Biaryl amides were discovered as novel and subtype selective M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described. ..more
Target
| Sequence: RecName: Full=Muscarinic acetylcholine receptor M2 Description ..   Protein Family: Signal recognition particle, alpha subunit, N-terminal Comment .. Gene:CHRM2 Related Protein 3D Structures |
BioActive Compounds: 4
Description:
Title: 2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.
Abstract: Biaryl amides were discovered as novel and subtype selective M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described.
(PMID: 20483611)
Abstract: Biaryl amides were discovered as novel and subtype selective M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described.
(PMID: 20483611)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 47
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 47
ChEMBL target type: Target is a single protein chain
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | IC50* | IC50 PubChem standard value |  | Float | μM | |
| 2 | -Log EC50 activity comment | -Log EC50 activity comment | String | |||
| 3 | -Log EC50 standard flag | -Log EC50 standard flag | | Integer | ||
| 4 | -Log EC50 qualifier | -Log EC50 qualifier | String | |||
| 5 | -Log EC50 published value | -Log EC50 published value | | Float | ||
| 6 | -Log EC50 standard value | -Log EC50 standard value | | Float | ||
| 7 | IC50 activity comment | IC50 activity comment | String | |||
| 8 | IC50 standard flag | IC50 standard flag | | Integer | ||
| 9 | IC50 qualifier | IC50 qualifier | String | |||
| 10 | IC50 published value | IC50 published value | | Float | nM | |
| 11 | IC50 standard value | IC50 standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
Classification
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