Assay Detail
Binding
CHEMBL675050
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Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.20 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.60 |
| CHEMBL286252 | NAFADOTRIDE | — | 1 | 9.09 |
| CHEMBL301559 | — | — | 1 | 8.66 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.66 |
| CHEMBL64553 | — | — | 1 | 8.62 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 8.52 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 8.46 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 8.10 |
| CHEMBL140184 | — | — | 1 | 7.89 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL445102 | — | — | 1 | 7.22 |
| CHEMBL27441 | — | — | 1 | 7.16 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL286252 | NAFADOTRIDE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL301559 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL64553 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL26 | SULPIRIDE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL140184 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL445102 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL27441 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL42 | CLOZAPINE | Ki | = | 88.0 | nM | 7.06 |