Assay Detail
Binding
CHEMBL671417
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In vitro binding affinity at human Dopamine receptor D2 expressed in CHO K1 cells was measured by its ability to displace [3H]- N-0437
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.97 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1303 | ROTIGOTINE | 4.0 | 1 | 10.22 |
| CHEMBL102582 | — | — | 1 | 8.21 |
| CHEMBL15136 | — | — | 1 | 7.85 |
| CHEMBL103622 | — | — | 1 | 7.70 |
| CHEMBL103857 | — | — | 1 | 7.57 |
| CHEMBL301559 | — | — | 1 | 7.47 |
| CHEMBL322638 | — | — | 1 | 6.43 |
| CHEMBL105623 | — | — | 1 | 6.36 |
| CHEMBL102632 | — | — | 1 | 6.20 |
| CHEMBL103441 | — | — | 1 | 5.97 |
| CHEMBL104135 | — | — | 1 | 5.69 |
| CHEMBL103912 | — | — | 1 | 5.51 |
| CHEMBL102414 | — | — | 1 | 5.43 |
| CHEMBL316584 | — | — | 1 | - |
| CHEMBL319051 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1303 | ROTIGOTINE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL102582 | — | Ki | = | 6.24 | nM | 8.21 |
| CHEMBL15136 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL103622 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL103857 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL301559 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL322638 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL105623 | — | Ki | = | 439.0 | nM | 6.36 |
| CHEMBL102632 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL103441 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL104135 | — | Ki | = | 2037.0 | nM | 5.69 |
| CHEMBL103912 | — | Ki | = | 3107.0 | nM | 5.51 |
| CHEMBL102414 | — | Ki | = | 3676.0 | nM | 5.43 |
| CHEMBL316584 | — | Ki | > | 3676.0 | nM | - |
| CHEMBL319051 | — | Ki | > | 4780.0 | nM | - |