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Assay Detail

CHEMBL744145

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

Binding
Inhibition of radioligand [3H]QNB binding to muscarinic acetylcholine receptor in the rat forebrain in the presence of zinc
29
Total Activities
29
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

Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
Davis L, Olsen GE, Klein JT, Kapples KJ, Huger FP, Smith CP, Petko WW, Cornfeldt M, Effland RC.
J Med Chem (1996) 39 : 582 -587
PubMed 8558530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.75 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL629 AMITRIPTYLINE 4.0 1 6.52
CHEMBL7634 OXOTREMORINE 1 5.57
CHEMBL29835 BESIPIRDINE 2.0 1 5.52
CHEMBL345535 1 5.09
CHEMBL157914 1 5.07
CHEMBL350903 1 4.90
CHEMBL347239 1 4.87
CHEMBL154030 1 4.77
CHEMBL350442 1 4.75
CHEMBL154576 1 4.67
CHEMBL155466 1 4.66
CHEMBL154501 1 4.62
CHEMBL346314 1 4.57
CHEMBL153830 1 4.48
CHEMBL156895 1 4.41
CHEMBL155252 1 4.37
CHEMBL154520 1 4.29
CHEMBL154921 1 4.28
CHEMBL154821 1 4.16
CHEMBL155012 1 4.12
CHEMBL154062 1 4.12
CHEMBL156601 1 -
CHEMBL154759 1 -
CHEMBL154109 1 -
CHEMBL346304 1 -
CHEMBL157442 1 -
CHEMBL155606 1 -
CHEMBL154961 1 -
CHEMBL347928 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL629 AMITRIPTYLINE IC50 = 300.0 nM 6.52
CHEMBL7634 OXOTREMORINE IC50 = 2700.0 nM 5.57
CHEMBL29835 BESIPIRDINE IC50 = 3000.0 nM 5.52
CHEMBL345535 IC50 = 8100.0 nM 5.09
CHEMBL157914 IC50 = 8600.0 nM 5.07
CHEMBL350903 IC50 = 12500.0 nM 4.90
CHEMBL347239 IC50 = 13500.0 nM 4.87
CHEMBL154030 IC50 = 17000.0 nM 4.77
CHEMBL350442 IC50 = 18000.0 nM 4.75
CHEMBL154576 IC50 = 21500.0 nM 4.67
CHEMBL155466 IC50 = 22000.0 nM 4.66
CHEMBL154501 IC50 = 24000.0 nM 4.62
CHEMBL346314 IC50 = 27000.0 nM 4.57
CHEMBL153830 IC50 = 33000.0 nM 4.48
CHEMBL156895 IC50 = 39000.0 nM 4.41
CHEMBL155252 IC50 = 43000.0 nM 4.37
CHEMBL154520 IC50 = 51000.0 nM 4.29
CHEMBL154921 IC50 = 52000.0 nM 4.28
CHEMBL154821 IC50 = 70000.0 nM 4.16
CHEMBL155012 IC50 = 76200.0 nM 4.12
CHEMBL154062 IC50 = 76400.0 nM 4.12
CHEMBL156601 IC50 = 721000.0 nM -
CHEMBL154759 IC50 = 184000.0 nM -
CHEMBL154109 IC50 = 295000.0 nM -
CHEMBL346304 IC50 > 1000000.0 nM -
CHEMBL157442 IC50 = 138000.0 nM -
CHEMBL155606 IC50 = 185000.0 nM -
CHEMBL154961 IC50 = 120000.0 nM -
CHEMBL347928 IC50 = 173000.0 nM -