Assay Detail
Binding
CHEMBL2182415
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine form human alpha7 nAchR expressed in HEK293 cells
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 68 | 7.50 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179874 | — | — | 1 | 9.29 |
| CHEMBL2179875 | — | — | 1 | 9.10 |
| CHEMBL2179877 | — | — | 1 | 9.05 |
| CHEMBL1258006 | BRADANICLINE | 2.0 | 1 | 9.00 |
| CHEMBL2179873 | — | — | 1 | 8.96 |
| CHEMBL2179878 | — | — | 1 | 8.92 |
| CHEMBL2180253 | — | — | 1 | 8.74 |
| CHEMBL2179881 | — | — | 1 | 8.68 |
| CHEMBL2180250 | — | — | 1 | 8.66 |
| CHEMBL2179862 | — | — | 1 | 8.55 |
| CHEMBL2151441 | — | — | 1 | 8.52 |
| CHEMBL2179879 | — | — | 1 | 8.42 |
| CHEMBL2179871 | — | — | 1 | 8.37 |
| CHEMBL2179872 | — | — | 1 | 8.35 |
| CHEMBL2180254 | — | — | 1 | 8.33 |
| CHEMBL194082 | — | — | 1 | 8.30 |
| CHEMBL2180251 | — | — | 1 | 8.30 |
| CHEMBL2180252 | — | — | 1 | 8.26 |
| CHEMBL2179882 | — | — | 1 | 8.23 |
| CHEMBL2179868 | — | — | 1 | 8.23 |
| CHEMBL2179865 | — | — | 1 | 8.21 |
| CHEMBL1258005 | — | — | 1 | 8.21 |
| CHEMBL2179844 | — | — | 1 | 8.19 |
| CHEMBL2151572 | ENCENICLINE | 3.0 | 1 | 8.00 |
| CHEMBL2179880 | — | — | 1 | 7.95 |
| CHEMBL2180258 | — | — | 1 | 7.94 |
| CHEMBL2180255 | — | — | 1 | 7.91 |
| CHEMBL365323 | — | — | 1 | 7.84 |
| CHEMBL2179842 | — | — | 1 | 7.82 |
| CHEMBL2180257 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179874 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL2179875 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2179877 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1258006 | BRADANICLINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2179873 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2179878 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2180253 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2179881 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2180250 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2179862 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2151441 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2179879 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2179871 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2179872 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2180254 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL194082 | — | Ki | = | 4.98 | nM | 8.30 |
| CHEMBL2180251 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2180252 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL2179882 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL2179868 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL2179865 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL1258005 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2179844 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL2151572 | ENCENICLINE | Ki | = | 9.98 | nM | 8.00 |
| CHEMBL2179880 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL2180258 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL2180255 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL365323 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL2179842 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2180257 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL2179849 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2179883 | — | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL2179851 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL2180263 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2179857 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2179839 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2180256 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL2180260 | — | Ki | = | 36.1 | nM | 7.44 |
| CHEMBL105374 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2179841 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2179847 | — | Ki | = | 52.5 | nM | 7.28 |
| CHEMBL2179866 | — | Ki | = | 56.3 | nM | 7.25 |
| CHEMBL2180262 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2179856 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2179864 | — | Ki | = | 66.2 | nM | 7.18 |
| CHEMBL2179846 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL2179870 | — | Ki | = | 87.7 | nM | 7.06 |
| CHEMBL2179853 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1257896 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL2179843 | — | Ki | = | 112.0 | nM | 6.95 |