The discovery of new spirocyclic muscarinic M3 antagonists.

Article Details

Citation

Stocks MJ, Alcaraz L, Bailey A, Bowers K, Donald D, Edwards H, Hunt F, Kindon N, Pairaudeau G, Theaker J, Warner DJ

The discovery of new spirocyclic muscarinic M3 antagonists.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7458-61. doi: 10.1016/j.bmcl.2010.10.016. Epub 2010 Oct 28.

PubMed ID
21036043 [ View in PubMed
]
Abstract

The optimisation of a new series of high potency muscarinic M3 antagonists, derived from high throughput screening library hit is described.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AclidiniumMuscarinic acetylcholine receptor M1IC 50 (nM)0.1N/AN/ADetails
AclidiniumMuscarinic acetylcholine receptor M2IC 50 (nM)0.126N/AN/ADetails
AclidiniumMuscarinic acetylcholine receptor M3IC 50 (nM)0.126N/AN/ADetails
AclidiniumMuscarinic acetylcholine receptor M4IC 50 (nM)0.2N/AN/ADetails
AclidiniumMuscarinic acetylcholine receptor M5IC 50 (nM)0.158N/AN/ADetails