Assay Detail
Binding
CHEMBL939131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 9.86 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | — | 1 | 10.70 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.59 |
| CHEMBL56682 | — | — | 1 | 10.57 |
| CHEMBL538844 | — | — | 1 | 10.54 |
| CHEMBL556786 | — | — | 1 | 10.36 |
| CHEMBL541399 | — | — | 1 | 10.28 |
| CHEMBL536098 | — | — | 1 | 10.14 |
| CHEMBL559188 | — | — | 1 | 10.06 |
| CHEMBL537896 | — | — | 1 | 10.02 |
| CHEMBL552980 | — | — | 1 | 9.92 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.92 |
| CHEMBL261281 | — | — | 1 | 9.82 |
| CHEMBL559189 | — | — | 1 | 9.80 |
| CHEMBL3216007 | — | — | 1 | 9.77 |
| CHEMBL3216650 | — | — | 1 | 9.77 |
| CHEMBL3215762 | — | — | 1 | 9.70 |
| CHEMBL406222 | — | — | 1 | 9.68 |
| CHEMBL557748 | — | — | 1 | 9.62 |
| CHEMBL539100 | — | — | 1 | 9.47 |
| CHEMBL3216884 | — | — | 1 | 9.47 |
| CHEMBL3217100 | — | — | 1 | 9.37 |
| CHEMBL3215761 | — | — | 1 | 9.30 |
| CHEMBL537679 | — | — | 1 | 8.94 |
| CHEMBL9732 | R-NICOTINE | — | 1 | 8.82 |
| CHEMBL558794 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL56682 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL538844 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL556786 | — | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL541399 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL536098 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL559188 | — | Ki | = | 0.087 | nM | 10.06 |
| CHEMBL537896 | — | Ki | = | 0.095 | nM | 10.02 |
| CHEMBL552980 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL261281 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL559189 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL3216007 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL3216650 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL3215762 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL406222 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL557748 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL539100 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3216884 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3217100 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL3215761 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL537679 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL9732 | R-NICOTINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL558794 | — | Ki | = | 0.009 | nM | - |