Assay Detail
Functional
CHEMBL2388573
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Modification of agonist binding moiety in hybrid derivative 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-1-ol/-2-amino versions: impact on functional activity and selectivity for dopamine D2/D3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 8.58 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152746 | — | — | 1 | 9.59 |
| CHEMBL571992 | — | — | 1 | 9.09 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.12 |
| CHEMBL2387709 | — | — | 1 | 7.52 |
| CHEMBL2387631 | — | — | 1 | - |
| CHEMBL2387632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152746 | — | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL571992 | — | EC50 | = | 0.82 | nM | 9.09 |
| CHEMBL59 | DOPAMINE | EC50 | = | 7.64 | nM | 8.12 |
| CHEMBL2387709 | — | EC50 | = | 30.3 | nM | 7.52 |
| CHEMBL2387631 | — | EC50 | - | — | - | |
| CHEMBL2387632 | — | EC50 | - | — | - |