Assay Detail
Binding
CHEMBL673254
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Inhibition of [3H]3-beta-(4-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to dopamine transporter of cynomolgus monkey striatum
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | monkey |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.01 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL169471 | — | — | 1 | 9.18 |
| CHEMBL14391 | — | — | 1 | 8.97 |
| CHEMBL87031 | — | — | 1 | 8.96 |
| CHEMBL81525 | — | — | 1 | 8.85 |
| CHEMBL306208 | — | — | 1 | 8.85 |
| CHEMBL171106 | — | — | 1 | 8.10 |
| CHEMBL2079586 | — | — | 1 | 7.96 |
| CHEMBL67387 | — | — | 1 | 7.56 |
| CHEMBL80515 | — | — | 1 | 7.47 |
| CHEMBL1790051 | — | — | 1 | 7.19 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.02 |
| CHEMBL170790 | 3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL169471 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL14391 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL87031 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL81525 | — | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL306208 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL171106 | — | IC50 | = | 7.93 | nM | 8.10 |
| CHEMBL2079586 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL67387 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL80515 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL1790051 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL370805 | COCAINE | IC50 | = | 95.6 | nM | 7.02 |
| CHEMBL170790 | 3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester | IC50 | = | 1100.0 | nM | 5.96 |