Assay Detail
Binding
CHEMBL744138
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
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 | 42 | 5.39 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 8.40 |
| CHEMBL435034 | — | — | 1 | 6.30 |
| CHEMBL154319 | — | — | 1 | 6.20 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.18 |
| CHEMBL154228 | — | — | 1 | 6.15 |
| CHEMBL29835 | BESIPIRDINE | 2.0 | 1 | 6.03 |
| CHEMBL347336 | — | — | 1 | 6.00 |
| CHEMBL154945 | — | — | 1 | 5.85 |
| CHEMBL155109 | — | — | 1 | 5.82 |
| CHEMBL347914 | — | — | 1 | 5.80 |
| CHEMBL155603 | — | — | 1 | 5.75 |
| CHEMBL155460 | — | — | 1 | 5.62 |
| CHEMBL154541 | — | — | 1 | 5.62 |
| CHEMBL348034 | — | — | 1 | 5.60 |
| CHEMBL347666 | — | — | 1 | 5.60 |
| CHEMBL154257 | — | — | 1 | 5.57 |
| CHEMBL345442 | — | — | 1 | 5.46 |
| CHEMBL346142 | — | — | 1 | 5.40 |
| CHEMBL350692 | — | — | 1 | 5.35 |
| CHEMBL155211 | — | — | 1 | 5.32 |
| CHEMBL152842 | — | — | 1 | 5.29 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 5.23 |
| CHEMBL357553 | — | — | 1 | 5.23 |
| CHEMBL152362 | — | — | 1 | 5.12 |
| CHEMBL348865 | — | — | 1 | 5.12 |
| CHEMBL157902 | — | — | 1 | 5.12 |
| CHEMBL345607 | — | — | 1 | 5.09 |
| CHEMBL345251 | — | — | 1 | 4.96 |
| CHEMBL356922 | — | — | 1 | 4.92 |
| CHEMBL345439 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569713 | SCOPOLAMINE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL435034 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL154319 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL7634 | OXOTREMORINE | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL154228 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL29835 | BESIPIRDINE | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL347336 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL154945 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL155109 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL347914 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL155603 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL154541 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL155460 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL348034 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL347666 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL154257 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL345442 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL346142 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL350692 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL155211 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL152842 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL95 | TACRINE | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL357553 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL152362 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL348865 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL157902 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL345607 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL345251 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL356922 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL345439 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL154488 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL347199 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL154297 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL155359 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL157971 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL351760 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL347933 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL346021 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL152748 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL348716 | — | IC50 | = | 128000.0 | nM | - |
| CHEMBL153847 | — | IC50 | = | 247000.0 | nM | - |
| CHEMBL154735 | — | IC50 | > | 1000000.0 | nM | - |