Assay Detail
Binding
CHEMBL744130
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro affinity evaluated using [3H]- oxotremorine 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 | 7.16 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341379 | — | — | 1 | 8.07 |
| CHEMBL135645 | — | — | 1 | 7.96 |
| CHEMBL134641 | SABCOMELINE | 2.0 | 1 | 7.85 |
| CHEMBL132698 | — | — | 1 | 7.82 |
| CHEMBL344892 | — | — | 1 | 7.72 |
| CHEMBL135328 | — | — | 1 | 7.68 |
| CHEMBL137384 | — | — | 1 | 7.64 |
| CHEMBL134288 | — | — | 1 | 7.60 |
| CHEMBL336590 | — | — | 1 | 7.48 |
| CHEMBL341766 | — | — | 1 | 7.47 |
| CHEMBL167982 | — | — | 1 | 7.37 |
| CHEMBL135836 | — | — | 1 | 7.36 |
| CHEMBL137816 | — | — | 1 | 7.34 |
| CHEMBL336727 | — | — | 1 | 7.29 |
| CHEMBL439977 | — | — | 1 | 7.26 |
| CHEMBL137385 | — | — | 1 | 7.23 |
| CHEMBL136920 | — | — | 1 | 7.22 |
| CHEMBL135260 | — | — | 1 | 7.19 |
| CHEMBL135604 | — | — | 1 | 7.16 |
| CHEMBL335254 | — | — | 1 | 7.16 |
| CHEMBL336162 | — | — | 1 | 7.14 |
| CHEMBL133372 | — | — | 1 | 7.02 |
| CHEMBL336279 | — | — | 1 | 7.00 |
| CHEMBL337400 | — | — | 1 | 7.00 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.94 |
| CHEMBL134660 | — | — | 1 | 6.94 |
| CHEMBL135670 | — | — | 1 | 6.92 |
| CHEMBL134345 | — | — | 1 | 6.85 |
| CHEMBL342468 | — | — | 1 | 6.80 |
| CHEMBL334674 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341379 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL135645 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL134641 | SABCOMELINE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL132698 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL344892 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL135328 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL137384 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL134288 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL336590 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL341766 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL167982 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL135836 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL137816 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL336727 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL439977 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL137385 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL136920 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL135260 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL335254 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL135604 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL336162 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL133372 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL336279 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL337400 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL134660 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL135670 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL134345 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL342468 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL334674 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL135229 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL335324 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL137717 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL137374 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL134456 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL132864 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL135705 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL14648 | — | IC50 | = | 520.0 | nM | 6.28 |