Assay Detail
Binding
CHEMBL3877552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells after 9.5 mins by 86Rb+ efflux assay
13
Total Activities
7
Compounds Tested
1
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 |
|---|---|---|---|
| EC50 | 13 | 7.58 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3948977 | — | — | 2 | 7.80 |
| CHEMBL3898434 | — | — | 2 | 7.77 |
| CHEMBL3970672 | — | — | 2 | 7.51 |
| CHEMBL3926480 | — | — | 1 | 6.90 |
| CHEMBL3889475 | — | — | 2 | - |
| CHEMBL3899499 | — | — | 2 | - |
| CHEMBL3908556 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3948977 | — | EC50 | = | 15.9 | nM | 7.80 |
| CHEMBL3948977 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3898434 | — | EC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3898434 | — | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL3970672 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL3970672 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL3926480 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3889475 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3899499 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3908556 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3889475 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3899499 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3908556 | — | EC50 | > | 1000.0 | nM | - |