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Assay Detail

CHEMBL753022

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

Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type A9L
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M3 (CHEMBL5105)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
Messer WS, Abuh YF, Liu Y, Periyasamy S, Ngur DO, Edgar MA, El-Assadi AA, Sbeih S, Dunbar PG, Roknich S, Rho T, Fang Z, Ojo B, Zhang H, Huzl JJ, Nagy PI.
J Med Chem (1997) 40 : 1230 -1246
PubMed 9111297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 5.01 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277014 1 5.96
CHEMBL12378 1 5.55
CHEMBL281411 1 5.24
CHEMBL416736 1 5.00
CHEMBL14 CARBACHOL 4.0 1 5.00
CHEMBL20835 ACECLIDINE 3.0 1 5.00
CHEMBL22089 1 4.96
CHEMBL21536 XANOMELINE 4.0 1 4.96
CHEMBL7303 ARECOLINE -1.0 1 4.92
CHEMBL557795 1 4.92
CHEMBL553602 1 4.85
CHEMBL541398 1 4.77
CHEMBL542065 1 4.75
CHEMBL538467 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277014 EC50 = 1100.0 nM 5.96
CHEMBL12378 EC50 = 2800.0 nM 5.55
CHEMBL281411 EC50 = 5800.0 nM 5.24
CHEMBL416736 EC50 = 10000.0 nM 5.00
CHEMBL14 CARBACHOL EC50 = 9900.0 nM 5.00
CHEMBL20835 ACECLIDINE EC50 = 10000.0 nM 5.00
CHEMBL22089 EC50 = 11000.0 nM 4.96
CHEMBL21536 XANOMELINE EC50 = 11000.0 nM 4.96
CHEMBL7303 ARECOLINE EC50 = 12000.0 nM 4.92
CHEMBL557795 EC50 = 12000.0 nM 4.92
CHEMBL553602 EC50 = 14000.0 nM 4.85
CHEMBL541398 EC50 = 17000.0 nM 4.77
CHEMBL542065 EC50 = 18000.0 nM 4.75
CHEMBL538467 EC50 = 50000.0 nM 4.30