Assay Detail
Binding
CHEMBL744321
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In vitro affinity against human Muscarinic acetylcholine receptor M1 using quinuclidynyl benzylate (QNB)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 9 | 5.67 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135645 | — | — | 1 | 7.00 |
| CHEMBL134641 | SABCOMELINE | 2.0 | 1 | 6.77 |
| CHEMBL137384 | — | — | 1 | 5.93 |
| CHEMBL135328 | — | — | 1 | 5.82 |
| CHEMBL344892 | — | — | 1 | 5.78 |
| CHEMBL132698 | — | — | 1 | 5.00 |
| CHEMBL341447 | — | — | 1 | 4.89 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 4.19 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135645 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL134641 | SABCOMELINE | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL137384 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL135328 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL344892 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL132698 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL341447 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL14 | CARBACHOL | IC50 | = | 150000.0 | nM | - |