Assay Detail
Binding
CHEMBL2410847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha3beta4 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; alpha3/beta4 (CHEMBL1907594) ↗| 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 | 4.73 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267936 | MECAMYLAMINE | 4.0 | 1 | 6.16 |
| CHEMBL1687 | — | — | 1 | 5.17 |
| CHEMBL2407121 | — | — | 1 | 4.96 |
| CHEMBL2407128 | — | — | 1 | 4.93 |
| CHEMBL2407134 | — | — | 1 | 4.90 |
| CHEMBL152025 | — | — | 1 | 4.76 |
| CHEMBL2407129 | — | — | 1 | 4.72 |
| CHEMBL2407123 | — | — | 1 | 4.66 |
| CHEMBL2407132 | — | — | 1 | 4.65 |
| CHEMBL2407122 | — | — | 1 | 4.61 |
| CHEMBL2407127 | — | — | 1 | 4.56 |
| CHEMBL2407133 | — | — | 1 | 4.54 |
| CHEMBL2407120 | — | — | 1 | 4.50 |
| CHEMBL2407124 | — | — | 1 | 4.21 |
| CHEMBL2407125 | — | — | 1 | 4.18 |
| CHEMBL2407135 | — | — | 1 | 4.11 |
| CHEMBL2407126 | — | — | 1 | - |
| CHEMBL2407131 | — | — | 1 | - |
| CHEMBL2407130 | — | — | 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 | = | 700.0 | nM | 6.16 |
| CHEMBL1687 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL2407121 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL2407128 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL2407134 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL152025 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL2407129 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL2407123 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL2407132 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL2407122 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL2407127 | — | IC50 | = | 27400.0 | nM | 4.56 |
| CHEMBL2407133 | — | IC50 | = | 29200.0 | nM | 4.54 |
| CHEMBL2407120 | — | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL2407124 | — | IC50 | = | 61400.0 | nM | 4.21 |
| CHEMBL2407125 | — | IC50 | = | 65500.0 | nM | 4.18 |
| CHEMBL2407135 | — | IC50 | = | 77800.0 | nM | 4.11 |
| CHEMBL2407126 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407131 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2407130 | — | 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 | - |