Assay Detail
Functional
CHEMBL783341
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Inhibition of uptake of 5-HT in rat brain cortex
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.47 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276520 | INDALPINE | 4.0 | 1 | 8.00 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 7.70 |
| CHEMBL24042 | — | — | 1 | 7.40 |
| CHEMBL429771 | — | — | 1 | 7.30 |
| CHEMBL278080 | — | — | 1 | 7.00 |
| CHEMBL25428 | — | — | 1 | 6.89 |
| CHEMBL24731 | — | — | 1 | 6.85 |
| CHEMBL543980 | — | — | 1 | 6.40 |
| CHEMBL284004 | — | — | 1 | 6.35 |
| CHEMBL1159866 | — | — | 1 | 6.22 |
| CHEMBL25416 | — | — | 1 | 6.16 |
| CHEMBL1159870 | — | — | 1 | 6.16 |
| CHEMBL24075 | — | — | 1 | 6.00 |
| CHEMBL1159861 | — | — | 1 | 6.00 |
| CHEMBL1159865 | — | — | 1 | 5.82 |
| CHEMBL544216 | — | — | 1 | 5.77 |
| CHEMBL557413 | — | — | 1 | 5.72 |
| CHEMBL24783 | — | — | 1 | 5.66 |
| CHEMBL278816 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276520 | INDALPINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL24042 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL429771 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL278080 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL25428 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL24731 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL543980 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL284004 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1159866 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL25416 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1159870 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL24075 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1159861 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1159865 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL544216 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL557413 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL24783 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL278816 | — | IC50 | = | 2500.0 | nM | 5.60 |