Assay Detail
Functional
CHEMBL1064407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha3beta4 nAChR receptor in human SH-SY5Y cells assessed as inhibition of carbamylcholine-induced 86Rb+ efflux by liquid scintillation counting
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.38 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566208 | — | — | 1 | 9.29 |
| CHEMBL566886 | — | — | 1 | 9.24 |
| CHEMBL566050 | — | — | 1 | 9.21 |
| CHEMBL565844 | — | — | 1 | 9.19 |
| CHEMBL569465 | — | — | 1 | 9.15 |
| CHEMBL578612 | — | — | 1 | 8.92 |
| CHEMBL565396 | — | — | 1 | 8.89 |
| CHEMBL566001 | — | — | 1 | 8.85 |
| CHEMBL566832 | — | — | 1 | 8.82 |
| CHEMBL603620 | — | — | 1 | 8.70 |
| CHEMBL566000 | — | — | 1 | 8.62 |
| CHEMBL566207 | — | — | 1 | 8.62 |
| CHEMBL578610 | — | — | 1 | 8.59 |
| CHEMBL565845 | — | — | 1 | 8.54 |
| CHEMBL578611 | — | — | 1 | 8.51 |
| CHEMBL567481 | — | — | 1 | 8.48 |
| CHEMBL592854 | — | — | 1 | 8.43 |
| CHEMBL599846 | — | — | 1 | 8.41 |
| CHEMBL576063 | — | — | 1 | 8.36 |
| CHEMBL589250 | — | — | 1 | 8.33 |
| CHEMBL568140 | — | — | 1 | 8.17 |
| CHEMBL566420 | — | — | 1 | 8.11 |
| CHEMBL565386 | — | — | 1 | 8.00 |
| CHEMBL605501 | — | — | 1 | 7.96 |
| CHEMBL589494 | — | — | 1 | 7.96 |
| CHEMBL599230 | — | — | 1 | 7.96 |
| CHEMBL598026 | — | — | 1 | 7.96 |
| CHEMBL596775 | — | — | 1 | 7.82 |
| CHEMBL580143 | — | — | 1 | 7.80 |
| CHEMBL566618 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566208 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL566886 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL566050 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL565844 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL569465 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL578612 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL565396 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL566001 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL566832 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL603620 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL566000 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL566207 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL578610 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL565845 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL578611 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL567481 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL592854 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL599846 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL576063 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL589250 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL568140 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL566420 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL565386 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL605501 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL589494 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL599230 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL598026 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL596775 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL580143 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL566618 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL599028 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL566830 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL599233 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL894 | BUPROPION | IC50 | = | 1.8 | nM | - |