Assay Detail
Binding
CHEMBL2060920
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Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
30
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D₁ receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.18 | 8.60 |
| Ki | 15 | 7.45 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62 | SCH-23390 | — | 2 | 8.91 |
| CHEMBL2057455 | — | — | 2 | 8.60 |
| CHEMBL487387 | STEPHOLIDINE | — | 2 | 8.21 |
| CHEMBL2057445 | — | — | 2 | 8.10 |
| CHEMBL2057456 | — | — | 2 | 7.76 |
| CHEMBL2057446 | — | — | 2 | 7.62 |
| CHEMBL2057457 | — | — | 2 | 7.54 |
| CHEMBL2057453 | — | — | 2 | 7.45 |
| CHEMBL2057454 | — | — | 2 | 7.28 |
| CHEMBL2057442 | — | — | 2 | 7.19 |
| CHEMBL2057443 | — | — | 2 | 7.13 |
| CHEMBL2057441 | — | — | 2 | 6.97 |
| CHEMBL2057438 | — | — | 2 | 6.74 |
| CHEMBL2057451 | — | — | 2 | 6.47 |
| CHEMBL2057452 | — | — | 2 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62 | SCH-23390 | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL62 | SCH-23390 | IC50 | = | 2.52 | nM | 8.60 |
| CHEMBL2057455 | — | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL2057455 | — | IC50 | = | 4.86 | nM | 8.31 |
| CHEMBL487387 | STEPHOLIDINE | Ki | = | 6.23 | nM | 8.21 |
| CHEMBL2057445 | — | Ki | = | 7.97 | nM | 8.10 |
| CHEMBL487387 | STEPHOLIDINE | IC50 | = | 12.29 | nM | 7.91 |
| CHEMBL2057445 | — | IC50 | = | 14.29 | nM | 7.84 |
| CHEMBL2057456 | — | Ki | = | 17.29 | nM | 7.76 |
| CHEMBL2057446 | — | Ki | = | 23.76 | nM | 7.62 |
| CHEMBL2057457 | — | Ki | = | 28.91 | nM | 7.54 |
| CHEMBL2057456 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL2057453 | — | Ki | = | 35.79 | nM | 7.45 |
| CHEMBL2057446 | — | IC50 | = | 45.45 | nM | 7.34 |
| CHEMBL2057454 | — | Ki | = | 52.34 | nM | 7.28 |
| CHEMBL2057457 | — | IC50 | = | 56.37 | nM | 7.25 |
| CHEMBL2057442 | — | Ki | = | 64.12 | nM | 7.19 |
| CHEMBL2057453 | — | IC50 | = | 68.89 | nM | 7.16 |
| CHEMBL2057443 | — | Ki | = | 74.51 | nM | 7.13 |
| CHEMBL2057454 | — | IC50 | = | 98.13 | nM | 7.01 |
| CHEMBL2057441 | — | Ki | = | 106.45 | nM | 6.97 |
| CHEMBL2057442 | — | IC50 | = | 113.81 | nM | 6.94 |
| CHEMBL2057443 | — | IC50 | = | 141.58 | nM | 6.85 |
| CHEMBL2057438 | — | Ki | = | 182.41 | nM | 6.74 |
| CHEMBL2057441 | — | IC50 | = | 188.96 | nM | 6.72 |
| CHEMBL2057438 | — | IC50 | = | 323.79 | nM | 6.49 |
| CHEMBL2057451 | — | Ki | = | 337.7 | nM | 6.47 |
| CHEMBL2057451 | — | IC50 | = | 684.0 | nM | 6.17 |
| CHEMBL2057452 | — | Ki | = | 1440.62 | nM | 5.84 |
| CHEMBL2057452 | — | IC50 | = | 2917.2 | nM | 5.54 |