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Assay Detail

CHEMBL1913621

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
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 M3 (CHEMBL245)
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 6 9.76 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1910856 PF-03635659 2.0 1 9.89
CHEMBL1910865 1 9.79
CHEMBL1910851 1 9.74
CHEMBL1910850 1 9.70
CHEMBL1908368 1 9.67
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1910856 PF-03635659 Ki = 0.128 nM 9.89
CHEMBL1910865 Ki = 0.163 nM 9.79
CHEMBL1910851 Ki = 0.18 nM 9.74
CHEMBL1910850 Ki = 0.201 nM 9.70
CHEMBL1908368 Ki = 0.213 nM 9.67
CHEMBL3545181 TIOTROPIUM BROMIDE Ki = 0.0098 nM -