul of a test drug and 50 mM Tris-hydrochloric acid buffer (pH 7.4) so that the total amount was 200 ul (final dimethylsulfoxide concentration 1%). The reaction was performed at 37° C. for 20 minutes and terminated by conducting suction filtration with a cell harvester on a glass fiber filter plate.The filter plate made of glass fiber was washed with 50 mM Tris-hydrochloric acid buffer (pH 7.4), and after dried, a microplate liquid scintillation cocktail was added and the radioactivity was measured with a microplate scintillation counter.
62
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Piperazine-substituted benzothiophenes for treatment of mental disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 62 | 8.46 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3958663 | — | — | 1 | 9.22 |
| CHEMBL3930364 | — | — | 1 | 9.00 |
| CHEMBL3915465 | — | — | 1 | 8.92 |
| CHEMBL3934217 | — | — | 1 | 8.89 |
| CHEMBL3904588 | — | — | 1 | 8.89 |
| CHEMBL3982910 | — | — | 1 | 8.82 |
| CHEMBL3905706 | — | — | 1 | 8.82 |
| CHEMBL3939353 | — | — | 1 | 8.77 |
| CHEMBL3965773 | — | — | 1 | 8.70 |
| CHEMBL3932669 | — | — | 1 | 8.68 |
| CHEMBL3948017 | — | — | 1 | 8.68 |
| CHEMBL3933730 | — | — | 1 | 8.68 |
| CHEMBL3907711 | — | — | 2 | 8.68 |
| CHEMBL3907815 | — | — | 1 | 8.64 |
| CHEMBL3945539 | — | — | 1 | 8.64 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 8.64 |
| CHEMBL3956410 | — | — | 1 | 8.60 |
| CHEMBL3957163 | — | — | 1 | 8.59 |
| CHEMBL3969404 | — | — | 1 | 8.59 |
| CHEMBL3902274 | — | — | 1 | 8.55 |
| CHEMBL3929237 | — | — | 1 | 8.55 |
| CHEMBL3902391 | — | — | 1 | 8.54 |
| CHEMBL3903749 | — | — | 1 | 8.54 |
| CHEMBL3905737 | — | — | 1 | 8.54 |
| CHEMBL3901333 | — | — | 1 | 8.52 |
| CHEMBL3976061 | — | — | 1 | 8.52 |
| CHEMBL3907222 | — | — | 1 | 8.51 |
| CHEMBL3905367 | — | — | 1 | 8.51 |
| CHEMBL3977357 | — | — | 1 | 8.49 |
| CHEMBL3985224 | — | — | 1 | 8.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3958663 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3930364 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3915465 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3934217 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3904588 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3982910 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3905706 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3939353 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3965773 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3932669 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3948017 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3933730 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3907711 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3945539 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3907815 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3956410 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3969404 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3957163 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3902274 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3929237 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3905737 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3903749 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3902391 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3976061 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3901333 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3905367 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3907222 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3977357 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3893296 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3980869 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3985224 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3961721 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3966032 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3931169 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3953447 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3892796 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3893739 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3916814 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL3935871 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3944717 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3974916 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL3909275 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3944691 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL3953082 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3912487 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3907711 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3958333 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3899929 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3941669 | — | Ki | = | 6.3 | nM | 8.20 |