Assay Detail
Functional
CHEMBL884408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was evaluated for functional activation to [86Rb+] efflux from human K177 cells expressing recombinant alpha4-beta2 receptors.
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | K177 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
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 |
|---|---|---|---|
| EC50 | 4 | 6.59 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | 2.0 | 2 | 7.22 |
| CHEMBL262769 | — | — | 1 | 6.40 |
| CHEMBL59986 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL430497 | TEBANICLINE | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL262769 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL59986 | — | EC50 | = | 700.0 | nM | 6.16 |