Assay Detail
Binding
CHEMBL748246
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In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M2
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 8 | 6.09 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134641 | SABCOMELINE | 2.0 | 1 | 6.75 |
| CHEMBL132698 | — | — | 1 | 6.66 |
| CHEMBL344892 | — | — | 1 | 6.62 |
| CHEMBL137384 | — | — | 1 | 6.21 |
| CHEMBL135328 | — | — | 1 | 6.16 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.85 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.75 |
| CHEMBL341447 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134641 | SABCOMELINE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL132698 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL344892 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL137384 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL135328 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL14 | CARBACHOL | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL341447 | — | IC50 | = | 18000.0 | nM | 4.75 |