Assay Detail
Functional
CHEMBL4406071
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Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.87 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 9.96 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 9.38 |
| CHEMBL4475406 | — | — | 1 | 8.45 |
| CHEMBL4443039 | — | — | 1 | 7.90 |
| CHEMBL4522558 | — | — | 1 | 7.53 |
| CHEMBL4439544 | — | — | 1 | 7.06 |
| CHEMBL4580817 | — | — | 1 | 7.00 |
| CHEMBL4586582 | — | — | 1 | 6.84 |
| CHEMBL4454380 | — | — | 1 | 6.75 |
| CHEMBL4593394 | — | — | 1 | - |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4475406 | — | EC50 | = | 3.58 | nM | 8.45 |
| CHEMBL4443039 | — | EC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4522558 | — | EC50 | = | 29.6 | nM | 7.53 |
| CHEMBL4439544 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4580817 | — | EC50 | = | 99.2 | nM | 7.00 |
| CHEMBL4586582 | — | EC50 | = | 142.8 | nM | 6.84 |
| CHEMBL4454380 | — | EC50 | = | 177.5 | nM | 6.75 |
| CHEMBL4593394 | — | EC50 | - | — | - | |
| CHEMBL39 | SEROTONIN | EC50 | - | — | - |