Assay Detail
Binding
CHEMBL915414
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Displacement of [3H]paroxetine from 5HTT
38
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.51 | 8.38 |
| Ki | 17 | 7.47 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311347 | — | — | 2 | 9.42 |
| CHEMBL218082 | — | — | 2 | 9.02 |
| CHEMBL610897 | — | — | 2 | 8.40 |
| CHEMBL375888 | — | — | 2 | 8.32 |
| CHEMBL375889 | — | — | 2 | 8.23 |
| CHEMBL2096860 | — | — | 2 | 8.22 |
| CHEMBL224819 | — | — | 2 | 7.69 |
| CHEMBL312037 | — | — | 2 | 7.64 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 7.35 |
| CHEMBL2079586 | — | — | 2 | 7.20 |
| CHEMBL2096859 | — | — | 2 | 6.85 |
| CHEMBL83729 | — | — | 2 | 6.75 |
| CHEMBL2096858 | — | — | 2 | 6.45 |
| CHEMBL373385 | — | — | 2 | 6.41 |
| CHEMBL374712 | — | — | 2 | 6.36 |
| CHEMBL222705 | — | — | 2 | 6.34 |
| CHEMBL376899 | — | — | 2 | 6.29 |
| CHEMBL2096856 | — | — | 1 | - |
| CHEMBL2096857 | — | — | 1 | - |
| CHEMBL2096861 | — | — | 1 | - |
| CHEMBL221993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311347 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL218082 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL610897 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL311347 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL375888 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL375889 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL2096860 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL218082 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL224819 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL312037 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL610897 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL370805 | COCAINE | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL375888 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2079586 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL375889 | — | IC50 | = | 64.9 | nM | 7.19 |
| CHEMBL2096860 | — | IC50 | = | 66.3 | nM | 7.18 |
| CHEMBL224819 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2096859 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL83729 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL312037 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2096858 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL373385 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL374712 | — | Ki | = | 441.0 | nM | 6.36 |
| CHEMBL222705 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL376899 | — | Ki | = | 518.0 | nM | 6.29 |
| CHEMBL2096859 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2079586 | — | IC50 | = | 692.0 | nM | 6.16 |
| CHEMBL370805 | COCAINE | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2096858 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL374712 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL83729 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL373385 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL222705 | — | IC50 | = | 5060.0 | nM | 5.30 |
| CHEMBL376899 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2096857 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2096861 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL221993 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2096856 | — | IC50 | > | 10000.0 | nM | - |