Assay Detail
Binding
CHEMBL1020766
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Displacement of [3H]epibatidine from alpha4beta2 nAChR expressed in HEK293 cells
43
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 5.74 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL466400 | — | — | 1 | 7.89 |
| CHEMBL451633 | — | — | 2 | 7.44 |
| CHEMBL466399 | — | — | 2 | 7.32 |
| CHEMBL448084 | — | — | 2 | 7.04 |
| CHEMBL500318 | — | — | 2 | 6.90 |
| CHEMBL501227 | — | — | 2 | 6.70 |
| CHEMBL468697 | — | — | 2 | 6.54 |
| CHEMBL445169 | — | — | 2 | 5.96 |
| CHEMBL468903 | — | — | 2 | 5.82 |
| CHEMBL479622 | — | — | 2 | 5.80 |
| CHEMBL480797 | — | — | 2 | 5.80 |
| CHEMBL449334 | — | — | 2 | 5.72 |
| CHEMBL480798 | — | — | 2 | 5.44 |
| CHEMBL480799 | — | — | 2 | 5.20 |
| CHEMBL503940 | — | — | 2 | 5.20 |
| CHEMBL479623 | — | — | 2 | 5.01 |
| CHEMBL499575 | — | — | 2 | 4.92 |
| CHEMBL466398 | — | — | 2 | 4.64 |
| CHEMBL479429 | — | — | 2 | 4.50 |
| CHEMBL479015 | — | — | 2 | 4.40 |
| CHEMBL457965 | — | — | 2 | 4.00 |
| CHEMBL449566 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL466400 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL451633 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL451633 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL466399 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL466399 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL448084 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL448084 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL500318 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL500318 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL501227 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL501227 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL468697 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL468697 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL445169 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL468903 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL479622 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL480797 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL479622 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL468903 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL480797 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL449334 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL449334 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL480798 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL480798 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL503940 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL480799 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL480799 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL503940 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL479623 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL445169 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL479623 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL499575 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL499575 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL466398 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL466398 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL479429 | — | Ki | = | 31622.78 | nM | 4.50 |
| CHEMBL479429 | — | Ki | = | 35000.0 | nM | 4.46 |
| CHEMBL479015 | — | Ki | = | 39810.72 | nM | 4.40 |
| CHEMBL479015 | — | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL457965 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL457965 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL449566 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL449566 | — | Ki | = | 300000.0 | nM | - |