Assay Detail
Functional
CHEMBL806826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 5.64 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL154541 | — | — | 1 | 6.60 |
| CHEMBL155109 | — | — | 1 | 6.37 |
| CHEMBL29835 | BESIPIRDINE | 2.0 | 1 | 6.37 |
| CHEMBL155211 | — | — | 1 | 6.24 |
| CHEMBL348034 | — | — | 1 | 6.17 |
| CHEMBL347199 | — | — | 1 | 6.17 |
| CHEMBL345442 | — | — | 1 | 6.12 |
| CHEMBL152842 | — | — | 1 | 6.00 |
| CHEMBL154945 | — | — | 1 | 5.96 |
| CHEMBL350692 | — | — | 1 | 5.89 |
| CHEMBL345251 | — | — | 1 | 5.85 |
| CHEMBL345607 | — | — | 1 | 5.85 |
| CHEMBL346142 | — | — | 1 | 5.85 |
| CHEMBL155460 | — | — | 1 | 5.72 |
| CHEMBL154228 | — | — | 1 | 5.68 |
| CHEMBL155603 | — | — | 1 | 5.66 |
| CHEMBL154319 | — | — | 1 | 5.64 |
| CHEMBL435034 | — | — | 1 | 5.62 |
| CHEMBL154488 | — | — | 1 | 5.60 |
| CHEMBL154735 | — | — | 1 | 5.58 |
| CHEMBL347914 | — | — | 1 | 5.58 |
| CHEMBL154257 | — | — | 1 | 5.48 |
| CHEMBL154297 | — | — | 1 | 5.44 |
| CHEMBL345439 | — | — | 1 | 5.33 |
| CHEMBL347336 | — | — | 1 | 5.21 |
| CHEMBL152748 | — | — | 1 | 5.16 |
| CHEMBL356922 | — | — | 1 | 5.00 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 4.96 |
| CHEMBL347933 | — | — | 1 | 4.92 |
| CHEMBL347666 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL154541 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL155109 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL29835 | BESIPIRDINE | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL155211 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL348034 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL347199 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL345442 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL152842 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL154945 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL350692 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL346142 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL345607 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL345251 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL155460 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL154228 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL155603 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL154319 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL435034 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL154488 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL154735 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL347914 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL154257 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL154297 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL345439 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL347336 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL152748 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL356922 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL95 | TACRINE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL347933 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL347666 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL351760 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL155359 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL15245 | YOHIMBINE | IC50 | > | 20000.0 | nM | - |
| CHEMBL152362 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL153847 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL348716 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL157902 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL346021 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL357553 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL157971 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL134 | CLONIDINE | IC50 | > | 20000.0 | nM | - |
| CHEMBL10316 | IDAZOXAN | IC50 | > | 20000.0 | nM | - |
| CHEMBL348865 | — | IC50 | > | 20000.0 | nM | - |