Assay Detail
Binding
CHEMBL675481
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Binding affinity determined against dopamine receptor D2 in rat caudate membranes using [3H]- raclopride as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.61 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79561 | — | — | 1 | 8.68 |
| CHEMBL83112 | — | — | 1 | 8.42 |
| CHEMBL81703 | — | — | 1 | 8.42 |
| CHEMBL83617 | — | — | 1 | 8.33 |
| CHEMBL82523 | — | — | 1 | 8.17 |
| CHEMBL310744 | — | — | 1 | 8.15 |
| CHEMBL1169435 | — | — | 1 | 8.15 |
| CHEMBL313452 | — | — | 1 | 8.07 |
| CHEMBL311694 | — | — | 1 | 7.82 |
| CHEMBL79674 | — | — | 1 | 7.72 |
| CHEMBL82488 | — | — | 1 | 7.68 |
| CHEMBL84171 | — | — | 1 | 7.58 |
| CHEMBL79725 | — | — | 1 | 7.55 |
| CHEMBL441259 | — | — | 1 | 7.48 |
| CHEMBL79853 | — | — | 1 | 7.43 |
| CHEMBL1159649 | — | — | 1 | 7.32 |
| CHEMBL79693 | — | — | 1 | 7.30 |
| CHEMBL2112307 | — | — | 1 | 7.28 |
| CHEMBL311323 | — | — | 1 | 7.14 |
| CHEMBL311787 | — | — | 1 | 7.07 |
| CHEMBL83732 | — | — | 1 | 7.06 |
| CHEMBL81191 | — | — | 1 | 6.78 |
| CHEMBL442974 | — | — | 1 | 6.74 |
| CHEMBL310082 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79561 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL83112 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL81703 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL83617 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL82523 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL310744 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL1169435 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL313452 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL311694 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL79674 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL82488 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL84171 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL79725 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL441259 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL79853 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1159649 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL79693 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2112307 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL311323 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL311787 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL83732 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL81191 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL442974 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL310082 | — | Ki | = | 491.0 | nM | 6.31 |