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Assay Detail

CHEMBL714426

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

Binding
Inhibition of [3H]-(R)-QNB binding to muscarinic receptors of rat brain membranes.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
Dunbar PG, Durant GJ, Fang Z, Abuh YF, el-Assadi AA, Ngur DO, Periyasamy S, Hoss WP, Messer WS.
J Med Chem (1993) 36 : 842 -847
PubMed 8464038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.95 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279356 1 6.46
CHEMBL422742 1 6.31
CHEMBL20835 ACECLIDINE 3.0 1 6.29
CHEMBL169625 1 6.28
CHEMBL169150 1 6.26
CHEMBL168472 1 6.25
CHEMBL12378 1 6.16
CHEMBL416736 1 6.00
CHEMBL7303 ARECOLINE -1.0 1 6.00
CHEMBL169019 1 5.64
CHEMBL168218 1 5.64
CHEMBL277014 1 5.57
CHEMBL14 CARBACHOL 4.0 1 5.26
CHEMBL550 PILOCARPINE 4.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279356 IC50 = 350.0 nM 6.46
CHEMBL422742 IC50 = 490.0 nM 6.31
CHEMBL20835 ACECLIDINE IC50 = 510.0 nM 6.29
CHEMBL169625 IC50 = 530.0 nM 6.28
CHEMBL169150 IC50 = 550.0 nM 6.26
CHEMBL168472 IC50 = 560.0 nM 6.25
CHEMBL12378 IC50 = 690.0 nM 6.16
CHEMBL416736 IC50 = 1000.0 nM 6.00
CHEMBL7303 ARECOLINE IC50 = 1000.0 nM 6.00
CHEMBL169019 IC50 = 2300.0 nM 5.64
CHEMBL168218 IC50 = 2300.0 nM 5.64
CHEMBL277014 IC50 = 2700.0 nM 5.57
CHEMBL14 CARBACHOL IC50 = 5500.0 nM 5.26
CHEMBL550 PILOCARPINE IC50 = 7600.0 nM 5.12