Assay Detail
Binding
CHEMBL1219686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nisoxetine from NET in rat frontal cortex by scintillation counting
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.08 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1214691 | — | — | 1 | 5.70 |
| CHEMBL1214689 | — | — | 1 | 5.58 |
| CHEMBL1215761 | — | — | 1 | 5.42 |
| CHEMBL1214768 | — | — | 1 | 5.38 |
| CHEMBL1214692 | — | — | 1 | 5.33 |
| CHEMBL1214844 | — | — | 1 | 5.30 |
| CHEMBL1215763 | — | — | 1 | 5.30 |
| CHEMBL1214910 | — | — | 1 | 5.29 |
| CHEMBL1214769 | — | — | 1 | 5.24 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 5.22 |
| CHEMBL1215759 | — | — | 1 | 5.21 |
| CHEMBL1214771 | — | — | 1 | 5.14 |
| CHEMBL1212960 | — | — | 1 | 5.12 |
| CHEMBL1214907 | — | — | 1 | 5.08 |
| CHEMBL1508 | ESCITALOPRAM | 4.0 | 1 | 4.98 |
| CHEMBL1215762 | — | — | 1 | 4.94 |
| CHEMBL1214842 | — | — | 1 | 4.92 |
| CHEMBL1214690 | — | — | 1 | 4.90 |
| CHEMBL1214909 | — | — | 1 | 4.78 |
| CHEMBL1215760 | — | — | 1 | 4.77 |
| CHEMBL1214908 | — | — | 1 | 4.67 |
| CHEMBL1214770 | — | — | 1 | 4.60 |
| CHEMBL1215695 | — | — | 1 | 4.55 |
| CHEMBL1214843 | — | — | 1 | 4.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1214691 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL1214689 | — | Ki | = | 2610.0 | nM | 5.58 |
| CHEMBL1215761 | — | Ki | = | 3820.0 | nM | 5.42 |
| CHEMBL1214768 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL1214692 | — | Ki | = | 4630.0 | nM | 5.33 |
| CHEMBL1214844 | — | Ki | = | 4980.0 | nM | 5.30 |
| CHEMBL1215763 | — | Ki | = | 4980.0 | nM | 5.30 |
| CHEMBL1214910 | — | Ki | = | 5190.0 | nM | 5.29 |
| CHEMBL1214769 | — | Ki | = | 5710.0 | nM | 5.24 |
| CHEMBL549 | CITALOPRAM | Ki | = | 5950.0 | nM | 5.22 |
| CHEMBL1215759 | — | Ki | = | 6170.0 | nM | 5.21 |
| CHEMBL1214771 | — | Ki | = | 7160.0 | nM | 5.14 |
| CHEMBL1212960 | — | Ki | = | 7670.0 | nM | 5.12 |
| CHEMBL1214907 | — | Ki | = | 8410.0 | nM | 5.08 |
| CHEMBL1508 | ESCITALOPRAM | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL1215762 | — | Ki | = | 11400.0 | nM | 4.94 |
| CHEMBL1214842 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL1214690 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL1214909 | — | Ki | = | 16800.0 | nM | 4.78 |
| CHEMBL1215760 | — | Ki | = | 16900.0 | nM | 4.77 |
| CHEMBL1214908 | — | Ki | = | 21600.0 | nM | 4.67 |
| CHEMBL1214770 | — | Ki | = | 25100.0 | nM | 4.60 |
| CHEMBL1215695 | — | Ki | = | 28400.0 | nM | 4.55 |
| CHEMBL1214843 | — | Ki | = | 32500.0 | nM | 4.49 |