Assay Detail
Binding
CHEMBL744177
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards norepinephrine transporter by displacement of [3H]nisoxetine radioligand from rat brain
16
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogues of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.85 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610897 | — | — | 1 | 7.43 |
| CHEMBL607051 | — | — | 1 | 7.22 |
| CHEMBL606995 | — | — | 1 | 6.87 |
| CHEMBL607054 | — | — | 1 | 6.61 |
| CHEMBL607050 | — | — | 1 | 6.44 |
| CHEMBL606997 | — | — | 1 | 6.11 |
| CHEMBL606996 | — | — | 1 | 6.08 |
| CHEMBL1790051 | — | — | 1 | 6.04 |
| CHEMBL607052 | — | — | 1 | 5.74 |
| CHEMBL14144 | — | — | 1 | 5.53 |
| CHEMBL607053 | — | — | 1 | 5.39 |
| CHEMBL607099 | — | — | 1 | 5.23 |
| CHEMBL606998 | — | — | 4 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610897 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL607051 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL606995 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL607054 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL607050 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL606997 | — | IC50 | = | 778.0 | nM | 6.11 |
| CHEMBL606996 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL1790051 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL607052 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL14144 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL607053 | — | IC50 | = | 4070.0 | nM | 5.39 |
| CHEMBL607099 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL606998 | — | IC50 | = | 6990.0 | nM | 5.16 |
| CHEMBL606998 | — | IC50 | = | 7880.0 | nM | 5.10 |
| CHEMBL606998 | — | IC50 | = | 35800.0 | nM | 4.45 |
| CHEMBL606998 | — | IC50 | = | 71000.0 | nM | 4.15 |