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Assay Detail

CHEMBL748967

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

Binding
Binding affinity (high) of [3H](R)-QNB binding to Muscarinic acetylcholine receptor M1 expressed in A9 L cell line in the absence of 300 uM GTP-gamma-S
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL3733)
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
Ki 7 7.12 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542064 1 7.85
CHEMBL277014 1 7.68
CHEMBL542559 1 7.51
CHEMBL542065 1 7.38
CHEMBL21284 1 6.86
CHEMBL538467 1 6.45
CHEMBL14 CARBACHOL 4.0 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542064 Ki = 14.0 nM 7.85
CHEMBL277014 Ki = 21.1 nM 7.68
CHEMBL542559 Ki = 30.9 nM 7.51
CHEMBL542065 Ki = 41.7 nM 7.38
CHEMBL21284 Ki = 138.0 nM 6.86
CHEMBL538467 Ki = 359.0 nM 6.45
CHEMBL14 CARBACHOL Ki = 739.0 nM 6.13