Assay Detail
Binding
CHEMBL963840
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Inhibition of serotonin uptake at human SERT transfected in HEK cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.45 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512044 | — | — | 1 | 8.30 |
| CHEMBL506137 | — | — | 1 | 8.22 |
| CHEMBL510915 | — | — | 1 | 8.00 |
| CHEMBL454770 | — | — | 1 | 7.85 |
| CHEMBL517423 | — | — | 1 | 7.44 |
| CHEMBL461143 | — | — | 1 | 7.30 |
| CHEMBL514937 | — | — | 1 | 7.00 |
| CHEMBL498904 | — | — | 1 | 6.82 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 6.75 |
| CHEMBL507359 | — | — | 1 | 6.74 |
| CHEMBL516507 | — | — | 1 | 6.70 |
| CHEMBL462384 | — | — | 1 | 6.30 |
| CHEMBL446321 | — | — | 1 | 6.16 |
| CHEMBL455448 | — | — | 1 | 6.16 |
| CHEMBL454674 | — | — | 1 | 6.16 |
| CHEMBL502379 | — | — | 1 | 6.10 |
| CHEMBL462402 | — | — | 1 | 5.85 |
| CHEMBL455447 | — | — | 1 | 5.85 |
| CHEMBL507379 | — | — | 1 | 5.75 |
| CHEMBL454675 | — | — | 1 | 5.66 |
| CHEMBL451620 | — | — | 1 | 5.60 |
| CHEMBL509446 | — | — | 1 | 5.52 |
| CHEMBL460295 | — | — | 1 | 5.46 |
| CHEMBL509373 | — | — | 1 | 5.40 |
| CHEMBL462401 | — | — | 1 | 5.26 |
| CHEMBL513618 | — | — | 1 | 5.24 |
| CHEMBL446260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512044 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL506137 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL510915 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL454770 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL517423 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL461143 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL514937 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL498904 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL507359 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL516507 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL462384 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL446321 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL455448 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL454674 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL502379 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL462402 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL455447 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL507379 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL454675 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL451620 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL509446 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL460295 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL509373 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL462401 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL513618 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL446260 | — | IC50 | > | 10000.0 | nM | - |