Assay Detail
Binding
CHEMBL5732166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
D2 Receptor Antagonism Activity Test: The D2 receptor antagonism activity test (The antagonism activity of test compounds on D2 receptor expressing human recombinant D2 receptor in HEK293 cells) was performed using LANCE cAMP 384 Kit (Product of USA PerkinElmer Inc.). The D2 antagonism activity of test compounds was evaluated through their inhibition on dopamine-induced decrease of cAMP production in HEK293 cells. cAMP concentration test was performed according to the method documented in the kit instructions. The concentration of the test compounds was 0.1 nM-10000 nM, risperidone was used as a positive control, IC50 value was calculated by the Excelfit software
288
Total Activities
94
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterocyclic compounds, process for preparation of the same and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 96 | 7.58 | 8.97 |
| kon | 96 | - | - |
| k_off | 96 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5851827 | — | — | 3 | 8.97 |
| CHEMBL5923077 | — | — | 3 | 8.73 |
| CHEMBL6045510 | — | — | 3 | 8.70 |
| CHEMBL4083333 | — | — | 3 | 8.58 |
| CHEMBL5988023 | — | — | 3 | 8.53 |
| CHEMBL4104261 | — | — | 3 | 8.48 |
| CHEMBL4116744 | — | — | 3 | 8.46 |
| CHEMBL5904347 | — | — | 3 | 8.42 |
| CHEMBL5945545 | — | — | 3 | 8.41 |
| CHEMBL5925148 | — | — | 3 | 8.34 |
| CHEMBL5792929 | — | — | 3 | 8.33 |
| CHEMBL4102670 | — | — | 9 | 8.27 |
| CHEMBL6007113 | — | — | 3 | 8.27 |
| CHEMBL6028182 | — | — | 3 | 8.26 |
| CHEMBL4079251 | — | — | 3 | 8.26 |
| CHEMBL5792875 | — | — | 3 | 8.22 |
| CHEMBL5975067 | — | — | 3 | 8.22 |
| CHEMBL5909924 | — | — | 3 | 8.17 |
| CHEMBL5996307 | — | — | 3 | 8.16 |
| CHEMBL6035657 | — | — | 3 | 8.15 |
| CHEMBL5900385 | — | — | 3 | 8.11 |
| CHEMBL5770003 | — | — | 3 | 8.09 |
| CHEMBL5914239 | — | — | 3 | 8.08 |
| CHEMBL5830707 | — | — | 3 | 8.07 |
| CHEMBL5771063 | — | — | 3 | 8.06 |
| CHEMBL5984307 | — | — | 3 | 8.05 |
| CHEMBL5804051 | — | — | 3 | 8.03 |
| CHEMBL6014626 | — | — | 3 | 8.03 |
| CHEMBL5765721 | — | — | 3 | 7.99 |
| CHEMBL4117823 | — | — | 3 | 7.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5851827 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL5923077 | — | IC50 | = | 1.84 | nM | 8.73 |
| CHEMBL6045510 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL4083333 | — | IC50 | = | 2.61 | nM | 8.58 |
| CHEMBL5988023 | — | IC50 | = | 2.94 | nM | 8.53 |
| CHEMBL4104261 | — | IC50 | = | 3.32 | nM | 8.48 |
| CHEMBL4116744 | — | IC50 | = | 3.51 | nM | 8.46 |
| CHEMBL5904347 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5945545 | — | IC50 | = | 3.87 | nM | 8.41 |
| CHEMBL5925148 | — | IC50 | = | 4.54 | nM | 8.34 |
| CHEMBL5792929 | — | IC50 | = | 4.69 | nM | 8.33 |
| CHEMBL6007113 | — | IC50 | = | 5.32 | nM | 8.27 |
| CHEMBL4102670 | — | IC50 | = | 5.43 | nM | 8.27 |
| CHEMBL4079251 | — | IC50 | = | 5.49 | nM | 8.26 |
| CHEMBL6028182 | — | IC50 | = | 5.46 | nM | 8.26 |
| CHEMBL5792875 | — | IC50 | = | 6.02 | nM | 8.22 |
| CHEMBL5975067 | — | IC50 | = | 5.97 | nM | 8.22 |
| CHEMBL5909924 | — | IC50 | = | 6.81 | nM | 8.17 |
| CHEMBL5996307 | — | IC50 | = | 6.91 | nM | 8.16 |
| CHEMBL4102670 | — | IC50 | = | 6.89 | nM | 8.16 |
| CHEMBL6035657 | — | IC50 | = | 7.06 | nM | 8.15 |
| CHEMBL5900385 | — | IC50 | = | 7.76 | nM | 8.11 |
| CHEMBL5770003 | — | IC50 | = | 8.06 | nM | 8.09 |
| CHEMBL5914239 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5830707 | — | IC50 | = | 8.43 | nM | 8.07 |
| CHEMBL5771063 | — | IC50 | = | 8.62 | nM | 8.06 |
| CHEMBL5984307 | — | IC50 | = | 8.83 | nM | 8.05 |
| CHEMBL6014626 | — | IC50 | = | 9.24 | nM | 8.03 |
| CHEMBL5804051 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5765721 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5885759 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5885838 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4117823 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5774536 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL6048629 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL6045417 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4087246 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL5832082 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5995642 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL6018186 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL5916019 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL4116465 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL5967130 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL5865978 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL4102670 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5997477 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL5785243 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL5890339 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL5763558 | — | IC50 | = | 25.1 | nM | 7.60 |