Assay Detail
Binding
CHEMBL861435
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Displacement of [3H]spiperone from D2L dopamine receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 7.61 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380464 | — | — | 1 | 9.00 |
| CHEMBL203047 | — | — | 1 | 8.70 |
| CHEMBL203637 | — | — | 1 | 8.40 |
| CHEMBL204065 | — | — | 1 | 8.19 |
| CHEMBL380330 | — | — | 1 | 7.89 |
| CHEMBL201170 | — | — | 1 | 7.76 |
| CHEMBL382010 | — | — | 1 | 7.43 |
| CHEMBL204098 | — | — | 1 | 7.43 |
| CHEMBL441618 | — | — | 1 | 7.35 |
| CHEMBL381936 | — | — | 1 | 7.23 |
| CHEMBL381946 | — | — | 1 | 7.21 |
| CHEMBL203689 | — | — | 1 | 7.08 |
| CHEMBL383451 | — | — | 1 | 7.06 |
| CHEMBL379662 | — | — | 1 | 6.79 |
| CHEMBL203734 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380464 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL203047 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL203637 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL204065 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL380330 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL201170 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL382010 | — | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL204098 | — | Ki | = | 37.3 | nM | 7.43 |
| CHEMBL441618 | — | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL381936 | — | Ki | = | 58.7 | nM | 7.23 |
| CHEMBL381946 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL203689 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL383451 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL379662 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL203734 | — | Ki | = | 210.0 | nM | 6.68 |