Assay Detail
Binding
CHEMBL3136960
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Agonist activity at human recombinant dopamine D2L receptor expressed in CHOFlpIn cells assessed as ERK1/2 phosphorylation by alphascreen assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.97 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 8.77 |
| CHEMBL3134061 | — | — | 1 | 8.00 |
| CHEMBL3134067 | — | — | 1 | 7.10 |
| CHEMBL3134068 | — | — | 1 | 6.96 |
| CHEMBL3134062 | — | — | 1 | 6.88 |
| CHEMBL3134065 | — | — | 1 | 6.83 |
| CHEMBL3134069 | — | — | 1 | 6.65 |
| CHEMBL3134071 | — | — | 1 | 6.61 |
| CHEMBL3134063 | — | — | 1 | 6.58 |
| CHEMBL3134070 | — | — | 1 | 6.42 |
| CHEMBL3134064 | — | — | 1 | 6.40 |
| CHEMBL3134066 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53 | APOMORPHINE | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3134061 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3134067 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3134068 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3134062 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3134065 | — | EC50 | = | 149.0 | nM | 6.83 |
| CHEMBL3134069 | — | EC50 | = | 224.0 | nM | 6.65 |
| CHEMBL3134071 | — | EC50 | = | 248.0 | nM | 6.61 |
| CHEMBL3134063 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3134070 | — | EC50 | = | 385.0 | nM | 6.42 |
| CHEMBL3134064 | — | EC50 | = | 396.0 | nM | 6.40 |
| CHEMBL3134066 | — | EC50 | = | 419.0 | nM | 6.38 |