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Assay Detail

CHEMBL748851

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

Binding
Compound was evaluated for the displacement of the muscarinic QNB in a genetically transformed rat cell line (m1c2) transfected with cloned m1 receptors (m1-QNBm1c2)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine
Hobbs SH, Johnson SJ, Kesten SR, Pavia MR, Davis RE, Schwarz RD, Coughenour LL, Myers SL, Dudley DT, Moss WH
Bioorg Med Chem Lett (1991) 1 : 147 -150
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.19 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7634 OXOTREMORINE 1 6.44
CHEMBL550 PILOCARPINE 4.0 1 5.35
CHEMBL7303 ARECOLINE -1.0 1 4.92
CHEMBL37132 1 4.90
CHEMBL14 CARBACHOL 4.0 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7634 OXOTREMORINE IC50 = 360.0 nM 6.44
CHEMBL550 PILOCARPINE IC50 = 4430.0 nM 5.35
CHEMBL7303 ARECOLINE IC50 = 11920.0 nM 4.92
CHEMBL37132 IC50 = 12690.0 nM 4.90
CHEMBL14 CARBACHOL IC50 = 44370.0 nM 4.35