Assay Detail
Binding
CHEMBL5147135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at high sensitivity isoform human (alpha4)2(beta2)3 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response at holding potential of -50 mV by two-electrode voltage clamp technique
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyrrolidinyl benzofurans and benzodioxanes: Selective α4β2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.21 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917231 | — | — | 1 | 6.89 |
| CHEMBL4785648 | — | — | 1 | 6.10 |
| CHEMBL5183330 | — | — | 1 | 5.63 |
| CHEMBL4741357 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917231 | — | EC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4785648 | — | EC50 | = | 799.0 | nM | 6.10 |
| CHEMBL5183330 | — | EC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4741357 | — | EC50 | - | — | - |