Assay Detail
Binding
CHEMBL938656
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat recombinant alpha-3-beta-4 nAChR expressed in HEK293 cells
38
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 4.98 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486572 | — | — | 2 | 6.40 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 6.22 |
| CHEMBL486773 | — | — | 2 | 5.60 |
| CHEMBL455778 | — | — | 2 | 5.60 |
| CHEMBL457916 | — | — | 2 | 5.50 |
| CHEMBL457737 | — | — | 2 | 5.40 |
| CHEMBL442890 | — | — | 2 | 5.40 |
| CHEMBL487350 | — | — | 2 | 5.10 |
| CHEMBL486774 | — | — | 2 | 5.00 |
| CHEMBL466400 | — | — | 2 | 5.00 |
| CHEMBL488380 | — | — | 2 | 4.72 |
| CHEMBL1202079 | — | — | 2 | 4.64 |
| CHEMBL528765 | — | — | 2 | 4.60 |
| CHEMBL486573 | — | — | 2 | 4.60 |
| CHEMBL488379 | — | — | 2 | 4.00 |
| CHEMBL488381 | — | — | 2 | 4.00 |
| CHEMBL486781 | — | — | 2 | 4.00 |
| CHEMBL449444 | — | — | 2 | 4.00 |
| CHEMBL486775 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486572 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL486572 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL3 | NICOTINE | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3 | NICOTINE | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL455778 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL455778 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL486773 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL486773 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL457916 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL457916 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL442890 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL457737 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL442890 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL457737 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL487350 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL487350 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL486774 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL466400 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL466400 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL486774 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL488380 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL488380 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL1202079 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL528765 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL528765 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL1202079 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL486573 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL486573 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL488379 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL449444 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL449444 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL486781 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL486781 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL488381 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL488381 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL488379 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL486775 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL486775 | — | Ki | = | 300000.0 | nM | - |