Assay Detail
Functional
CHEMBL5324930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human D4 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.94 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.10 |
| CHEMBL5403504 | — | — | 1 | 8.66 |
| CHEMBL5437265 | — | — | 1 | 8.21 |
| CHEMBL2037521 | — | — | 1 | 7.72 |
| CHEMBL5400876 | — | — | 1 | 7.59 |
| CHEMBL5394387 | — | — | 1 | 7.28 |
| CHEMBL3289656 | — | — | 1 | 7.15 |
| CHEMBL5436702 | — | — | 1 | 6.98 |
| CHEMBL5406300 | — | — | 1 | 6.91 |
| CHEMBL5399689 | — | — | 1 | 6.61 |
| CHEMBL5425920 | — | — | 1 | 6.56 |
| CHEMBL5434856 | — | — | 1 | 6.48 |
| CHEMBL5400983 | — | — | 1 | 6.42 |
| CHEMBL5426481 | — | — | 1 | 6.38 |
| CHEMBL5399720 | — | — | 1 | 6.14 |
| CHEMBL5422150 | — | — | 1 | 5.64 |
| CHEMBL5403610 | — | — | 1 | 5.63 |
| CHEMBL5403986 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5403504 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5437265 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2037521 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL5400876 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL5394387 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL3289656 | — | IC50 | = | 71.5 | nM | 7.15 |
| CHEMBL5436702 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5406300 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5399689 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL5425920 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL5434856 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL5400983 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL5426481 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL5399720 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL5422150 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL5403610 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL5403986 | — | IC50 | = | 3260.0 | nM | 5.49 |