Assay Detail
Binding
CHEMBL805637
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Binding affinity at the Serotonin transporter in rat midbrain by inhibition of 0.5 nM [3H]-paroxetine binding
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Midbrain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| 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 | 66 | 5.78 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87031 | — | — | 1 | 8.50 |
| CHEMBL14391 | — | — | 1 | 8.38 |
| CHEMBL127323 | — | — | 1 | 7.98 |
| CHEMBL97887 | — | — | 1 | 7.97 |
| CHEMBL341336 | — | — | 1 | 7.81 |
| CHEMBL306208 | — | — | 1 | 7.35 |
| CHEMBL127546 | — | — | 1 | 7.17 |
| CHEMBL126336 | — | — | 1 | 7.13 |
| CHEMBL339149 | — | — | 1 | 7.01 |
| CHEMBL126261 | — | — | 1 | 6.92 |
| CHEMBL339763 | — | — | 1 | 6.89 |
| CHEMBL127011 | — | — | 1 | 6.78 |
| CHEMBL340761 | — | — | 1 | 6.74 |
| CHEMBL82027 | — | — | 1 | 6.62 |
| CHEMBL127981 | — | — | 1 | 6.52 |
| CHEMBL130531 | — | — | 1 | 6.43 |
| CHEMBL338093 | — | — | 1 | 6.43 |
| CHEMBL127561 | — | — | 1 | 6.31 |
| CHEMBL339809 | — | — | 1 | 6.21 |
| CHEMBL2079586 | — | — | 1 | 6.16 |
| CHEMBL126538 | — | — | 1 | 6.14 |
| CHEMBL338220 | — | — | 1 | 6.09 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.98 |
| CHEMBL126772 | — | — | 1 | 5.97 |
| CHEMBL126682 | — | — | 1 | 5.97 |
| CHEMBL421651 | — | — | 1 | 5.92 |
| CHEMBL446357 | — | — | 1 | 5.91 |
| CHEMBL339130 | — | — | 1 | 5.88 |
| CHEMBL127040 | — | — | 1 | 5.85 |
| CHEMBL127533 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87031 | — | IC50 | = | 3.13 | nM | 8.50 |
| CHEMBL14391 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL127323 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL97887 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL341336 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL306208 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL127546 | — | IC50 | = | 66.8 | nM | 7.17 |
| CHEMBL126336 | — | IC50 | = | 73.9 | nM | 7.13 |
| CHEMBL339149 | — | IC50 | = | 97.8 | nM | 7.01 |
| CHEMBL126261 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL339763 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL127011 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL340761 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL82027 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL127981 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL130531 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL338093 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL127561 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL339809 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL2079586 | — | IC50 | = | 692.0 | nM | 6.16 |
| CHEMBL126538 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL338220 | — | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL370805 | COCAINE | IC50 | = | 1045.0 | nM | 5.98 |
| CHEMBL126772 | — | IC50 | = | 1066.0 | nM | 5.97 |
| CHEMBL126682 | — | IC50 | = | 1079.0 | nM | 5.97 |
| CHEMBL421651 | — | IC50 | = | 1203.0 | nM | 5.92 |
| CHEMBL446357 | — | IC50 | = | 1227.0 | nM | 5.91 |
| CHEMBL339130 | — | IC50 | = | 1313.0 | nM | 5.88 |
| CHEMBL127040 | — | IC50 | = | 1404.0 | nM | 5.85 |
| CHEMBL127533 | — | IC50 | = | 1621.0 | nM | 5.79 |
| CHEMBL1643896 | — | IC50 | = | 1728.0 | nM | 5.76 |
| CHEMBL126410 | — | IC50 | = | 2019.0 | nM | 5.70 |
| CHEMBL125974 | — | IC50 | = | 2153.0 | nM | 5.67 |
| CHEMBL14144 | — | IC50 | = | 2336.0 | nM | 5.63 |
| CHEMBL127260 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL126610 | — | IC50 | = | 3402.0 | nM | 5.47 |
| CHEMBL340138 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL127472 | — | IC50 | = | 3772.0 | nM | 5.42 |
| CHEMBL338584 | — | IC50 | = | 4499.0 | nM | 5.35 |
| CHEMBL125574 | — | IC50 | = | 4517.0 | nM | 5.34 |
| CHEMBL126503 | — | IC50 | = | 5237.0 | nM | 5.28 |
| CHEMBL127457 | — | IC50 | = | 5801.0 | nM | 5.24 |
| CHEMBL321806 | — | IC50 | = | 6090.0 | nM | 5.21 |
| CHEMBL127479 | — | IC50 | = | 6371.0 | nM | 5.20 |
| CHEMBL126229 | — | IC50 | = | 9433.0 | nM | 5.03 |
| CHEMBL127908 | — | IC50 | = | 11040.0 | nM | 4.96 |
| CHEMBL3085512 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL340372 | — | IC50 | = | 13725.0 | nM | 4.86 |
| CHEMBL126660 | — | IC50 | = | 15954.0 | nM | 4.80 |
| CHEMBL420343 | — | IC50 | = | 16914.0 | nM | 4.77 |