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Assay Detail

CHEMBL1913618

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 2 hrs by filter binding assay
7
Total Activities
7
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 7 9.10 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 10.12
CHEMBL1910848 1 9.96
CHEMBL1908368 1 9.54
CHEMBL1910846 1 8.74
CHEMBL1910845 1 8.72
CHEMBL1910849 1 8.41
CHEMBL1910847 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE Ki = 0.075 nM 10.12
CHEMBL1910848 Ki = 0.11 nM 9.96
CHEMBL1908368 Ki = 0.29 nM 9.54
CHEMBL1910846 Ki = 1.8 nM 8.74
CHEMBL1910845 Ki = 1.9 nM 8.72
CHEMBL1910849 Ki = 3.9 nM 8.41
CHEMBL1910847 Ki = 6.4 nM 8.19