Assay Detail
Functional
CHEMBL740143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices
36
Total Activities
34
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
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.80 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 7.05 |
| CHEMBL287064 | NOMELIDINE | 2.0 | 2 | 7.00 |
| CHEMBL36864 | — | — | 2 | 6.70 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 6.52 |
| CHEMBL811 | BROMPHENIRAMINE | 4.0 | 1 | 6.52 |
| CHEMBL37791 | — | — | 1 | 6.30 |
| CHEMBL36918 | — | — | 1 | 6.30 |
| CHEMBL36865 | — | — | 1 | 6.22 |
| CHEMBL36591 | ALAPROCLATE | 2.0 | 1 | 6.16 |
| CHEMBL285385 | — | — | 1 | 6.10 |
| CHEMBL37065 | — | — | 1 | 6.05 |
| CHEMBL37144 | — | — | 1 | 6.00 |
| CHEMBL36089 | — | — | 1 | 5.85 |
| CHEMBL446651 | — | — | 1 | 5.85 |
| CHEMBL288594 | — | — | 1 | 5.82 |
| CHEMBL34607 | — | — | 1 | 5.80 |
| CHEMBL37164 | — | — | 1 | 5.80 |
| CHEMBL354646 | — | — | 1 | 5.77 |
| CHEMBL37018 | — | — | 1 | 5.70 |
| CHEMBL38036 | — | — | 1 | 5.70 |
| CHEMBL36546 | — | — | 1 | 5.68 |
| CHEMBL37298 | — | — | 1 | 5.62 |
| CHEMBL37121 | — | — | 1 | 5.58 |
| CHEMBL37216 | — | — | 1 | 5.52 |
| CHEMBL37311 | — | — | 1 | 5.46 |
| CHEMBL290573 | — | — | 1 | 5.43 |
| CHEMBL37011 | — | — | 1 | 5.40 |
| CHEMBL37068 | — | — | 1 | 5.38 |
| CHEMBL37744 | ZIMELDINE | 4.0 | 1 | 5.21 |
| CHEMBL36095 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL287064 | NOMELIDINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL36864 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL811 | BROMPHENIRAMINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL37791 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL36864 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL36918 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL36865 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL36591 | ALAPROCLATE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL285385 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL37065 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL37144 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL446651 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL36089 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL288594 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL37164 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL34607 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL354646 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL37018 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL38036 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL36546 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL37298 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL287064 | NOMELIDINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL37121 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL37216 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL37311 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL290573 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL37011 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL37068 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL37744 | ZIMELDINE | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL36095 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL36958 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL36267 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL37878 | — | IC50 | = | 25000.0 | nM | 4.60 |