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Assay Detail

CHEMBL748850

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

Binding
Inhibition of [3H](R)-QNB binding to muscarinic receptor in rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Brain membranes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis, biochemical activity and behavioral effects of a series of 1,4,5,6-tetrahydropyrimidines as novel ligands for M1 receptors
Messer WS, Dunbar PG, Rho T, Periyasamy S, Ngur D, Ellerbrock BR, Bohnett M, Ryan K, Durant GJ, Hoss W
Bioorg Med Chem Lett (1992) 2 : 781 -786
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.46 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20835 ACECLIDINE 3.0 1 6.29
CHEMBL7303 ARECOLINE -1.0 1 6.00
CHEMBL541398 1 5.66
CHEMBL544556 1 5.62
CHEMBL536249 1 5.58
CHEMBL542065 1 5.48
CHEMBL537928 1 5.48
CHEMBL14 CARBACHOL 4.0 1 5.26
CHEMBL550 PILOCARPINE 4.0 1 5.12
CHEMBL538467 1 5.04
CHEMBL536704 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20835 ACECLIDINE IC50 = 510.0 nM 6.29
CHEMBL7303 ARECOLINE IC50 = 1000.0 nM 6.00
CHEMBL541398 IC50 = 2200.0 nM 5.66
CHEMBL544556 IC50 = 2400.0 nM 5.62
CHEMBL536249 IC50 = 2600.0 nM 5.58
CHEMBL542065 IC50 = 3300.0 nM 5.48
CHEMBL537928 IC50 = 3300.0 nM 5.48
CHEMBL14 CARBACHOL IC50 = 5500.0 nM 5.26
CHEMBL550 PILOCARPINE IC50 = 7600.0 nM 5.12
CHEMBL538467 IC50 = 9200.0 nM 5.04
CHEMBL536704 IC50 = 32000.0 nM 4.50