Assay Detail
Functional
CHEMBL872029
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Inhibition of [3H]-dopamine uptake in rat brain synaptosomes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.53 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105013 | — | — | 1 | 6.89 |
| CHEMBL95636 | TEFLUDAZINE | 2.0 | 1 | 5.66 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 5.20 |
| CHEMBL6066837 | (-)-BUTACLAMOL | — | 1 | 5.02 |
| CHEMBL1255588 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105013 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL95636 | TEFLUDAZINE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL64249 | CLOROTEPINE | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL6066837 | (-)-BUTACLAMOL | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1255588 | — | IC50 | = | 13000.0 | nM | 4.89 |