Assay Detail
Binding
CHEMBL748858
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Binding affinity towards nicotinic acetylcholine receptor using [125I]alpha-bungarotoxin as radioligand in rat forebrain homogenates
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor (CHEMBL2094110) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Rigidified acetylcholine mimics: conformational requirements for binding to neuronal nicotinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 5.42 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 8.43 |
| CHEMBL25619 | — | — | 1 | 8.40 |
| CHEMBL338918 | — | — | 1 | 6.82 |
| CHEMBL338558 | — | — | 1 | 6.80 |
| CHEMBL124471 | — | — | 1 | 6.77 |
| CHEMBL125190 | — | — | 1 | 6.68 |
| CHEMBL338316 | — | — | 1 | 5.62 |
| CHEMBL609401 | — | — | 1 | 5.57 |
| CHEMBL609144 | — | — | 1 | 5.55 |
| CHEMBL126222 | — | — | 1 | 5.54 |
| CHEMBL420150 | — | — | 1 | 5.27 |
| CHEMBL126015 | — | — | 1 | 4.91 |
| CHEMBL609140 | — | — | 1 | 4.82 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 4.74 |
| CHEMBL435616 | — | — | 1 | 4.60 |
| CHEMBL609406 | — | — | 1 | 4.51 |
| CHEMBL609146 | — | — | 1 | 4.43 |
| CHEMBL332008 | — | — | 1 | 4.37 |
| CHEMBL609145 | — | — | 1 | 4.36 |
| CHEMBL612094 | — | — | 1 | 4.30 |
| CHEMBL612097 | — | — | 1 | 4.09 |
| CHEMBL126527 | — | — | 1 | 4.06 |
| CHEMBL127640 | — | — | 1 | 4.04 |
| CHEMBL332009 | — | — | 1 | - |
| CHEMBL126637 | — | — | 1 | - |
| CHEMBL612093 | — | — | 1 | - |
| CHEMBL340079 | — | — | 1 | - |
| CHEMBL1161006 | — | — | 1 | - |
| CHEMBL609142 | — | — | 1 | - |
| CHEMBL339474 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL25619 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL338918 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL338558 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL124471 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL125190 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL338316 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL609401 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL609144 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL126222 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL420150 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL126015 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL609140 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL122270 | LOBELINE | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL435616 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL609406 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL609146 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL332008 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL609145 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL612094 | — | IC50 | = | 49500.0 | nM | 4.30 |
| CHEMBL612097 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL126527 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL127640 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL332009 | — | IC50 | = | 207000.0 | nM | - |
| CHEMBL126637 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL612093 | — | IC50 | = | 111000.0 | nM | - |
| CHEMBL340079 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1161006 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL609142 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL339474 | — | IC50 | = | 134000.0 | nM | - |
| CHEMBL609404 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL609399 | — | IC50 | = | 115000.0 | nM | - |
| CHEMBL609402 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1161007 | — | IC50 | = | 436000.0 | nM | - |