Assay Detail
Binding
CHEMBL3745239
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Spiroperidol from cloned rat dopamine D2L receptor expressed in HEK293 cells by liquid scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.48 | 7.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3740041 | — | — | 1 | 7.79 |
| CHEMBL3740286 | — | — | 1 | 7.13 |
| CHEMBL3740778 | — | — | 1 | 7.06 |
| CHEMBL269004 | — | — | 1 | 6.82 |
| CHEMBL3740760 | — | — | 1 | 6.81 |
| CHEMBL3742140 | — | — | 1 | 6.76 |
| CHEMBL3742127 | — | — | 1 | 6.42 |
| CHEMBL3740143 | — | — | 1 | 6.07 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 6.00 |
| CHEMBL3740829 | — | — | 1 | 6.00 |
| CHEMBL3741175 | — | — | 1 | 5.93 |
| CHEMBL3740474 | — | — | 1 | 5.79 |
| CHEMBL3742273 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3740041 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL3740286 | — | Ki | = | 74.5 | nM | 7.13 |
| CHEMBL3740778 | — | Ki | = | 86.5 | nM | 7.06 |
| CHEMBL269004 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL3740760 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL3742140 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL3742127 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL3740143 | — | Ki | = | 854.0 | nM | 6.07 |
| CHEMBL59 | DOPAMINE | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL3740829 | — | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL3741175 | — | Ki | = | 1164.0 | nM | 5.93 |
| CHEMBL3740474 | — | Ki | = | 1636.0 | nM | 5.79 |
| CHEMBL3742273 | — | Ki | = | 1883.0 | nM | 5.72 |