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Assay Detail

CHEMBL747408

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

Binding
In vitro inhibition of [3H]OXO-M binding to Muscarinic receptor from rat cortical homogenates
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
Wadsworth HJ, Jenkins SM, Orlek BS, Cassidy F, Clark MS, Brown F, Riley GJ, Graves D, Hawkins J, Naylor CB.
J Med Chem (1992) 35 : 1280 -1290
PubMed 1560440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.36 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279356 1 7.85
CHEMBL7634 OXOTREMORINE 1 7.77
CHEMBL23721 1 7.32
CHEMBL23335 1 7.12
CHEMBL7303 ARECOLINE -1.0 1 6.94
CHEMBL276975 1 6.85
CHEMBL434772 1 6.77
CHEMBL23563 1 6.62
CHEMBL9967 PIRENZEPINE 2.0 1 6.49
CHEMBL429230 1 6.03
CHEMBL22926 1 5.47
CHEMBL278352 1 5.34
CHEMBL23222 1 5.30
CHEMBL23962 1 5.19
CHEMBL22925 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279356 IC50 = 14.0 nM 7.85
CHEMBL7634 OXOTREMORINE IC50 = 17.0 nM 7.77
CHEMBL23721 IC50 = 48.0 nM 7.32
CHEMBL23335 IC50 = 75.0 nM 7.12
CHEMBL7303 ARECOLINE IC50 = 115.0 nM 6.94
CHEMBL276975 IC50 = 140.0 nM 6.85
CHEMBL434772 IC50 = 170.0 nM 6.77
CHEMBL23563 IC50 = 240.0 nM 6.62
CHEMBL9967 PIRENZEPINE IC50 = 322.0 nM 6.49
CHEMBL429230 IC50 = 930.0 nM 6.03
CHEMBL22926 IC50 = 3400.0 nM 5.47
CHEMBL278352 IC50 = 4600.0 nM 5.34
CHEMBL23222 IC50 = 5000.0 nM 5.30
CHEMBL23962 IC50 = 6500.0 nM 5.19
CHEMBL22925 IC50 = 40000.0 nM 4.40