Assay Detail
Functional
CHEMBL2184680
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at alpha4beta2 nAChR in human SH-EP1 cells assessed as calcium flux by calcium4-based FLIPR assay
14
Total Activities
14
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/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.04 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179540 | — | — | 1 | 6.52 |
| CHEMBL2179541 | — | — | 1 | 6.10 |
| CHEMBL2179543 | — | — | 1 | 5.85 |
| CHEMBL2179549 | — | — | 1 | 5.15 |
| CHEMBL2179546 | — | — | 1 | 5.08 |
| CHEMBL2179552 | — | — | 1 | 5.07 |
| CHEMBL2179548 | — | — | 1 | 5.07 |
| CHEMBL2179547 | — | — | 1 | 4.75 |
| CHEMBL2179542 | — | — | 1 | 4.66 |
| CHEMBL2179553 | — | — | 1 | 4.60 |
| CHEMBL2179551 | — | — | 1 | 4.58 |
| CHEMBL2179545 | — | — | 1 | 4.12 |
| CHEMBL2179544 | — | — | 1 | 4.00 |
| CHEMBL2179550 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179540 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2179541 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2179543 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2179549 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2179546 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL2179552 | — | EC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2179548 | — | EC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2179547 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2179542 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179553 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2179551 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL2179545 | — | EC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL2179544 | — | EC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL2179550 | — | EC50 | = | 110000.0 | nM | - |