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Assay Detail

CHEMBL749239

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

Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) radioligand in human cloned Muscarinic acetylcholine receptor M4
1
Total Activities
1
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 M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
Bromidge SM, Brown F, Cassidy F, Clark MS, Dabbs S, Hadley MS, Hawkins J, Loudon JM, Naylor CB, Orlek BS, Riley GJ.
J Med Chem (1997) 40 : 4265 -4280
PubMed 9435896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.31 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135645 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135645 IC50 = 49.0 nM 7.31