Assay Detail
Functional
CHEMBL784334
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Compound was evaluated for its ability to inhibit high-affinity uptake of [3H]dopamine into striatal nerve endings of rat
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
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 | 7.13 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281288 | — | — | 1 | 8.55 |
| CHEMBL610897 | — | — | 1 | 8.49 |
| CHEMBL145589 | — | — | 1 | 6.43 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.24 |
| CHEMBL145275 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281288 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL610897 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL145589 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL370805 | COCAINE | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL145275 | — | IC50 | = | 1120.0 | nM | 5.95 |