Assay Detail
Binding
CHEMBL4154648
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at alpha4beta2 nAChR (unknown origin)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2 nACh receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 9.77 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245243 | — | — | 1 | 10.74 |
| CHEMBL4168511 | — | — | 1 | 10.70 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 10.35 |
| CHEMBL4160595 | — | — | 1 | 9.82 |
| CHEMBL4169986 | — | — | 1 | 9.40 |
| CHEMBL4177192 | — | — | 1 | 9.02 |
| CHEMBL129801 | — | — | 1 | 8.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245243 | — | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL4168511 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3 | NICOTINE | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL4160595 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4169986 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4177192 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL129801 | — | Ki | = | 4.1 | nM | 8.39 |