Assay Detail
Binding
CHEMBL804187
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Inhibition of [3H]peroxitine binding to rat cortical membranes as measure of inhibitory activity towards 5-HT uptake
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
New indole derivatives as potent and selective serotonin uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.56 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19613 | — | — | 1 | 9.70 |
| CHEMBL18224 | — | — | 1 | 9.52 |
| CHEMBL19267 | — | — | 1 | 9.52 |
| CHEMBL18512 | — | — | 1 | 9.40 |
| CHEMBL19347 | — | — | 1 | 9.40 |
| CHEMBL19111 | — | — | 1 | 9.22 |
| CHEMBL274517 | — | — | 1 | 9.22 |
| CHEMBL19203 | — | — | 1 | 9.10 |
| CHEMBL19051 | — | — | 1 | 8.96 |
| CHEMBL274728 | RP-68303 | — | 1 | 8.92 |
| CHEMBL18501 | — | — | 1 | 8.85 |
| CHEMBL429768 | — | — | 1 | 8.85 |
| CHEMBL278080 | — | — | 1 | 8.80 |
| CHEMBL18625 | — | — | 1 | 8.77 |
| CHEMBL276920 | — | — | 1 | 8.70 |
| CHEMBL19270 | — | — | 1 | 8.40 |
| CHEMBL276922 | — | — | 1 | 8.30 |
| CHEMBL416544 | — | — | 1 | 8.30 |
| CHEMBL275354 | — | — | 1 | 8.22 |
| CHEMBL18212 | — | — | 1 | 8.00 |
| CHEMBL276565 | — | — | 1 | 8.00 |
| CHEMBL279414 | — | — | 1 | 8.00 |
| CHEMBL281808 | — | — | 1 | 7.96 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.82 |
| CHEMBL19228 | — | — | 1 | 7.66 |
| CHEMBL19652 | — | — | 1 | 7.60 |
| CHEMBL19226 | — | — | 1 | 7.46 |
| CHEMBL19335 | — | — | 1 | 7.00 |
| CHEMBL414187 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19613 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL18224 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL19267 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL18512 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL19347 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL19111 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL274517 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL19203 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL19051 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL274728 | RP-68303 | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL18501 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL429768 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL278080 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL18625 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL276920 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL19270 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL276922 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL416544 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL275354 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL18212 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL276565 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL279414 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL281808 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL19228 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL19652 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL19226 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL19335 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL414187 | — | IC50 | > | 100.0 | nM | - |