Assay Detail
Binding
CHEMBL747854
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Binding affinity towards nicotinic acetylcholine receptor using [3H]-cytisine as radioligand in rat forebrain homogenates
66
Total Activities
66
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 | 66 | 5.18 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.10 |
| CHEMBL25619 | — | — | 1 | 8.35 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 7.06 |
| CHEMBL338558 | — | — | 1 | 6.92 |
| CHEMBL609406 | — | — | 1 | 6.34 |
| CHEMBL609144 | — | — | 1 | 6.32 |
| CHEMBL332008 | — | — | 1 | 6.12 |
| CHEMBL338918 | — | — | 1 | 6.08 |
| CHEMBL609145 | — | — | 1 | 6.03 |
| CHEMBL339474 | — | — | 1 | 5.82 |
| CHEMBL124471 | — | — | 1 | 5.75 |
| CHEMBL609140 | — | — | 1 | 5.43 |
| CHEMBL612093 | — | — | 1 | 5.26 |
| CHEMBL609400 | — | — | 1 | 5.22 |
| CHEMBL332009 | — | — | 1 | 5.19 |
| CHEMBL612086 | — | — | 1 | 4.98 |
| CHEMBL609397 | — | — | 1 | 4.95 |
| CHEMBL435616 | — | — | 1 | 4.91 |
| CHEMBL609395 | — | — | 1 | 4.90 |
| CHEMBL612094 | — | — | 1 | 4.70 |
| CHEMBL125190 | — | — | 1 | 4.69 |
| CHEMBL609139 | — | — | 1 | 4.63 |
| CHEMBL612091 | — | — | 1 | 4.62 |
| CHEMBL609396 | — | — | 1 | 4.61 |
| CHEMBL609401 | — | — | 1 | 4.58 |
| CHEMBL420152 | — | — | 1 | 4.54 |
| CHEMBL127640 | — | — | 1 | 4.49 |
| CHEMBL612092 | — | — | 1 | 4.45 |
| CHEMBL340894 | — | — | 1 | 4.37 |
| CHEMBL609399 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL25619 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL122270 | LOBELINE | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL338558 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL609406 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL609144 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL332008 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL338918 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL609145 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL339474 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL124471 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL609140 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL612093 | — | IC50 | = | 5460.0 | nM | 5.26 |
| CHEMBL609400 | — | IC50 | = | 5990.0 | nM | 5.22 |
| CHEMBL332009 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL612086 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL609397 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL435616 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL609395 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL612094 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL125190 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL609139 | — | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL612091 | — | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL609396 | — | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL609401 | — | IC50 | = | 26300.0 | nM | 4.58 |
| CHEMBL420152 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL127640 | — | IC50 | = | 32300.0 | nM | 4.49 |
| CHEMBL612092 | — | IC50 | = | 35900.0 | nM | 4.45 |
| CHEMBL340894 | — | IC50 | = | 42600.0 | nM | 4.37 |
| CHEMBL609399 | — | IC50 | = | 52500.0 | nM | 4.28 |
| CHEMBL127620 | — | IC50 | = | 53700.0 | nM | 4.27 |
| CHEMBL1161006 | — | IC50 | = | 57700.0 | nM | 4.24 |
| CHEMBL127580 | — | IC50 | = | 59400.0 | nM | 4.23 |
| CHEMBL339483 | — | IC50 | = | 59400.0 | nM | 4.23 |
| CHEMBL124568 | — | IC50 | = | 62600.0 | nM | 4.20 |
| CHEMBL123508 | — | IC50 | = | 68600.0 | nM | 4.16 |
| CHEMBL609142 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL338898 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL126015 | — | IC50 | = | 93000.0 | nM | 4.03 |
| CHEMBL126866 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL126222 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL612095 | — | IC50 | = | 207000.0 | nM | - |
| CHEMBL612087 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL126637 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL127621 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL332074 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1161007 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL609402 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL341099 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125917 | — | IC50 | > | 100000.0 | nM | - |