Assay Detail
Binding
CHEMBL2185121
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat cortex 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 | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 7.33 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179963 | — | — | 1 | 9.00 |
| CHEMBL2179519 | — | — | 1 | 8.96 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.70 |
| CHEMBL2179962 | — | — | 1 | 8.70 |
| CHEMBL1876219 | — | — | 1 | 8.22 |
| CHEMBL2179961 | — | — | 1 | 8.15 |
| CHEMBL2179543 | — | — | 1 | 8.15 |
| CHEMBL2179534 | — | — | 1 | 8.10 |
| CHEMBL2179964 | — | — | 1 | 8.00 |
| CHEMBL2179970 | — | — | 1 | 7.96 |
| CHEMBL2179531 | — | — | 1 | 7.92 |
| CHEMBL2179540 | — | — | 1 | 7.82 |
| CHEMBL2179557 | — | — | 1 | 7.77 |
| CHEMBL2179968 | — | — | 1 | 7.72 |
| CHEMBL2179971 | — | — | 1 | 7.70 |
| CHEMBL2179965 | — | — | 1 | 7.66 |
| CHEMBL2179539 | — | — | 1 | 7.66 |
| CHEMBL2179525 | — | — | 1 | 7.60 |
| CHEMBL2179550 | — | — | 1 | 7.57 |
| CHEMBL2179541 | — | — | 1 | 7.55 |
| CHEMBL2179967 | — | — | 1 | 7.54 |
| CHEMBL2179529 | AZD1446 | 2.0 | 1 | 7.47 |
| CHEMBL2179527 | — | — | 1 | 7.44 |
| CHEMBL2179521 | — | — | 1 | 7.41 |
| CHEMBL2179544 | — | — | 1 | 7.40 |
| CHEMBL2179956 | — | — | 1 | 7.33 |
| CHEMBL2179535 | — | — | 1 | 7.30 |
| CHEMBL2179526 | — | — | 1 | 7.29 |
| CHEMBL2179559 | — | — | 1 | 7.28 |
| CHEMBL2179966 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179963 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2179519 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2179962 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3 | NICOTINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1876219 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2179961 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2179543 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2179534 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2179964 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2179970 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2179531 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2179540 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2179557 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2179968 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2179971 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2179965 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2179539 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2179525 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2179550 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2179541 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2179967 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2179529 | AZD1446 | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2179527 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2179521 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL2179544 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2179956 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2179535 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2179526 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL2179559 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2179966 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2179528 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2179524 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL2179558 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL2179547 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL2179516 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2179530 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL2179537 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2179549 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2179556 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2179533 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL2179969 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL2179546 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2179554 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2179555 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2179536 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2179545 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2179548 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2179957 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2179520 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2179517 | — | Ki | = | 160.0 | nM | 6.80 |