Assay Detail
Functional
CHEMBL964079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.99 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | 2.0 | 1 | 7.70 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 6.92 |
| CHEMBL494773 | — | — | 1 | 5.80 |
| CHEMBL492593 | — | — | 1 | 5.60 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 5.33 |
| CHEMBL449142 | — | — | 1 | 4.60 |
| CHEMBL389964 | — | — | 1 | - |
| CHEMBL509239 | — | — | 1 | - |
| CHEMBL504652 | TC-2216 | 1.0 | 1 | - |
| CHEMBL504126 | — | — | 1 | - |
| CHEMBL504595 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430497 | TEBANICLINE | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL494773 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL492593 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3 | NICOTINE | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL449142 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL389964 | — | EC50 | - | — | - | |
| CHEMBL509239 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL504652 | TC-2216 | EC50 | > | 100000.0 | nM | - |
| CHEMBL504126 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL504595 | — | EC50 | > | 100000.0 | nM | - |