Assay Detail
Binding
CHEMBL3057567
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Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterodimerization of G-Protein-Coupled Receptors Reveals an Unexpected Level of Pharmacological Diversity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.45 | 7.62 |
| Ki | 5 | 8.01 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 9.28 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.00 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.90 |
| CHEMBL540612 | — | — | 1 | 7.62 |
| CHEMBL531 | PERGOLIDE | 4.0 | 1 | 7.50 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.19 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 6.93 |
| CHEMBL285755 | — | — | 1 | 6.72 |
| CHEMBL65280 | — | — | 1 | 6.69 |
| CHEMBL484599 | — | — | 1 | 6.39 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | 6.35 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 5.74 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 5.50 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219916 | DOMPERIDONE | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL715 | OLANZAPINE | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL540612 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL531 | PERGOLIDE | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL42 | CLOZAPINE | Ki | = | 64.2 | nM | 7.19 |
| CHEMBL53 | APOMORPHINE | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL285755 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL65280 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL484599 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL301265 | PRAMIPEXOLE | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL589 | ROPINIROLE | IC50 | = | 1803.0 | nM | 5.74 |
| CHEMBL59 | DOPAMINE | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL240773 | QUINPIROLE | IC50 | = | 4784.0 | nM | 5.32 |