Assay Detail
Binding
CHEMBL2184686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in CHO cells after 2 hrs by liquid scintillation counting
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| 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 |
|---|---|---|---|
| Ki | 58 | 5.36 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179964 | — | — | 1 | 6.96 |
| CHEMBL2179962 | — | — | 1 | 6.96 |
| CHEMBL2179965 | — | — | 1 | 6.70 |
| CHEMBL2179963 | — | — | 1 | 6.38 |
| CHEMBL2179970 | — | — | 1 | 6.35 |
| CHEMBL2179554 | — | — | 1 | 6.22 |
| CHEMBL2179961 | — | — | 1 | 6.17 |
| CHEMBL2179557 | — | — | 1 | 6.05 |
| CHEMBL2179540 | — | — | 1 | 5.96 |
| CHEMBL2179525 | — | — | 1 | 5.82 |
| CHEMBL2179558 | — | — | 1 | 5.82 |
| CHEMBL2179969 | — | — | 1 | 5.77 |
| CHEMBL2179968 | — | — | 1 | 5.77 |
| CHEMBL2179539 | — | — | 1 | 5.66 |
| CHEMBL2179531 | — | — | 1 | 5.62 |
| CHEMBL2179556 | — | — | 1 | 5.52 |
| CHEMBL2179537 | — | — | 1 | 5.50 |
| CHEMBL2179541 | — | — | 1 | 5.50 |
| CHEMBL2179534 | — | — | 1 | 5.42 |
| CHEMBL2179517 | — | — | 1 | 5.36 |
| CHEMBL2179535 | — | — | 1 | 5.32 |
| CHEMBL2179559 | — | — | 1 | 5.32 |
| CHEMBL2179555 | — | — | 1 | 5.28 |
| CHEMBL2179971 | — | — | 1 | 5.27 |
| CHEMBL2179528 | — | — | 1 | 5.19 |
| CHEMBL2179543 | — | — | 1 | 5.19 |
| CHEMBL2179546 | — | — | 1 | 5.19 |
| CHEMBL2179548 | — | — | 1 | 5.19 |
| CHEMBL2179544 | — | — | 1 | 5.18 |
| CHEMBL2179530 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179964 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2179962 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2179965 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2179963 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL2179970 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL2179554 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL2179961 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL2179557 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL2179540 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2179525 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2179558 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2179969 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL2179968 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL2179539 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL2179531 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL2179556 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2179537 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL2179541 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL2179534 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL2179517 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL2179535 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL2179559 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL2179555 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL2179971 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL2179548 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL2179543 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL2179528 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL2179546 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL2179544 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL2179530 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL2179956 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL2179532 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL2179533 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL2179967 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL2179527 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL2179520 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL2179545 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL2179536 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL2179547 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL2179957 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL2179526 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL2179521 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL2179519 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL2179518 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL2179549 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL2179516 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL2179523 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL2179966 | — | Ki | = | 72000.0 | nM | 4.14 |
| CHEMBL2179522 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2179560 | — | Ki | = | 100000.0 | nM | 4.00 |