Assay Detail
Binding
CHEMBL672390
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Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.48 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2079586 | — | — | 1 | 7.76 |
| CHEMBL48225 | — | — | 1 | 7.65 |
| CHEMBL21112 | — | — | 1 | 7.44 |
| CHEMBL416818 | — | — | 1 | 7.37 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2079586 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL48225 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL21112 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL416818 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL370805 | COCAINE | IC50 | = | 67.8 | nM | 7.17 |