Assay Detail
Binding
CHEMBL671450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was evaluated for its ability to displace [3H]mazindol binding from rat striatal membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.27 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281288 | — | — | 1 | 8.92 |
| CHEMBL610897 | — | — | 1 | 8.80 |
| CHEMBL145589 | — | — | 1 | 6.65 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.24 |
| CHEMBL145275 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281288 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL610897 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL145589 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL370805 | COCAINE | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL145275 | — | IC50 | = | 1730.0 | nM | 5.76 |