Assay Detail
Functional
CHEMBL861440
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.88 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203637 | — | — | 1 | 9.34 |
| CHEMBL201170 | — | — | 1 | 8.87 |
| CHEMBL382010 | — | — | 1 | 8.59 |
| CHEMBL381936 | — | — | 1 | 8.48 |
| CHEMBL383451 | — | — | 1 | 8.42 |
| CHEMBL380464 | — | — | 1 | 8.17 |
| CHEMBL203047 | — | — | 1 | 7.97 |
| CHEMBL204098 | — | — | 1 | 7.68 |
| CHEMBL380330 | — | — | 1 | 7.62 |
| CHEMBL204065 | — | — | 1 | 7.57 |
| CHEMBL203734 | — | — | 1 | 7.47 |
| CHEMBL379662 | — | — | 1 | 7.42 |
| CHEMBL441618 | — | — | 1 | 7.22 |
| CHEMBL203689 | — | — | 1 | 7.19 |
| CHEMBL381946 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203637 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL201170 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL382010 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL381936 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL383451 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL380464 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL203047 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL204098 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL380330 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL204065 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL203734 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL379662 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL441618 | — | Ki | = | 60.4 | nM | 7.22 |
| CHEMBL203689 | — | Ki | = | 64.1 | nM | 7.19 |
| CHEMBL381946 | — | Ki | = | 567.0 | nM | 6.25 |