Assay Detail
Binding
CHEMBL1118593
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]cytisine from alpha4beta2 nACHR in rat brain homogenate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.61 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083028 | — | — | 1 | 9.70 |
| CHEMBL1083279 | — | — | 1 | 8.37 |
| CHEMBL1083027 | — | — | 1 | 8.22 |
| CHEMBL1083278 | — | — | 1 | 7.58 |
| CHEMBL1083029 | — | — | 1 | 6.86 |
| CHEMBL1083281 | — | — | 1 | 6.16 |
| CHEMBL1082972 | — | — | 1 | 5.26 |
| CHEMBL1082655 | — | — | 1 | 4.90 |
| CHEMBL1082615 | — | — | 1 | 4.57 |
| CHEMBL1083280 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083028 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1083279 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1083027 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1083278 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1083029 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL1083281 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL1082972 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL1082655 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL1082615 | — | Ki | = | 26700.0 | nM | 4.57 |
| CHEMBL1083280 | — | Ki | = | 31200.0 | nM | 4.51 |