Assay Detail
Binding
CHEMBL3089200
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Displacement of [3H]epibatidine from rat alpha2beta2 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/beta2 (CHEMBL1907592) ↗| 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 | 9.81 | 10.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086994 | — | — | 1 | 10.54 |
| CHEMBL3086992 | — | — | 1 | 10.35 |
| CHEMBL3086982 | — | — | 1 | 10.28 |
| CHEMBL3086984 | — | — | 1 | 10.28 |
| CHEMBL3086995 | — | — | 1 | 10.20 |
| CHEMBL3086985 | — | — | 1 | 10.19 |
| CHEMBL3086993 | — | — | 1 | 10.09 |
| CHEMBL2024096 | — | — | 1 | 10.06 |
| CHEMBL3086986 | — | — | 1 | 10.04 |
| CHEMBL3086991 | — | — | 1 | 9.96 |
| CHEMBL3086983 | — | — | 1 | 9.72 |
| CHEMBL3086989 | — | — | 1 | 9.72 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.66 |
| CHEMBL96201 | — | — | 1 | 9.66 |
| CHEMBL3086996 | — | — | 1 | 9.55 |
| CHEMBL3086990 | — | — | 1 | 8.54 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.92 |
| CHEMBL3086987 | — | — | 1 | - |
| CHEMBL3086988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086994 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3086992 | — | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL3086982 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL3086984 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL3086995 | — | Ki | = | 0.063 | nM | 10.20 |
| CHEMBL3086985 | — | Ki | = | 0.064 | nM | 10.19 |
| CHEMBL3086993 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL2024096 | — | Ki | = | 0.087 | nM | 10.06 |
| CHEMBL3086986 | — | Ki | = | 0.091 | nM | 10.04 |
| CHEMBL3086991 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL3086983 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL3086989 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL96201 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3086996 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3086990 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3 | NICOTINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3086987 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3086988 | — | Ki | > | 5000.0 | nM | - |