Assay Detail
Binding
CHEMBL750359
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was evaluated for its ability to displace [3H]-cytisine binding from high-affinity Nicotinic acetylcholine receptor in rat brain (principally the alpha4-beta2 nAChR subtype)
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor (CHEMBL2094110) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 9.87 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | 2.0 | 2 | 10.40 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.37 |
| CHEMBL262769 | — | — | 1 | 10.30 |
| CHEMBL334860 | — | — | 1 | 10.05 |
| CHEMBL132486 | — | — | 1 | 9.35 |
| CHEMBL59986 | — | — | 1 | 9.28 |
| CHEMBL133570 | — | — | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL430497 | TEBANICLINE | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL262769 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL334860 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL132486 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL59986 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL133570 | — | Ki | = | 1.6 | nM | 8.80 |