Assay Detail
Binding
CHEMBL1293147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-citalopram in human SERT expressed in LLCPK cells by filtration assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LLCPK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.10 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289618 | — | — | 1 | 9.60 |
| CHEMBL1289510 | — | — | 1 | 9.30 |
| CHEMBL1289509 | — | — | 1 | 9.30 |
| CHEMBL1289394 | — | — | 1 | 9.30 |
| CHEMBL1289617 | — | — | 1 | 9.00 |
| CHEMBL1289721 | — | — | 1 | 8.90 |
| CHEMBL1287827 | — | — | 1 | 8.60 |
| CHEMBL1290716 | — | — | 1 | 8.60 |
| CHEMBL1289277 | — | — | 1 | 8.40 |
| CHEMBL1289276 | — | — | 1 | 8.00 |
| CHEMBL469345 | — | — | 1 | 8.00 |
| CHEMBL1289163 | — | — | 1 | 7.90 |
| CHEMBL1289048 | — | — | 1 | 7.90 |
| CHEMBL1290487 | — | — | 1 | 7.90 |
| CHEMBL1289164 | — | — | 1 | 7.80 |
| CHEMBL1290597 | — | — | 1 | 7.60 |
| CHEMBL1290596 | — | — | 1 | 7.30 |
| CHEMBL1289047 | — | — | 1 | 7.00 |
| CHEMBL1290715 | — | — | 1 | 6.70 |
| CHEMBL1290486 | — | — | 1 | 6.60 |
| CHEMBL513715 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289618 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1289510 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL1289509 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL1289394 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL1289617 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1289721 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL1287827 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1290716 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1289277 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL1289276 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL469345 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1289163 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1289048 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1290487 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1289164 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1290597 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1290596 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1289047 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1290715 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1290486 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL513715 | — | Ki | = | 316.23 | nM | 6.50 |