Assay Detail
Binding
CHEMBL750796
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Binding affinity at the Norepinephrine transporter in rat frontal cortex by inhibition of 0.5 nM [3H]nisoxetine binding
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 5.72 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87031 | — | — | 1 | 7.75 |
| CHEMBL14391 | — | — | 1 | 7.44 |
| CHEMBL127323 | — | — | 1 | 7.44 |
| CHEMBL306208 | — | — | 1 | 7.43 |
| CHEMBL97887 | — | — | 1 | 7.43 |
| CHEMBL82027 | — | — | 1 | 7.22 |
| CHEMBL341336 | — | — | 1 | 6.99 |
| CHEMBL126336 | — | — | 1 | 6.99 |
| CHEMBL339149 | — | — | 1 | 6.84 |
| CHEMBL127011 | — | — | 1 | 6.63 |
| CHEMBL127546 | — | — | 1 | 6.54 |
| CHEMBL339763 | — | — | 1 | 6.45 |
| CHEMBL126610 | — | — | 1 | 6.36 |
| CHEMBL126538 | — | — | 1 | 6.26 |
| CHEMBL126772 | — | — | 1 | 6.19 |
| CHEMBL127040 | — | — | 1 | 6.11 |
| CHEMBL2079586 | — | — | 1 | 6.08 |
| CHEMBL1790051 | — | — | 1 | 6.04 |
| CHEMBL126682 | — | — | 1 | 6.03 |
| CHEMBL446357 | — | — | 1 | 6.01 |
| CHEMBL338220 | — | — | 1 | 6.00 |
| CHEMBL1643896 | — | — | 1 | 6.00 |
| CHEMBL127260 | — | — | 1 | 5.96 |
| CHEMBL421651 | — | — | 1 | 5.89 |
| CHEMBL126261 | — | — | 1 | 5.88 |
| CHEMBL126751 | — | — | 1 | 5.82 |
| CHEMBL339130 | — | — | 1 | 5.80 |
| CHEMBL340138 | — | — | 1 | 5.76 |
| CHEMBL321806 | — | — | 1 | 5.71 |
| CHEMBL126503 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87031 | — | IC50 | = | 17.96 | nM | 7.75 |
| CHEMBL14391 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL127323 | — | IC50 | = | 36.2 | nM | 7.44 |
| CHEMBL306208 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL97887 | — | IC50 | = | 37.4 | nM | 7.43 |
| CHEMBL82027 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL341336 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL126336 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL339149 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL127011 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL127546 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL339763 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL126610 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL126538 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL126772 | — | IC50 | = | 644.0 | nM | 6.19 |
| CHEMBL127040 | — | IC50 | = | 778.0 | nM | 6.11 |
| CHEMBL2079586 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL1790051 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL126682 | — | IC50 | = | 942.0 | nM | 6.03 |
| CHEMBL446357 | — | IC50 | = | 967.6 | nM | 6.01 |
| CHEMBL338220 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1643896 | — | IC50 | = | 991.0 | nM | 6.00 |
| CHEMBL127260 | — | IC50 | = | 1083.0 | nM | 5.96 |
| CHEMBL421651 | — | IC50 | = | 1277.0 | nM | 5.89 |
| CHEMBL126261 | — | IC50 | = | 1329.0 | nM | 5.88 |
| CHEMBL126751 | — | IC50 | = | 1522.0 | nM | 5.82 |
| CHEMBL339130 | — | IC50 | = | 1584.0 | nM | 5.80 |
| CHEMBL340138 | — | IC50 | = | 1752.0 | nM | 5.76 |
| CHEMBL321806 | — | IC50 | = | 1926.0 | nM | 5.71 |
| CHEMBL126503 | — | IC50 | = | 2136.0 | nM | 5.67 |
| CHEMBL125524 | — | IC50 | = | 2202.0 | nM | 5.66 |
| CHEMBL127561 | — | IC50 | = | 2628.0 | nM | 5.58 |
| CHEMBL125974 | — | IC50 | = | 2744.0 | nM | 5.56 |
| CHEMBL14144 | — | IC50 | = | 2955.0 | nM | 5.53 |
| CHEMBL126887 | — | IC50 | = | 3151.0 | nM | 5.50 |
| CHEMBL370805 | COCAINE | IC50 | = | 3298.0 | nM | 5.48 |
| CHEMBL338584 | — | IC50 | = | 3444.0 | nM | 5.46 |
| CHEMBL340761 | — | IC50 | = | 3791.0 | nM | 5.42 |
| CHEMBL340505 | — | IC50 | = | 3935.0 | nM | 5.41 |
| CHEMBL3085512 | — | IC50 | = | 3950.0 | nM | 5.40 |
| CHEMBL340372 | — | IC50 | = | 3981.0 | nM | 5.40 |
| CHEMBL126660 | — | IC50 | = | 4096.0 | nM | 5.39 |
| CHEMBL127700 | — | IC50 | = | 4213.0 | nM | 5.38 |
| CHEMBL127533 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL127479 | — | IC50 | = | 4398.0 | nM | 5.36 |
| CHEMBL126410 | — | IC50 | = | 4738.0 | nM | 5.32 |
| CHEMBL127472 | — | IC50 | = | 4783.0 | nM | 5.32 |
| CHEMBL338093 | — | IC50 | = | 4893.0 | nM | 5.31 |
| CHEMBL420343 | — | IC50 | = | 4883.0 | nM | 5.31 |
| CHEMBL126229 | — | IC50 | = | 5532.0 | nM | 5.26 |