Assay Detail

CHEMBL1913682

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Binding

Displacement of [3H]-NMS from human recombinant M2 receptor expressed in CHO cells after 24 hrs by filter binding assay

ChEMBL ↗

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Target

Muscarinic acetylcholine receptor M2 (CHEMBL211) ↗

Open DB target context

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Muscarinic acetylcholine receptor M2 (CHEMBL211) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Muscarinic acetylcholine receptor M2

CHEMBL211

Anchored from Assay target.

Protein identity Muscarinic acetylcholine receptor M2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	CHO
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.

Glossop PA, Watson CA, Price DA, Bunnage ME, Middleton DS, Wood A, James K, Roberts D, Strang RS, Yeadon M, Perros-Huguet C, Clarke NP, Trevethick MA, Machin I, Stuart EF, Evans SM, Harrison AC, Fairman DA, Agoram B, Burrows JL, Feeder N, Fulton CK, Dillon BR, Entwistle DA, Spence FJ.
J Med Chem (2011) 54 : 6888 -6904
PubMed 21870878 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	3	9.97	10.67

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3545181	TIOTROPIUM BROMIDE	4.0	1	10.67
CHEMBL1910856	PF-03635659	2.0	1	9.86
CHEMBL1908368	—	—	1	9.38

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3545181	TIOTROPIUM BROMIDE	Ki	=	0.0215	nM	10.67
CHEMBL1910856	PF-03635659	Ki	=	0.137	nM	9.86
CHEMBL1908368	—	Ki	=	0.413	nM	9.38