Assay Detail
Binding
CHEMBL3877553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha4beta2 expressed in human SH-EP1 cells assessed as reduction in carbamylcholine induced 86Rb+ efflux preincubated for 10 mins followed by carbamylcholine addition measured after 5 mins by Cherenkov counting
20
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.51 | 7.80 |
| Efficacy | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3948977 | — | — | 3 | 7.80 |
| CHEMBL3898434 | — | — | 3 | 7.80 |
| CHEMBL3970672 | — | — | 3 | 7.29 |
| CHEMBL3926480 | — | — | 2 | 6.77 |
| CHEMBL3889475 | — | — | 3 | - |
| CHEMBL3899499 | — | — | 3 | - |
| CHEMBL3908556 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3948977 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3898434 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3948977 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3898434 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL3970672 | — | IC50 | = | 50.8 | nM | 7.29 |
| CHEMBL3970672 | — | IC50 | = | 51.29 | nM | 7.29 |
| CHEMBL3926480 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL3889475 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3899499 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3908556 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3889475 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3908556 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3948977 | — | Efficacy | = | 74.0 | % | - |
| CHEMBL3889475 | — | Efficacy | - | — | - | |
| CHEMBL3926480 | — | Efficacy | - | — | - | |
| CHEMBL3898434 | — | Efficacy | = | 79.0 | % | - |
| CHEMBL3899499 | — | Efficacy | - | — | - | |
| CHEMBL3970672 | — | Efficacy | = | 68.0 | % | - |
| CHEMBL3908556 | — | Efficacy | - | — | - | |
| CHEMBL3899499 | — | IC50 | > | 1000.0 | nM | - |