Assay Detail
Functional
CHEMBL2183118
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at high sensitivity and low sensitivity alpha4beta2-nAChR expressed in human SH-EP1 cells assessed as inhibition of carbamylcholine-induced stimulation effect measured after 10 mins carbamylcholine challenge by 86Rb+ ion flux assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.90 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177344 | — | — | 1 | 8.07 |
| CHEMBL2177345 | — | — | 1 | 7.99 |
| CHEMBL2177346 | — | — | 1 | 7.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177344 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2177345 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL2177346 | — | IC50 | = | 22.2 | nM | 7.65 |