Assay Detail
Binding
CHEMBL2410848
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha4beta2 nAChR expressed in HEK-tsA201 cells assessed as inhibition of epibatidine-induced intracellular calcium level by fluorescence plate reader analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-tsA201 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: pharmacophore modeling and structure-activity relationship studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 4.77 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267936 | MECAMYLAMINE | 4.0 | 1 | 6.22 |
| CHEMBL2407120 | — | — | 1 | 5.22 |
| CHEMBL2407121 | — | — | 1 | 5.12 |
| CHEMBL1687 | — | — | 1 | 5.04 |
| CHEMBL2407128 | — | — | 1 | 4.83 |
| CHEMBL2407134 | — | — | 1 | 4.81 |
| CHEMBL152025 | — | — | 1 | 4.77 |
| CHEMBL2407122 | — | — | 1 | 4.71 |
| CHEMBL2407123 | — | — | 1 | 4.71 |
| CHEMBL2407124 | — | — | 1 | 4.71 |
| CHEMBL2407127 | — | — | 1 | 4.69 |
| CHEMBL2407129 | — | — | 1 | 4.65 |
| CHEMBL2407132 | — | — | 1 | 4.63 |
| CHEMBL2407133 | — | — | 1 | 4.42 |
| CHEMBL2407135 | — | — | 1 | 4.27 |
| CHEMBL2407125 | — | — | 1 | 4.15 |
| CHEMBL2407130 | — | — | 1 | 4.09 |
| CHEMBL2407126 | — | — | 1 | - |
| CHEMBL2407131 | — | — | 1 | - |
| CHEMBL2409794 | — | — | 1 | - |
| CHEMBL2407136 | — | — | 1 | - |
| CHEMBL2407137 | — | — | 1 | - |
| CHEMBL2407138 | — | — | 1 | - |
| CHEMBL2407139 | — | — | 1 | - |
| CHEMBL2407140 | — | — | 1 | - |
| CHEMBL2407141 | — | — | 1 | - |
| CHEMBL2409791 | — | — | 1 | - |
| CHEMBL2409792 | — | — | 1 | - |
| CHEMBL2409793 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267936 | MECAMYLAMINE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2407120 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2407121 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL1687 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2407128 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL2407134 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL152025 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL2407122 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL2407123 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL2407124 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL2407127 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL2407129 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL2407132 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL2407133 | — | IC50 | = | 37600.0 | nM | 4.42 |
| CHEMBL2407135 | — | IC50 | = | 54100.0 | nM | 4.27 |
| CHEMBL2407125 | — | IC50 | = | 70100.0 | nM | 4.15 |
| CHEMBL2407130 | — | IC50 | = | 80700.0 | nM | 4.09 |
| CHEMBL2407126 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407131 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2409794 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407136 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407137 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407138 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407139 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407140 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407141 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2409791 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2409792 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2409793 | — | IC50 | > | 100000.0 | nM | - |