Assay Detail
Binding
CHEMBL938657
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Displacement of [3H]epibatidine from rat recombinant alpha-4-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; alpha4/beta4 (CHEMBL1907595) ↗| 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 | 6.10 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486572 | — | — | 2 | 6.82 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 6.82 |
| CHEMBL488380 | — | — | 2 | 6.75 |
| CHEMBL486774 | — | — | 2 | 6.72 |
| CHEMBL455778 | — | — | 2 | 6.64 |
| CHEMBL1202079 | — | — | 2 | 6.60 |
| CHEMBL457737 | — | — | 2 | 6.60 |
| CHEMBL486773 | — | — | 2 | 6.50 |
| CHEMBL442890 | — | — | 2 | 6.43 |
| CHEMBL457916 | — | — | 2 | 6.34 |
| CHEMBL486775 | — | — | 2 | 6.14 |
| CHEMBL487350 | — | — | 2 | 6.12 |
| CHEMBL486781 | — | — | 2 | 5.80 |
| CHEMBL486573 | — | — | 2 | 5.70 |
| CHEMBL466400 | — | — | 2 | 5.60 |
| CHEMBL528765 | — | — | 2 | 5.50 |
| CHEMBL488379 | — | — | 2 | 5.15 |
| CHEMBL488381 | — | — | 2 | 5.00 |
| CHEMBL449444 | — | — | 2 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486572 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3 | NICOTINE | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL486572 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL3 | NICOTINE | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL488380 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL486774 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL486774 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL488380 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL455778 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL1202079 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL457737 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL455778 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL457737 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL1202079 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL486773 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL486773 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL442890 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL442890 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL457916 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL457916 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL486775 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL487350 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL486775 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL487350 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL486781 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL486781 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL486573 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL486573 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL466400 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL466400 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL528765 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL528765 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL488379 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL488379 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL488381 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL449444 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL449444 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL488381 | — | Ki | = | 11000.0 | nM | 4.96 |