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Assay Detail

CHEMBL748430

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

Binding
In vitro inhibition of [3H]quinuclidinyl benzilate (QNB) binding to muscarinic receptors of rat cerebral cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

A novel and selective class of azabicyclic muscarinic agonists incorporating an N-methoxy imidoyl halide or nitrile functionality
Bromidge SM, Brown F, Cassidy F, Clark MS, Dabbs S, Hawkins J, Loudon JM, Orlek BS, Riley GJ
Bioorg Med Chem Lett (1992) 2 : 791 -796
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.62 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135645 1 6.66
CHEMBL336590 1 6.33
CHEMBL135604 1 5.96
CHEMBL344892 1 5.71
CHEMBL341766 1 5.70
CHEMBL350757 1 5.64
CHEMBL335324 1 5.64
CHEMBL167982 1 5.62
CHEMBL137385 1 5.52
CHEMBL336162 1 5.52
CHEMBL135260 1 5.52
CHEMBL341379 1 5.51
CHEMBL334674 1 5.09
CHEMBL336727 1 5.07
CHEMBL135836 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135645 IC50 = 220.0 nM 6.66
CHEMBL336590 IC50 = 470.0 nM 6.33
CHEMBL135604 IC50 = 1100.0 nM 5.96
CHEMBL344892 IC50 = 1950.0 nM 5.71
CHEMBL341766 IC50 = 2000.0 nM 5.70
CHEMBL350757 IC50 = 2300.0 nM 5.64
CHEMBL335324 IC50 = 2300.0 nM 5.64
CHEMBL167982 IC50 = 2400.0 nM 5.62
CHEMBL137385 IC50 = 3000.0 nM 5.52
CHEMBL336162 IC50 = 3000.0 nM 5.52
CHEMBL135260 IC50 = 3000.0 nM 5.52
CHEMBL341379 IC50 = 3100.0 nM 5.51
CHEMBL334674 IC50 = 8100.0 nM 5.09
CHEMBL336727 IC50 = 8500.0 nM 5.07
CHEMBL135836 IC50 = 15500.0 nM 4.81