Assay Detail
Binding
CHEMBL5534958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha3beta4 nAChR expressed in HEK293 cells assessed as inhibition of nicotine induced calcium flux preincubated for 10 mins followed by nicotine addition and measured for 5 mins by FLIPR assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.88 | 6.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5572105 | — | — | 1 | 6.25 |
| CHEMBL5571457 | — | — | 1 | 5.98 |
| CHEMBL5595517 | — | — | 1 | 5.96 |
| CHEMBL5574911 | — | — | 1 | 5.92 |
| CHEMBL5569258 | — | — | 1 | 5.84 |
| CHEMBL5572459 | — | — | 1 | 5.83 |
| CHEMBL5570620 | — | — | 1 | 5.80 |
| CHEMBL5575320 | — | — | 1 | 5.67 |
| CHEMBL5572736 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5572105 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5571457 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5595517 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5574911 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL5569258 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL5572459 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL5570620 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL5575320 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5572736 | — | IC50 | = | 2130.0 | nM | 5.67 |