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Assay Detail

CHEMBL744146

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

Binding
Muscarinic acetylcholine receptor binding (rat cortical membranes) was determined by displacement of [3H]quinuclidinyl benzylate [3H]QNB)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.
Cosford ND, Bleicher L, Herbaut A, McCallum JS, Vernier JM, Dawson H, Whitten JP, Adams P, Chavez-Noriega L, Correa LD, Crona JH, Mahaffy LS, Menzaghi F, Rao TS, Reid R, Sacaan AI, Santori E, Stauderman KA, Whelan K, Lloyd GK, McDonald IA.
J Med Chem (1996) 39 : 3235 -3237
PubMed 8765504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.29 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61772 1 5.80
CHEMBL1788226 1 5.35
CHEMBL111526 1 5.24
CHEMBL111659 ALTINICLINE 2.0 1 5.05
CHEMBL111580 1 5.00
CHEMBL3 NICOTINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61772 IC50 = 1600.0 nM 5.80
CHEMBL1788226 IC50 = 4500.0 nM 5.35
CHEMBL111526 IC50 = 5800.0 nM 5.24
CHEMBL111659 ALTINICLINE IC50 = 8900.0 nM 5.05
CHEMBL111580 IC50 = 10100.0 nM 5.00
CHEMBL3 NICOTINE IC50 = 360000.0 nM -