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Assay Detail

CHEMBL929415

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

Functional
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diphenidol-related diamines as novel muscarinic M4 receptor antagonists.
Varoli L, Andreani A, Burnelli S, Granaiola M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Bedini A, Fazio N, Spampinato S.
Bioorg Med Chem Lett (2008) 18 : 2972 -2976
PubMed 18395442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.10 7.27
IC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59898 2 7.27
CHEMBL402207 2 7.17
CHEMBL403773 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59898 EC50 = 54.0 nM 7.27
CHEMBL402207 EC50 = 67.0 nM 7.17
CHEMBL403773 EC50 = 138.0 nM 6.86
CHEMBL59898 IC50 > 1000.0 nM -
CHEMBL402207 IC50 > 1000.0 nM -