Assay Detail
Binding
CHEMBL750083
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against neuronal nicotinic acetylcholine receptor(nAChR) by using [3H]cytisine as radioligand in whole rat brain
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Neuronal acetylcholine receptor subunit alpha-10 (CHEMBL3461) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 6.70 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305674 | — | — | 1 | 8.51 |
| CHEMBL74249 | — | — | 1 | 8.30 |
| CHEMBL72198 | — | — | 1 | 7.89 |
| CHEMBL72502 | — | — | 1 | 7.84 |
| CHEMBL74045 | — | — | 1 | 7.84 |
| CHEMBL73294 | — | — | 1 | 7.76 |
| CHEMBL75277 | — | — | 1 | 7.75 |
| CHEMBL73293 | — | — | 1 | 7.75 |
| CHEMBL73141 | — | — | 1 | 7.75 |
| CHEMBL74845 | — | — | 1 | 7.71 |
| CHEMBL73381 | — | — | 1 | 7.43 |
| CHEMBL73786 | — | — | 1 | 7.38 |
| CHEMBL72015 | — | — | 1 | 7.29 |
| CHEMBL72031 | — | — | 1 | 7.28 |
| CHEMBL72968 | — | — | 1 | 7.16 |
| CHEMBL72197 | — | — | 1 | 7.11 |
| CHEMBL306055 | — | — | 1 | 7.11 |
| CHEMBL75446 | — | — | 1 | 7.00 |
| CHEMBL73784 | — | — | 1 | 6.97 |
| CHEMBL308250 | — | — | 1 | 6.95 |
| CHEMBL312342 | — | — | 1 | 6.87 |
| CHEMBL74636 | — | — | 1 | 6.77 |
| CHEMBL305820 | — | — | 1 | 6.76 |
| CHEMBL418900 | — | — | 1 | 6.71 |
| CHEMBL75672 | — | — | 1 | 6.69 |
| CHEMBL310032 | — | — | 1 | 6.52 |
| CHEMBL76287 | — | — | 1 | 6.47 |
| CHEMBL76268 | — | — | 1 | 6.33 |
| CHEMBL306594 | — | — | 1 | 6.28 |
| CHEMBL76321 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305674 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL74249 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL72198 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL72502 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL74045 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL73294 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL75277 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL73293 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL73141 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL74845 | — | Ki | = | 19.3 | nM | 7.71 |
| CHEMBL73381 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL73786 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL72015 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL72031 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL72968 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL72197 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL306055 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL75446 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL73784 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL308250 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL312342 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL74636 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL305820 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL418900 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL75672 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL310032 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL76287 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL76268 | — | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL306594 | — | Ki | = | 523.0 | nM | 6.28 |
| CHEMBL76321 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL309589 | — | Ki | = | 592.0 | nM | 6.23 |
| CHEMBL73657 | — | Ki | = | 603.0 | nM | 6.22 |
| CHEMBL73249 | — | Ki | = | 1059.0 | nM | 5.97 |
| CHEMBL74984 | — | Ki | = | 1191.0 | nM | 5.92 |
| CHEMBL306845 | — | Ki | = | 1866.0 | nM | 5.73 |
| CHEMBL73276 | — | Ki | = | 2433.0 | nM | 5.61 |
| CHEMBL73287 | — | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL312749 | — | Ki | = | 3067.0 | nM | 5.51 |
| CHEMBL73275 | — | Ki | = | 3333.0 | nM | 5.48 |
| CHEMBL75575 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL306293 | — | Ki | = | 5166.0 | nM | 5.29 |
| CHEMBL309428 | — | Ki | = | 5086.0 | nM | 5.29 |
| CHEMBL307954 | — | Ki | = | 5406.0 | nM | 5.27 |
| CHEMBL541458 | — | Ki | = | 6889.0 | nM | 5.16 |
| CHEMBL307434 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL72954 | — | Ki | > | 10000.0 | nM | - |