Assay Detail
Binding
CHEMBL744131
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In vitro affinity evaluated using [3H]- quinuclidinyl benzilate as radioligand in rat cerebral cortex for muscarinic acetylcholine receptor
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 5.46 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135645 | — | — | 1 | 6.66 |
| CHEMBL134641 | SABCOMELINE | 2.0 | 1 | 6.51 |
| CHEMBL336590 | — | — | 1 | 6.33 |
| CHEMBL135604 | — | — | 1 | 5.96 |
| CHEMBL134345 | — | — | 1 | 5.95 |
| CHEMBL137374 | — | — | 1 | 5.89 |
| CHEMBL344892 | — | — | 1 | 5.71 |
| CHEMBL134288 | — | — | 1 | 5.71 |
| CHEMBL335254 | — | — | 1 | 5.70 |
| CHEMBL341766 | — | — | 1 | 5.66 |
| CHEMBL335324 | — | — | 1 | 5.64 |
| CHEMBL137384 | — | — | 1 | 5.64 |
| CHEMBL135229 | — | — | 1 | 5.64 |
| CHEMBL167982 | — | — | 1 | 5.62 |
| CHEMBL134660 | — | — | 1 | 5.54 |
| CHEMBL135705 | — | — | 1 | 5.54 |
| CHEMBL137385 | — | — | 1 | 5.52 |
| CHEMBL135260 | — | — | 1 | 5.52 |
| CHEMBL336162 | — | — | 1 | 5.52 |
| CHEMBL341379 | — | — | 1 | 5.51 |
| CHEMBL132698 | — | — | 1 | 5.51 |
| CHEMBL135328 | — | — | 1 | 5.50 |
| CHEMBL137816 | — | — | 1 | 5.47 |
| CHEMBL134456 | — | — | 1 | 5.44 |
| CHEMBL342468 | — | — | 1 | 5.43 |
| CHEMBL136920 | — | — | 1 | 5.28 |
| CHEMBL137717 | — | — | 1 | 5.28 |
| CHEMBL133372 | — | — | 1 | 5.24 |
| CHEMBL336279 | — | — | 1 | 5.12 |
| CHEMBL334674 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135645 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL134641 | SABCOMELINE | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL336590 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL135604 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL134345 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL137374 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL344892 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL134288 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL335254 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL341766 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL137384 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL135229 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL335324 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL167982 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL135705 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL134660 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL137385 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL135260 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL336162 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL341379 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL132698 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL135328 | — | IC50 | = | 3175.0 | nM | 5.50 |
| CHEMBL137816 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL134456 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL342468 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL136920 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL137717 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL133372 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL336279 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL334674 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL336727 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL337400 | — | IC50 | = | 8880.0 | nM | 5.05 |
| CHEMBL132864 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL439977 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL135836 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL14648 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL135670 | — | IC50 | = | 38000.0 | nM | 4.42 |