Assay Detail
Binding
CHEMBL4604683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in CHOK1 cell membrane by microbeta scintillation counting method
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 64 | 7.63 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 10.40 |
| CHEMBL4636163 | — | — | 1 | 9.85 |
| CHEMBL4638732 | — | — | 1 | 9.72 |
| CHEMBL4647019 | — | — | 1 | 9.70 |
| CHEMBL4647198 | — | — | 1 | 9.70 |
| CHEMBL4644169 | — | — | 1 | 9.43 |
| CHEMBL4648557 | — | — | 1 | 9.00 |
| CHEMBL4638919 | — | — | 1 | 8.96 |
| CHEMBL4648098 | — | — | 1 | 8.92 |
| CHEMBL4634253 | — | — | 1 | 8.86 |
| CHEMBL4642118 | — | — | 1 | 8.82 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.66 |
| CHEMBL4637076 | — | — | 1 | 8.57 |
| CHEMBL4634110 | — | — | 1 | 8.54 |
| CHEMBL4648968 | — | — | 1 | 8.47 |
| CHEMBL4642769 | — | — | 1 | 8.44 |
| CHEMBL4642865 | — | — | 1 | 8.41 |
| CHEMBL4634727 | — | — | 1 | 8.38 |
| CHEMBL4637371 | — | — | 1 | 8.33 |
| CHEMBL4649539 | — | — | 1 | 8.26 |
| CHEMBL4645367 | — | — | 1 | 8.19 |
| CHEMBL4637698 | — | — | 1 | 8.19 |
| CHEMBL4643942 | — | — | 1 | 8.10 |
| CHEMBL4641432 | — | — | 1 | 7.94 |
| CHEMBL4640279 | — | — | 1 | 7.76 |
| CHEMBL4645127 | — | — | 1 | 7.76 |
| CHEMBL504652 | TC-2216 | 1.0 | 1 | 7.73 |
| CHEMBL4646061 | — | — | 1 | 7.70 |
| CHEMBL4642287 | — | — | 1 | 7.69 |
| CHEMBL127071 | POZANICLINE | 2.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL4636163 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4638732 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL4647019 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4647198 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4644169 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL4648557 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4638919 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4648098 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4634253 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL4642118 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3 | NICOTINE | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4637076 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4634110 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4648968 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4642769 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4642865 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4634727 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL4637371 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL4649539 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4645367 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4637698 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4643942 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL4641432 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL4645127 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL4640279 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL504652 | TC-2216 | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL4646061 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4642287 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL127071 | POZANICLINE | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4639792 | — | Ki | = | 26.2 | nM | 7.58 |
| CHEMBL4634566 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL4640410 | — | Ki | = | 31.9 | nM | 7.50 |
| CHEMBL4646023 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL4641810 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4640566 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL4636272 | — | Ki | = | 131.1 | nM | 6.88 |
| CHEMBL4646643 | — | Ki | = | 149.2 | nM | 6.83 |
| CHEMBL4637361 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL4642328 | — | Ki | = | 241.9 | nM | 6.62 |
| CHEMBL4637625 | — | Ki | = | 265.4 | nM | 6.58 |
| CHEMBL4638726 | — | Ki | = | 327.1 | nM | 6.49 |
| CHEMBL4634584 | — | Ki | = | 327.3 | nM | 6.49 |
| CHEMBL4649507 | — | Ki | = | 329.3 | nM | 6.48 |
| CHEMBL4640672 | — | Ki | = | 340.7 | nM | 6.47 |
| CHEMBL4636268 | — | Ki | = | 394.7 | nM | 6.40 |
| CHEMBL4642416 | — | Ki | = | 407.3 | nM | 6.39 |
| CHEMBL4639862 | — | Ki | = | 577.4 | nM | 6.24 |
| CHEMBL4640520 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL4638072 | — | Ki | = | 768.0 | nM | 6.12 |