Assay Detail
Binding
CHEMBL3887672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Dopamine D2 Receptor Binding Assay: The assay was performed according to the method by Kohler et al. (Kohler C, Hall H, Ogren S O and Gawell L, Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain. Biochem. Pharmacol., 1985; 34: 2251-2259). The binding assay was performed using 40 ul of the membrane specimen, 20 ul of [3H]-raclopride (final concentration 1 to 2 nM), 20 ul of a test drug and 50 mM Tris-hydrochloric acid buffer (containing 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2, pH 7.4) so that the total amount was 200 ul (final dimethylsulfoxide concentration 1%). The reaction was performed at room temperature for 1 hour 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.
60
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| 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 | 60 | 8.88 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907711 | — | — | 2 | 10.00 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 9.70 |
| CHEMBL3966032 | — | — | 1 | 9.70 |
| CHEMBL3893296 | — | — | 1 | 9.70 |
| CHEMBL3901333 | — | — | 1 | 9.40 |
| CHEMBL3953082 | — | — | 1 | 9.40 |
| CHEMBL3945539 | — | — | 1 | 9.30 |
| CHEMBL3974916 | — | — | 1 | 9.30 |
| CHEMBL3931169 | — | — | 1 | 9.30 |
| CHEMBL3936629 | — | — | 1 | 9.22 |
| CHEMBL3962323 | — | — | 1 | 9.15 |
| CHEMBL3965773 | — | — | 1 | 9.15 |
| CHEMBL3939353 | — | — | 1 | 9.15 |
| CHEMBL3899929 | — | — | 1 | 9.10 |
| CHEMBL3969756 | — | — | 1 | 9.10 |
| CHEMBL3969404 | — | — | 1 | 9.10 |
| CHEMBL3905737 | — | — | 1 | 9.10 |
| CHEMBL3960031 | — | — | 1 | 9.00 |
| CHEMBL3932669 | — | — | 1 | 9.00 |
| CHEMBL3942695 | — | — | 1 | 8.96 |
| CHEMBL3929237 | — | — | 1 | 8.92 |
| CHEMBL3915465 | — | — | 1 | 8.92 |
| CHEMBL3905706 | — | — | 1 | 8.92 |
| CHEMBL3948017 | — | — | 1 | 8.92 |
| CHEMBL3920216 | — | — | 1 | 8.92 |
| CHEMBL3941669 | — | — | 1 | 8.89 |
| CHEMBL3981820 | — | — | 1 | 8.85 |
| CHEMBL3935871 | — | — | 1 | 8.85 |
| CHEMBL3985224 | — | — | 1 | 8.82 |
| CHEMBL3956410 | — | — | 1 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907711 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3907711 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3893296 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3966032 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3953082 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3901333 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3945539 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3931169 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3974916 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3936629 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3962323 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3939353 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3965773 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3905737 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3969404 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3899929 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3969756 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3960031 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3932669 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3942695 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3920216 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3948017 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3915465 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3929237 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3905706 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3941669 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3981820 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3935871 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3985224 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3956410 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3911283 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3933730 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3937293 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3958333 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3905367 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3977357 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3898190 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3902274 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3979507 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3976061 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3980869 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3889759 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3893739 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3969878 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3909275 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3918214 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3892225 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3890947 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3903749 | — | Ki | = | 3.3 | nM | 8.48 |