Assay Detail
Binding
CHEMBL673204
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Binding affinity at the Dopamine transporter in rat striata by inhibition of 0.5 nM [3H]WIN-35428 binding
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 67 | 7.94 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643896 | — | — | 1 | 9.43 |
| CHEMBL127546 | — | — | 1 | 9.37 |
| CHEMBL341336 | — | — | 1 | 9.21 |
| CHEMBL339763 | — | — | 1 | 9.12 |
| CHEMBL87031 | — | — | 1 | 9.10 |
| CHEMBL127323 | — | — | 1 | 9.09 |
| CHEMBL126538 | — | — | 1 | 9.07 |
| CHEMBL127011 | — | — | 1 | 9.02 |
| CHEMBL126336 | — | — | 1 | 8.97 |
| CHEMBL306208 | — | — | 1 | 8.95 |
| CHEMBL14391 | — | — | 1 | 8.90 |
| CHEMBL126261 | — | — | 1 | 8.87 |
| CHEMBL126682 | — | — | 1 | 8.86 |
| CHEMBL3085512 | — | — | 1 | 8.86 |
| CHEMBL127040 | — | — | 1 | 8.85 |
| CHEMBL127260 | — | — | 1 | 8.83 |
| CHEMBL340761 | — | — | 1 | 8.82 |
| CHEMBL126772 | — | — | 1 | 8.78 |
| CHEMBL97887 | — | — | 1 | 8.77 |
| CHEMBL82027 | — | — | 1 | 8.77 |
| CHEMBL14144 | — | — | 1 | 8.70 |
| CHEMBL339149 | — | — | 1 | 8.69 |
| CHEMBL126610 | — | — | 1 | 8.59 |
| CHEMBL126271 | — | — | 1 | 8.54 |
| CHEMBL340912 | — | — | 1 | 8.49 |
| CHEMBL126410 | — | — | 1 | 8.43 |
| CHEMBL127472 | — | — | 1 | 8.41 |
| CHEMBL126229 | — | — | 1 | 8.26 |
| CHEMBL321806 | — | — | 1 | 8.19 |
| CHEMBL338220 | — | — | 1 | 8.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643896 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL127546 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL341336 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL339763 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL87031 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL127323 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL126538 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL127011 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL126336 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL306208 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL14391 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL126261 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL126682 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL3085512 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL127040 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL127260 | — | IC50 | = | 1.47 | nM | 8.83 |
| CHEMBL340761 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL126772 | — | IC50 | = | 1.68 | nM | 8.78 |
| CHEMBL97887 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL82027 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL14144 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL339149 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL126610 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL126271 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL340912 | — | IC50 | = | 3.26 | nM | 8.49 |
| CHEMBL126410 | — | IC50 | = | 3.74 | nM | 8.43 |
| CHEMBL127472 | — | IC50 | = | 3.91 | nM | 8.41 |
| CHEMBL126229 | — | IC50 | = | 5.48 | nM | 8.26 |
| CHEMBL321806 | — | IC50 | = | 6.45 | nM | 8.19 |
| CHEMBL338220 | — | IC50 | = | 6.57 | nM | 8.18 |
| CHEMBL340138 | — | IC50 | = | 6.95 | nM | 8.16 |
| CHEMBL126503 | — | IC50 | = | 8.19 | nM | 8.09 |
| CHEMBL125974 | — | IC50 | = | 9.37 | nM | 8.03 |
| CHEMBL340760 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL127533 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL127146 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL339130 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL2079586 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL127561 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL338584 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL127908 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL126848 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL421651 | — | IC50 | = | 27.4 | nM | 7.56 |
| CHEMBL446357 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL127479 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL125524 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL420343 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL340505 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL126751 | — | IC50 | = | 71.0 | nM | 7.15 |