Assay Detail
Binding
CHEMBL749347
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Inhibition of [3H]- epibatidine binding at the Nicotinic acetylcholine receptor alpha beta (nAChR) in male rat cerebral cortex
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 10.08 | 10.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142279 | — | — | 1 | 10.89 |
| CHEMBL357016 | — | — | 1 | 10.85 |
| CHEMBL145136 | — | — | 1 | 10.82 |
| CHEMBL142598 | — | — | 1 | 10.70 |
| CHEMBL143576 | — | — | 1 | 10.64 |
| CHEMBL54686 | — | — | 1 | 10.60 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.59 |
| CHEMBL145673 | — | — | 1 | 10.57 |
| CHEMBL56682 | — | — | 1 | 10.57 |
| CHEMBL357597 | — | — | 1 | 10.29 |
| CHEMBL142055 | — | — | 1 | 10.26 |
| CHEMBL54586 | — | — | 1 | 10.15 |
| CHEMBL142280 | — | — | 1 | 10.15 |
| CHEMBL145613 | — | — | 1 | 9.54 |
| CHEMBL143213 | — | — | 1 | 9.28 |
| CHEMBL345012 | — | — | 1 | 8.89 |
| CHEMBL144958 | — | — | 1 | 8.82 |
| CHEMBL359409 | — | — | 1 | 7.84 |
| CHEMBL142278 | — | — | 1 | - |
| CHEMBL300467 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142279 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL357016 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL145136 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL142598 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL143576 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL54686 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL145673 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL56682 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL357597 | — | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL142055 | — | Ki | = | 0.055 | nM | 10.26 |
| CHEMBL54586 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL142280 | — | Ki | = | 0.071 | nM | 10.15 |
| CHEMBL145613 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL143213 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL345012 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL144958 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL359409 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL142278 | — | Ki | = | 0.001 | nM | - |
| CHEMBL300467 | — | Ki | = | 0.008 | nM | - |