Assay Detail
Functional
CHEMBL1176289
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha4beta4 nicotinic receptor in human SH-EP1 cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting
26
Total Activities
26
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/beta4 (CHEMBL1907591) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 4.51 | 5.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173701 | — | — | 1 | 5.09 |
| CHEMBL1173771 | — | — | 1 | 4.96 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 4.92 |
| CHEMBL1173770 | — | — | 1 | 4.89 |
| CHEMBL1173428 | — | — | 1 | 4.85 |
| CHEMBL1173772 | — | — | 1 | 4.80 |
| CHEMBL1173430 | — | — | 1 | 4.75 |
| CHEMBL1173597 | — | — | 1 | 4.75 |
| CHEMBL1172929 | — | — | 1 | 4.52 |
| CHEMBL1173276 | — | — | 1 | 4.52 |
| CHEMBL1173354 | — | — | 1 | 4.48 |
| CHEMBL1172928 | RADAFAXINE | 2.0 | 1 | 4.39 |
| CHEMBL1171260 | — | — | 1 | 4.37 |
| CHEMBL1173429 | — | — | 1 | 4.21 |
| CHEMBL1170441 | — | — | 1 | 4.21 |
| CHEMBL1173277 | — | — | 1 | 4.19 |
| CHEMBL1173355 | — | — | 1 | 4.14 |
| CHEMBL1173280 | — | — | 1 | 4.10 |
| CHEMBL1173274 | — | — | 1 | 4.04 |
| CHEMBL1173598 | — | — | 1 | 4.04 |
| CHEMBL1173279 | — | — | 1 | - |
| CHEMBL1173353 | — | — | 1 | - |
| CHEMBL1173600 | — | — | 1 | - |
| CHEMBL1173275 | — | — | 1 | - |
| CHEMBL1173427 | — | — | 1 | - |
| CHEMBL1173599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173701 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL1173771 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL894 | BUPROPION | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1173770 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1173428 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1173772 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1173430 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1173597 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1172929 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1173276 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1173354 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL1172928 | RADAFAXINE | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL1171260 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL1173429 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL1170441 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL1173277 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL1173355 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL1173280 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL1173274 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL1173598 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL1173279 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173353 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173600 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173275 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173427 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173599 | — | IC50 | > | 100000.0 | nM | - |