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Assay Detail

CHEMBL748852

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

Binding
Displacement of [3H]-Pz (pirenzepine) from the muscarinic receptor M1 of the rat hippocampus
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP
Sauerberg P, Olesen PH, Suzdak PD, Sheardown MJ, Mitch CH, Sawyer BD, Shannon HE
Bioorg Med Chem Lett (1992) 2 : 809 -814
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.64 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101054 1 8.30
CHEMBL21536 XANOMELINE 4.0 1 8.15
CHEMBL74786 1 6.56
CHEMBL75907 1 6.46
CHEMBL355465 1 6.43
CHEMBL353779 1 6.25
CHEMBL168581 1 6.18
CHEMBL166115 1 6.15
CHEMBL74300 1 6.02
CHEMBL7303 ARECOLINE -1.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101054 IC50 = 5.0 nM 8.30
CHEMBL21536 XANOMELINE IC50 = 7.0 nM 8.15
CHEMBL74786 IC50 = 277.0 nM 6.56
CHEMBL75907 IC50 = 345.0 nM 6.46
CHEMBL355465 IC50 = 369.0 nM 6.43
CHEMBL353779 IC50 = 565.0 nM 6.25
CHEMBL168581 IC50 = 663.0 nM 6.18
CHEMBL166115 IC50 = 715.0 nM 6.15
CHEMBL74300 IC50 = 955.0 nM 6.02
CHEMBL7303 ARECOLINE IC50 = 1300.0 nM 5.89