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Assay Detail

CHEMBL747588

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

Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor of rat heart membranes.
8
Total Activities
8
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

6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.
Daly JW, Gupta TH, Padgett WL, Pei XF.
J Med Chem (2000) 43 : 2514 -2522
PubMed 10891110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.75 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7634 OXOTREMORINE 1 6.48
CHEMBL64000 1 6.40
CHEMBL84113 1 5.85
CHEMBL85190 1 5.85
CHEMBL7303 ARECOLINE -1.0 1 5.72
CHEMBL14 CARBACHOL 4.0 1 5.54
CHEMBL12587 MUSCARINE 1 5.36
CHEMBL294273 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7634 OXOTREMORINE Ki = 330.0 nM 6.48
CHEMBL64000 Ki = 400.0 nM 6.40
CHEMBL84113 Ki = 1400.0 nM 5.85
CHEMBL85190 Ki = 1400.0 nM 5.85
CHEMBL7303 ARECOLINE Ki = 1900.0 nM 5.72
CHEMBL14 CARBACHOL Ki = 2900.0 nM 5.54
CHEMBL12587 MUSCARINE Ki = 4400.0 nM 5.36
CHEMBL294273 Ki = 17000.0 nM 4.77