Assay Detail
Functional
CHEMBL2184684
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at alpha4beta2 nAChR in human SH-EP1 cells assessed as calcium flux by calcium4-based FLIPR assay
46
Total Activities
46
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 | 46 | 5.16 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1876219 | — | — | 1 | 6.77 |
| CHEMBL2179965 | — | — | 1 | 6.35 |
| CHEMBL2179961 | — | — | 1 | 6.33 |
| CHEMBL2179962 | — | — | 1 | 6.07 |
| CHEMBL2179527 | — | — | 1 | 5.85 |
| CHEMBL2179963 | — | — | 1 | 5.77 |
| CHEMBL2179964 | — | — | 1 | 5.77 |
| CHEMBL2179554 | — | — | 1 | 5.77 |
| CHEMBL2179967 | — | — | 1 | 5.72 |
| CHEMBL2179557 | — | — | 1 | 5.68 |
| CHEMBL2179968 | — | — | 1 | 5.58 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 5.52 |
| CHEMBL2179555 | — | — | 1 | 5.52 |
| CHEMBL2179957 | — | — | 1 | 5.38 |
| CHEMBL2179534 | — | — | 1 | 5.38 |
| CHEMBL2179523 | — | — | 1 | 5.37 |
| CHEMBL2179966 | — | — | 1 | 5.35 |
| CHEMBL2179969 | — | — | 1 | 5.33 |
| CHEMBL2179556 | — | — | 1 | 5.32 |
| CHEMBL2179528 | — | — | 1 | 5.32 |
| CHEMBL2179529 | AZD1446 | 2.0 | 1 | 5.31 |
| CHEMBL2179559 | — | — | 1 | 5.24 |
| CHEMBL2179526 | — | — | 1 | 5.24 |
| CHEMBL2179533 | — | — | 1 | 5.19 |
| CHEMBL2179516 | — | — | 1 | 5.17 |
| CHEMBL2179956 | — | — | 1 | 5.17 |
| CHEMBL2179970 | — | — | 1 | 5.13 |
| CHEMBL2179530 | — | — | 1 | 4.96 |
| CHEMBL2179536 | — | — | 1 | 4.96 |
| CHEMBL2179558 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1876219 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2179965 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2179961 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2179962 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL2179527 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2179963 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2179964 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2179554 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2179967 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2179557 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2179968 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3 | NICOTINE | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2179555 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2179957 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2179534 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2179523 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2179966 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2179969 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2179556 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2179528 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2179529 | AZD1446 | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2179559 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2179526 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2179533 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2179956 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL2179516 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL2179970 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2179530 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2179536 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2179558 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2179539 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2179531 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2179524 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2179971 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2179532 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179538 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2179535 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2179517 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2179560 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2179518 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2179519 | — | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL2179525 | — | EC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2179520 | — | EC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL2179521 | — | EC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL2179537 | — | EC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL2179522 | — | EC50 | = | 100000.0 | nM | 4.00 |