Assay Detail
Functional
CHEMBL674129
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Inhibitory concentration against [3H]dopamine uptake
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.76 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28394 | — | — | 2 | 9.00 |
| CHEMBL27336 | — | — | 1 | 8.59 |
| CHEMBL281288 | — | — | 1 | 8.55 |
| CHEMBL610897 | — | — | 1 | 8.49 |
| CHEMBL27586 | — | — | 1 | 7.98 |
| CHEMBL2115570 | — | — | 2 | 7.80 |
| CHEMBL285342 | — | — | 2 | 6.90 |
| CHEMBL120901 | — | — | 1 | 6.46 |
| CHEMBL28376 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28394 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL28394 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL27336 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL281288 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL610897 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL27586 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL2115570 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2115570 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL285342 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL120901 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL28376 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL285342 | — | IC50 | = | 525.0 | nM | 6.28 |