Assay Detail
Binding
CHEMBL803043
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Selectivity for the Serotonin transporter using [3H]paroxetine binding assay
18
Total Activities
8
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 serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.44 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL357443 | — | — | 4 | 7.28 |
| CHEMBL358368 | — | — | 1 | 6.58 |
| CHEMBL2079586 | — | — | 1 | 6.09 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.98 |
| CHEMBL145732 | — | — | 4 | 5.61 |
| CHEMBL436211 | — | — | 4 | 5.08 |
| CHEMBL145534 | — | — | 2 | 4.50 |
| CHEMBL827 | DEXMETHYLPHENIDATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL357443 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL358368 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL357443 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2079586 | — | IC50 | = | 809.0 | nM | 6.09 |
| CHEMBL370805 | COCAINE | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL357443 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL145732 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL145732 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL436211 | — | IC50 | = | 8380.0 | nM | 5.08 |
| CHEMBL357443 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL436211 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL436211 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL145732 | — | IC50 | = | 22800.0 | nM | 4.64 |
| CHEMBL145534 | — | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL145534 | — | IC50 | = | 61200.0 | nM | 4.21 |
| CHEMBL436211 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL145732 | — | IC50 | = | 176000.0 | nM | - |
| CHEMBL827 | DEXMETHYLPHENIDATE | IC50 | = | 224000.0 | nM | - |