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Assay Detail

CHEMBL749008

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

Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A rationale for the design and synthesis of m1 selective muscarinic agonists.
Tecle H, Mirzadegan T, Moos W, Moreland D, Pavia M, Schwarz R, Davis R
Bioorg Med Chem Lett (1992) 2 : 821 -826
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.32 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314737 OXADIAZOLE 1 7.70
CHEMBL315676 1 5.98
CHEMBL354259 1 5.79
CHEMBL354738 1 5.77
CHEMBL83074 1 5.66
CHEMBL313918 1 5.55
CHEMBL166423 1 5.50
CHEMBL14 CARBACHOL 4.0 1 5.46
CHEMBL167438 1 5.40
CHEMBL166593 1 5.35
CHEMBL168561 1 5.29
CHEMBL166537 1 5.28
CHEMBL85678 1 5.10
CHEMBL168545 1 5.07
CHEMBL168639 1 5.01
CHEMBL74300 1 4.89
CHEMBL352832 1 4.81
CHEMBL169011 1 4.80
CHEMBL84893 1 4.59
CHEMBL312823 1 4.52
CHEMBL168991 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314737 OXADIAZOLE IC50 = 20.0 nM 7.70
CHEMBL315676 IC50 = 1040.0 nM 5.98
CHEMBL354259 IC50 = 1630.0 nM 5.79
CHEMBL354738 IC50 = 1700.0 nM 5.77
CHEMBL83074 IC50 = 2180.0 nM 5.66
CHEMBL313918 IC50 = 2840.0 nM 5.55
CHEMBL166423 IC50 = 3150.0 nM 5.50
CHEMBL14 CARBACHOL IC50 = 3460.0 nM 5.46
CHEMBL167438 IC50 = 3980.0 nM 5.40
CHEMBL166593 IC50 = 4460.0 nM 5.35
CHEMBL168561 IC50 = 5080.0 nM 5.29
CHEMBL166537 IC50 = 5280.0 nM 5.28
CHEMBL85678 IC50 = 7890.0 nM 5.10
CHEMBL168545 IC50 = 8600.0 nM 5.07
CHEMBL168639 IC50 = 9650.0 nM 5.01
CHEMBL74300 IC50 = 12930.0 nM 4.89
CHEMBL352832 IC50 = 15590.0 nM 4.81
CHEMBL169011 IC50 = 15900.0 nM 4.80
CHEMBL84893 IC50 = 25800.0 nM 4.59
CHEMBL312823 IC50 = 30200.0 nM 4.52
CHEMBL168991 IC50 = 59300.0 nM 4.23