Assay Detail
Functional
CHEMBL890746
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NET in HEK cells assessed as [3H]norepinephrine reuptake
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.79 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227232 | — | — | 1 | 6.24 |
| CHEMBL227233 | — | — | 1 | 6.21 |
| CHEMBL388760 | — | — | 1 | 6.19 |
| CHEMBL390743 | — | — | 1 | 6.16 |
| CHEMBL227179 | — | — | 1 | 6.12 |
| CHEMBL227180 | — | — | 1 | 6.04 |
| CHEMBL388759 | — | — | 1 | 6.02 |
| CHEMBL229381 | — | — | 1 | 5.93 |
| CHEMBL229436 | — | — | 1 | 5.81 |
| CHEMBL375685 | — | — | 1 | 5.74 |
| CHEMBL226933 | — | — | 1 | 5.74 |
| CHEMBL226984 | — | — | 1 | 5.69 |
| CHEMBL227231 | — | — | 1 | 5.64 |
| CHEMBL436132 | — | — | 1 | 5.49 |
| CHEMBL376113 | — | — | 1 | 5.40 |
| CHEMBL388832 | — | — | 1 | 5.38 |
| CHEMBL229699 | — | — | 1 | 5.31 |
| CHEMBL388612 | — | — | 1 | 5.19 |
| CHEMBL2113279 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227232 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL227233 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL388760 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL390743 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL227179 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL227180 | — | IC50 | = | 912.0 | nM | 6.04 |
| CHEMBL388759 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL229381 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL229436 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL375685 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL226933 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL226984 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL227231 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL436132 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL376113 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL388832 | — | IC50 | = | 4210.0 | nM | 5.38 |
| CHEMBL229699 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL388612 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2113279 | — | IC50 | > | 6900.0 | nM | - |