Assay Detail
Binding
CHEMBL3095480
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from Sprague-Dawley rat brain alpha4beta2 nAChR after 90 mins by liquid scintillation counting analysis
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 7.67 | 9.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.91 |
| CHEMBL3093669 | — | — | 1 | 9.04 |
| CHEMBL3093705 | — | — | 1 | 9.00 |
| CHEMBL3093697 | — | — | 1 | 8.99 |
| CHEMBL3093685 | — | — | 1 | 8.92 |
| CHEMBL3093704 | — | — | 1 | 8.68 |
| CHEMBL3093708 | — | — | 1 | 8.51 |
| CHEMBL3093670 | — | — | 1 | 8.41 |
| CHEMBL3093666 | — | — | 1 | 8.25 |
| CHEMBL3093702 | — | — | 1 | 8.20 |
| CHEMBL3093707 | — | — | 1 | 8.15 |
| CHEMBL3093665 | — | — | 1 | 8.15 |
| CHEMBL3093703 | — | — | 1 | 8.11 |
| CHEMBL3093680 | — | — | 1 | 7.99 |
| CHEMBL3093706 | — | — | 1 | 7.96 |
| CHEMBL3093700 | — | — | 1 | 7.96 |
| CHEMBL3093677 | — | — | 1 | 7.95 |
| CHEMBL3093679 | — | — | 1 | 7.88 |
| CHEMBL3093678 | — | — | 1 | 7.84 |
| CHEMBL3093691 | — | — | 1 | 7.68 |
| CHEMBL3093675 | — | — | 1 | 7.64 |
| CHEMBL3093688 | — | — | 1 | 7.62 |
| CHEMBL3093689 | — | — | 1 | 7.61 |
| CHEMBL3093664 | — | — | 1 | 7.60 |
| CHEMBL3093696 | — | — | 1 | 7.49 |
| CHEMBL3093698 | — | — | 1 | 7.43 |
| CHEMBL3093690 | — | — | 1 | 7.41 |
| CHEMBL3093682 | — | — | 1 | 7.41 |
| CHEMBL3093692 | — | — | 1 | 7.40 |
| CHEMBL3093663 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.122 | nM | 9.91 |
| CHEMBL3093669 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL3093705 | — | Ki | = | 0.991 | nM | 9.00 |
| CHEMBL3093697 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL3093685 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3093704 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3093708 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3093670 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL3093666 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL3093702 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3093707 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3093665 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3093703 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL3093680 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL3093700 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL3093706 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL3093677 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL3093679 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL3093678 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL3093691 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL3093675 | — | Ki | = | 22.9 | nM | 7.64 |
| CHEMBL3093688 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL3093689 | — | Ki | = | 24.6 | nM | 7.61 |
| CHEMBL3093664 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3093696 | — | Ki | = | 32.59 | nM | 7.49 |
| CHEMBL3093698 | — | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL3093690 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL3093682 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3093692 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL3093663 | — | Ki | = | 39.9 | nM | 7.40 |
| CHEMBL3093709 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3093676 | — | Ki | = | 46.9 | nM | 7.33 |
| CHEMBL3093681 | — | Ki | = | 52.5 | nM | 7.28 |
| CHEMBL3093686 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL3093695 | — | Ki | = | 57.1 | nM | 7.24 |
| CHEMBL3093673 | — | Ki | = | 57.6 | nM | 7.24 |
| CHEMBL3093694 | — | Ki | = | 96.9 | nM | 7.01 |
| CHEMBL3093671 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3093668 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL3093687 | — | Ki | = | 171.8 | nM | 6.76 |
| CHEMBL3093683 | — | Ki | = | 232.6 | nM | 6.63 |
| CHEMBL3093701 | — | Ki | = | 241.9 | nM | 6.62 |
| CHEMBL3093693 | — | Ki | = | 287.5 | nM | 6.54 |
| CHEMBL3093699 | — | Ki | = | 296.6 | nM | 6.53 |
| CHEMBL3093672 | — | Ki | = | 453.6 | nM | 6.34 |
| CHEMBL3093684 | — | Ki | = | 548.0 | nM | 6.26 |
| CHEMBL3093674 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL3093667 | — | Ki | > | 1000.0 | nM | - |