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Assay Detail

CHEMBL1067396

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

Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
17
Total Activities
17
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

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.
Piergentili A, Quaglia W, Del Bello F, Giannella M, Pigini M, Barocelli E, Bertoni S, Matucci R, Nesi M, Bruni B, Di Vaira M.
Bioorg Med Chem (2009) 17 : 8174 -8185
PubMed 19896386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 4.63 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74300 1 5.62
CHEMBL390842 1 5.12
CHEMBL593620 1 4.98
CHEMBL595265 1 4.96
CHEMBL593685 1 4.79
CHEMBL594801 1 4.67
CHEMBL594803 1 4.49
CHEMBL404557 1 4.45
CHEMBL593861 1 4.39
CHEMBL14 CARBACHOL 4.0 1 4.36
CHEMBL593443 1 4.35
CHEMBL595022 1 4.33
CHEMBL594376 1 4.18
CHEMBL594802 1 4.11
CHEMBL593871 1 -
CHEMBL608985 1 -
CHEMBL593864 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74300 Ki = 2398.83 nM 5.62
CHEMBL390842 Ki = 7585.78 nM 5.12
CHEMBL593620 Ki = 10471.29 nM 4.98
CHEMBL595265 Ki = 10964.78 nM 4.96
CHEMBL593685 Ki = 16218.1 nM 4.79
CHEMBL594801 Ki = 21379.62 nM 4.67
CHEMBL594803 Ki = 32359.37 nM 4.49
CHEMBL404557 Ki = 35481.34 nM 4.45
CHEMBL593861 Ki = 40738.03 nM 4.39
CHEMBL14 CARBACHOL Ki = 43651.58 nM 4.36
CHEMBL593443 Ki = 44668.36 nM 4.35
CHEMBL595022 Ki = 46773.51 nM 4.33
CHEMBL594376 Ki = 66069.34 nM 4.18
CHEMBL594802 Ki = 77624.71 nM 4.11
CHEMBL593871 Ki > 100000.0 nM -
CHEMBL608985 Ki > 100000.0 nM -
CHEMBL593864 Ki > 100000.0 nM -