Assay Detail
Binding
CHEMBL744135
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In vitro displacement of [3H]oxotremorine-M from muscarinic 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
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| 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 | 5.72 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148107 | — | — | 1 | 7.72 |
| CHEMBL291780 | — | — | 1 | 6.56 |
| CHEMBL342567 | — | — | 1 | 6.51 |
| CHEMBL356088 | — | — | 1 | 6.43 |
| CHEMBL343458 | — | — | 1 | 6.38 |
| CHEMBL147965 | — | — | 1 | 6.25 |
| CHEMBL58416 | — | — | 1 | 6.18 |
| CHEMBL358977 | — | — | 1 | 6.07 |
| CHEMBL344781 | — | — | 1 | 6.06 |
| CHEMBL60656 | — | — | 1 | 6.05 |
| CHEMBL148144 | — | — | 1 | 6.04 |
| CHEMBL291442 | — | — | 1 | 5.99 |
| CHEMBL344573 | — | — | 1 | 5.84 |
| CHEMBL342546 | — | — | 1 | 5.83 |
| CHEMBL144540 | — | — | 1 | 5.80 |
| CHEMBL293142 | — | — | 1 | 5.74 |
| CHEMBL341677 | — | — | 1 | 5.71 |
| CHEMBL147563 | — | — | 1 | 5.64 |
| CHEMBL148432 | — | — | 1 | 5.64 |
| CHEMBL149831 | — | — | 1 | 5.48 |
| CHEMBL146176 | — | — | 1 | 5.40 |
| CHEMBL144412 | — | — | 1 | 5.36 |
| CHEMBL358576 | — | — | 1 | 5.24 |
| CHEMBL145976 | — | — | 1 | 5.16 |
| CHEMBL148738 | — | — | 1 | 5.14 |
| CHEMBL147397 | — | — | 1 | 5.02 |
| CHEMBL145969 | — | — | 1 | 4.80 |
| CHEMBL358535 | — | — | 1 | 4.71 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 4.50 |
| CHEMBL274525 | ABT-418 | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148107 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL291780 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL342567 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL356088 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL343458 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL147965 | — | IC50 | = | 566.0 | nM | 6.25 |
| CHEMBL58416 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL358977 | — | IC50 | = | 852.0 | nM | 6.07 |
| CHEMBL344781 | — | IC50 | = | 867.0 | nM | 6.06 |
| CHEMBL60656 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL148144 | — | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL291442 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL344573 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL342546 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL144540 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL293142 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL341677 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL147563 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL148432 | — | IC50 | = | 2263.0 | nM | 5.64 |
| CHEMBL149831 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL146176 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL144412 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL358576 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL145976 | — | IC50 | = | 6950.0 | nM | 5.16 |
| CHEMBL148738 | — | IC50 | = | 7220.0 | nM | 5.14 |
| CHEMBL147397 | — | IC50 | = | 9540.0 | nM | 5.02 |
| CHEMBL145969 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL358535 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL3 | NICOTINE | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL274525 | ABT-418 | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL6623 | EPIBATIDINE | IC50 | > | 1.0 | nM | - |