Assay Detail
Binding
CHEMBL2184685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha7 nAChR expressed in CHO cells after 2 hrs by liquid scintillation counting
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| 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 | 60 | 5.24 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179962 | — | — | 1 | 7.70 |
| CHEMBL2179964 | — | — | 1 | 7.40 |
| CHEMBL2179965 | — | — | 1 | 6.68 |
| CHEMBL2179963 | — | — | 1 | 6.46 |
| CHEMBL2179969 | — | — | 1 | 6.25 |
| CHEMBL2179961 | — | — | 1 | 6.08 |
| CHEMBL2179526 | — | — | 1 | 5.92 |
| CHEMBL2179525 | — | — | 1 | 5.89 |
| CHEMBL2179554 | — | — | 1 | 5.80 |
| CHEMBL2179531 | — | — | 1 | 5.58 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 5.52 |
| CHEMBL2179539 | — | — | 1 | 5.43 |
| CHEMBL2179533 | — | — | 1 | 5.34 |
| CHEMBL2179540 | — | — | 1 | 5.33 |
| CHEMBL2179970 | — | — | 1 | 5.26 |
| CHEMBL2179516 | — | — | 1 | 5.23 |
| CHEMBL2179966 | — | — | 1 | 5.23 |
| CHEMBL2179534 | — | — | 1 | 5.20 |
| CHEMBL2179529 | AZD1446 | 2.0 | 1 | 5.17 |
| CHEMBL2179957 | — | — | 1 | 5.12 |
| CHEMBL2179968 | — | — | 1 | 5.11 |
| CHEMBL2179967 | — | — | 1 | 5.09 |
| CHEMBL2179558 | — | — | 1 | 5.09 |
| CHEMBL2179538 | — | — | 1 | 5.09 |
| CHEMBL2179536 | — | — | 1 | 5.07 |
| CHEMBL2179537 | — | — | 1 | 5.06 |
| CHEMBL2179521 | — | — | 1 | 4.89 |
| CHEMBL2179556 | — | — | 1 | 4.85 |
| CHEMBL2179557 | — | — | 1 | 4.85 |
| CHEMBL2179555 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179962 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2179964 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2179965 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2179963 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2179969 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL2179961 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL2179526 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2179525 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL2179554 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL2179531 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL3 | NICOTINE | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2179539 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL2179533 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL2179540 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL2179970 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL2179516 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL2179966 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL2179534 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL2179529 | AZD1446 | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL2179957 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL2179968 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL2179967 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL2179558 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL2179538 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL2179536 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL2179537 | — | Ki | = | 8800.0 | nM | 5.06 |
| CHEMBL2179521 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL2179556 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL2179557 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL2179555 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL2179560 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL2179971 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL2179956 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL2179519 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL2179517 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL2179522 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL1876219 | — | Ki | = | 71000.0 | nM | 4.15 |
| CHEMBL2179523 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2179518 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2179520 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2179559 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL2179553 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179535 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179552 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179551 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179550 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179549 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179548 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179547 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2179546 | — | Ki | > | 10000.0 | nM | - |