Assay Detail
Binding
CHEMBL3610684
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced mean current response by two-electrode voltage clamp electrophysiology assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.63 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 6.70 |
| CHEMBL3608514 | — | — | 1 | 5.92 |
| CHEMBL243971 | — | — | 1 | 5.89 |
| CHEMBL3608518 | — | — | 1 | 5.75 |
| CHEMBL3608516 | — | — | 1 | 5.57 |
| CHEMBL3608511 | — | — | 1 | 5.54 |
| CHEMBL3608515 | — | — | 1 | 5.19 |
| CHEMBL3608510 | — | — | 1 | 5.15 |
| CHEMBL3608512 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3608514 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL243971 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3608518 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3608516 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3608511 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3608515 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3608510 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3608512 | — | IC50 | = | 11000.0 | nM | 4.96 |