Assay Detail
Binding
CHEMBL747856
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro displacement of [3H]methylcarbamylcholine from nicotinic acetylcholine receptor in rat brain cortex
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor (CHEMBL2094110) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.45 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.52 |
| CHEMBL148107 | — | — | 1 | 9.49 |
| CHEMBL342567 | — | — | 1 | 8.78 |
| CHEMBL343458 | — | — | 1 | 8.49 |
| CHEMBL58416 | — | — | 1 | 8.41 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.18 |
| CHEMBL291442 | — | — | 1 | 7.64 |
| CHEMBL291780 | — | — | 1 | 7.54 |
| CHEMBL144540 | — | — | 1 | 7.28 |
| CHEMBL274525 | ABT-418 | — | 1 | 7.25 |
| CHEMBL148738 | — | — | 1 | 7.06 |
| CHEMBL147965 | — | — | 1 | 7.00 |
| CHEMBL148144 | — | — | 1 | 6.97 |
| CHEMBL60656 | — | — | 1 | 6.89 |
| CHEMBL358977 | — | — | 1 | 6.78 |
| CHEMBL342546 | — | — | 1 | 6.66 |
| CHEMBL344573 | — | — | 1 | 6.59 |
| CHEMBL293142 | — | — | 1 | 6.30 |
| CHEMBL148432 | — | — | 1 | 6.15 |
| CHEMBL144412 | — | — | 1 | 6.11 |
| CHEMBL147563 | — | — | 1 | - |
| CHEMBL341677 | — | — | 1 | - |
| CHEMBL358535 | — | — | 1 | - |
| CHEMBL145976 | — | — | 1 | - |
| CHEMBL344781 | — | — | 1 | - |
| CHEMBL146176 | — | — | 1 | - |
| CHEMBL149831 | — | — | 1 | - |
| CHEMBL145969 | — | — | 1 | - |
| CHEMBL358576 | — | — | 1 | - |
| CHEMBL356088 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL148107 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL342567 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL343458 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL58416 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3 | NICOTINE | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL291442 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL291780 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL144540 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL274525 | ABT-418 | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL148738 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL147965 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL148144 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL60656 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL358977 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL342546 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL344573 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL293142 | — | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL148432 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL144412 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL147563 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL341677 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL358535 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL145976 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL344781 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL146176 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL149831 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL145969 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL358576 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL356088 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL147397 | — | IC50 | > | 1000.0 | nM | - |