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Assay Detail

CHEMBL929996

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

Binding
Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells by wash-resistant binding method
20
Total Activities
20
Compounds Tested
2
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 M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.
Kane BE, Grant MK, El-Fakahany EE, Ferguson DM.
Bioorg Med Chem (2008) 16 : 1376 -1392
PubMed 17977730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.86 5.67
Activity 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291351 1 5.67
CHEMBL406802 1 5.40
CHEMBL21536 XANOMELINE 4.0 1 5.31
CHEMBL327754 1 5.07
CHEMBL99768 1 5.04
CHEMBL270031 1 4.83
CHEMBL408822 1 4.54
CHEMBL255791 1 4.35
CHEMBL272468 1 4.28
CHEMBL101054 1 4.11
CHEMBL405125 1 -
CHEMBL272359 1 -
CHEMBL406570 1 -
CHEMBL255793 1 -
CHEMBL403829 1 -
CHEMBL401694 1 -
CHEMBL257683 1 -
CHEMBL271774 1 -
CHEMBL99476 1 -
CHEMBL303922 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291351 IC50 = 2137.96 nM 5.67
CHEMBL406802 IC50 = 3981.07 nM 5.40
CHEMBL21536 XANOMELINE IC50 = 4897.79 nM 5.31
CHEMBL327754 IC50 = 8511.38 nM 5.07
CHEMBL99768 IC50 = 9120.11 nM 5.04
CHEMBL270031 IC50 = 14791.08 nM 4.83
CHEMBL408822 IC50 = 28840.32 nM 4.54
CHEMBL255791 IC50 = 44668.36 nM 4.35
CHEMBL272468 IC50 = 52480.75 nM 4.28
CHEMBL101054 IC50 = 77624.71 nM 4.11
CHEMBL405125 Activity - -
CHEMBL272359 Activity - -
CHEMBL406570 IC50 = 109647.82 nM -
CHEMBL255793 Activity - -
CHEMBL403829 Activity - -
CHEMBL401694 Activity - -
CHEMBL257683 Activity - -
CHEMBL271774 Activity - -
CHEMBL99476 Activity - -
CHEMBL303922 Activity - -