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Assay Detail

CHEMBL2400142

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Functional
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
2
Total Activities
2
Compounds Tested
1
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 M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.
Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.
J Med Chem (2013) 56 : 5151 -5172
PubMed 23718562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.20 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594432 1 7.50
CHEMBL608112 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594432 EC50 = 31.62 nM 7.50
CHEMBL608112 EC50 = 128.82 nM 6.89