Assay Detail
Binding
CHEMBL3089199
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Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells after 4 hrs
19
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; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.14 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086995 | — | — | 1 | 7.64 |
| CHEMBL3086994 | — | — | 1 | 7.51 |
| CHEMBL96201 | — | — | 1 | 7.44 |
| CHEMBL3086992 | — | — | 1 | 7.43 |
| CHEMBL3086985 | — | — | 1 | 7.42 |
| CHEMBL3086989 | — | — | 1 | 7.34 |
| CHEMBL3086982 | — | — | 1 | 7.34 |
| CHEMBL3086993 | — | — | 1 | 7.33 |
| CHEMBL3086986 | — | — | 1 | 7.28 |
| CHEMBL3086996 | — | — | 1 | 7.27 |
| CHEMBL3086991 | — | — | 1 | 7.24 |
| CHEMBL3086984 | — | — | 1 | 7.18 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.15 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.96 |
| CHEMBL3086983 | — | — | 1 | 6.82 |
| CHEMBL2024096 | — | — | 1 | 6.68 |
| CHEMBL3086990 | — | — | 1 | 5.39 |
| CHEMBL3086987 | — | — | 1 | - |
| CHEMBL3086988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086995 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3086994 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL96201 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3086992 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3086985 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL3086989 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3086982 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3086993 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL3086986 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL3086996 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3086991 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3086984 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL3 | NICOTINE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3086983 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2024096 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3086990 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL3086987 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL3086988 | — | Ki | > | 250000.0 | nM | - |