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Assay Detail

CHEMBL749006

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

Binding
Binding affinity of [3H]QNB to CHO cells expressing human Muscarinic acetylcholine receptor M2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.
Tecle H, Barrett SD, Lauffer DJ, Augelli-Szafran C, Brann MR, Callahan MJ, Caprathe BW, Davis RE, Doyle PD, Eubanks D, Lipiniski W, Mirzadegan T, Moos WH, Moreland DW, Nelson CB, Pavia MR, Raby C, Schwarz RD, Spencer CJ, Thomas AJ, Jaen JC.
J Med Chem (1998) 41 : 2524 -2536
PubMed 9651157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.87 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312823 1 6.29
CHEMBL86903 1 5.72
CHEMBL83074 1 5.66
CHEMBL85264 1 5.40
CHEMBL315676 1 5.22
CHEMBL87622 1 5.22
CHEMBL84726 1 5.10
CHEMBL313918 1 5.09
CHEMBL85936 1 5.05
CHEMBL87485 1 4.97
CHEMBL85645 1 4.82
CHEMBL85678 1 4.78
CHEMBL81895 1 4.69
CHEMBL313749 1 4.68
CHEMBL420781 1 4.61
CHEMBL84893 1 4.59
CHEMBL314420 1 4.57
CHEMBL86288 1 4.41
CHEMBL86197 1 4.33
CHEMBL85460 1 4.32
CHEMBL81878 1 4.28
CHEMBL86150 1 4.16
CHEMBL84919 1 4.07
CHEMBL14 CARBACHOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312823 IC50 = 519.0 nM 6.29
CHEMBL86903 IC50 = 1900.0 nM 5.72
CHEMBL83074 IC50 = 2180.0 nM 5.66
CHEMBL85264 IC50 = 4010.0 nM 5.40
CHEMBL315676 IC50 = 6030.0 nM 5.22
CHEMBL87622 IC50 = 6010.0 nM 5.22
CHEMBL84726 IC50 = 7930.0 nM 5.10
CHEMBL313918 IC50 = 8070.0 nM 5.09
CHEMBL85936 IC50 = 8900.0 nM 5.05
CHEMBL87485 IC50 = 10800.0 nM 4.97
CHEMBL85645 IC50 = 15200.0 nM 4.82
CHEMBL85678 IC50 = 16800.0 nM 4.78
CHEMBL81895 IC50 = 20600.0 nM 4.69
CHEMBL313749 IC50 = 20800.0 nM 4.68
CHEMBL420781 IC50 = 24700.0 nM 4.61
CHEMBL84893 IC50 = 25800.0 nM 4.59
CHEMBL314420 IC50 = 27200.0 nM 4.57
CHEMBL86288 IC50 = 38600.0 nM 4.41
CHEMBL86197 IC50 = 46600.0 nM 4.33
CHEMBL85460 IC50 = 47900.0 nM 4.32
CHEMBL81878 IC50 = 52000.0 nM 4.28
CHEMBL86150 IC50 = 69300.0 nM 4.16
CHEMBL84919 IC50 = 84400.0 nM 4.07
CHEMBL14 CARBACHOL IC50 = 119000.0 nM -