Assay Detail
Binding
CHEMBL5739044
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Inhibition for Dopamine D3 Receptor: Buffer solution: 50 mM Tris-HCl (35409-45, Nacalai Tesque) (pH 7.4) containing 120 mM NaCl (31320-05, Nacalai Tesque), 1 mM MgCl.6HO (20909-55, Nacalai Tesque), 5 mM KCl (28514-75, Nacalai Tesque) and 2 mM CaCl) (067-31, NAKARAI CHEMICALS, LTD.) Radioligand: (final concentration) 2 nM [H]-Methylspiperone ([H���N-methyl-]-Methylspiperone, NET-856, 83.8 Ci/mmol, PerkinElmer)Non-specific ligand: (final concentration) 10 uM Butaclamol [(+)-Butaclamol Hydrochloride, D033, Sigma] SPA beads solution: SPA beads [WGA PVT SPA Scintillation Beads, RPNQ0001 (500 mg), RPNQ0060 (2 g), PerkinElmer] (0.2 mg/well) Incubation time and temperature: 120 min at 25° C.
687
Total Activities
224
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Condensed ring compounds having dopamine D3 receptor antagonistic effect
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 229 | 9.61 | 10.80 |
| kon | 229 | - | - |
| k_off | 229 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5924177 | — | — | 3 | 10.80 |
| CHEMBL5870203 | — | — | 3 | 10.60 |
| CHEMBL5975724 | — | — | 6 | 10.54 |
| CHEMBL5949574 | — | — | 6 | 10.47 |
| CHEMBL5964833 | — | — | 3 | 10.46 |
| CHEMBL6060696 | — | — | 3 | 10.41 |
| CHEMBL5841988 | — | — | 3 | 10.37 |
| CHEMBL5875273 | — | — | 3 | 10.36 |
| CHEMBL5951227 | — | — | 3 | 10.32 |
| CHEMBL6047349 | — | — | 3 | 10.24 |
| CHEMBL6006998 | — | — | 3 | 10.20 |
| CHEMBL5849356 | — | — | 3 | 10.15 |
| CHEMBL5833883 | — | — | 3 | 10.15 |
| CHEMBL5957439 | — | — | 3 | 10.15 |
| CHEMBL6025855 | — | — | 3 | 10.14 |
| CHEMBL6049838 | — | — | 3 | 10.11 |
| CHEMBL6045711 | — | — | 3 | 10.10 |
| CHEMBL5968576 | — | — | 3 | 10.09 |
| CHEMBL5928686 | — | — | 3 | 10.09 |
| CHEMBL5755159 | — | — | 3 | 10.08 |
| CHEMBL5837758 | — | — | 3 | 10.08 |
| CHEMBL5766722 | — | — | 3 | 10.07 |
| CHEMBL5787390 | — | — | 3 | 10.07 |
| CHEMBL6021169 | — | — | 3 | 10.05 |
| CHEMBL6013919 | — | — | 3 | 10.05 |
| CHEMBL5843758 | — | — | 3 | 10.02 |
| CHEMBL6012333 | — | — | 3 | 10.01 |
| CHEMBL6040249 | — | — | 3 | 10.00 |
| CHEMBL5898048 | — | — | 3 | 10.00 |
| CHEMBL5987260 | — | — | 3 | 10.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5924177 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL5870203 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL5975724 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL5975724 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL5949574 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL5964833 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL6060696 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL5841988 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL5875273 | — | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL5951227 | — | Ki | = | 0.048 | nM | 10.32 |
| CHEMBL6047349 | — | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL6006998 | — | Ki | = | 0.063 | nM | 10.20 |
| CHEMBL5957439 | — | Ki | = | 0.071 | nM | 10.15 |
| CHEMBL5833883 | — | Ki | = | 0.071 | nM | 10.15 |
| CHEMBL5849356 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL6025855 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL5949574 | — | Ki | = | 0.072 | nM | 10.14 |
| CHEMBL6049838 | — | Ki | = | 0.078 | nM | 10.11 |
| CHEMBL6045711 | — | Ki | = | 0.079 | nM | 10.10 |
| CHEMBL5968576 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL5928686 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL5755159 | — | Ki | = | 0.083 | nM | 10.08 |
| CHEMBL5837758 | — | Ki | = | 0.084 | nM | 10.08 |
| CHEMBL5787390 | — | Ki | = | 0.085 | nM | 10.07 |
| CHEMBL5766722 | — | Ki | = | 0.086 | nM | 10.07 |
| CHEMBL6021169 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL6013919 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL5843758 | — | Ki | = | 0.095 | nM | 10.02 |
| CHEMBL6012333 | — | Ki | = | 0.097 | nM | 10.01 |
| CHEMBL5987260 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL5898048 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL6040249 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL5970185 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL6036651 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL5776224 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL5972904 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL5886479 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL6058309 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL5823979 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5811527 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5886479 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL6010116 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5791870 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5750440 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5870651 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5750695 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL6053782 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL5754091 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL5955136 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL5861015 | — | Ki | = | 0.13 | nM | 9.89 |