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Assay Detail

CHEMBL748168

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

Binding
Binding affinity against muscarinic receptor using radioligand [3H]quinuclidinyl benzilate (QNB) binding assay in membrane preparations of rat neocortex.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

()-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oximes: Potent muscarinic agonists
Tecle H, Lauffer D, Davis R, Mirzadegan T, Moreland D, Schwan R, Thomas A, Raby C, Eubanks D, Brann M, Jaen J
Bioorg Med Chem Lett (1995) 5 : 637 -642
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.14 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL156050 1 7.82
CHEMBL351561 1 7.68
CHEMBL160582 1 7.36
CHEMBL348412 1 7.19
CHEMBL405426 1 7.09
CHEMBL156445 1 7.06
CHEMBL346580 1 6.77
CHEMBL345415 1 6.74
CHEMBL160939 1 6.66
CHEMBL345205 1 6.42
CHEMBL434469 1 6.42
CHEMBL160541 1 6.36
CHEMBL348079 1 6.22
CHEMBL346123 1 6.17
CHEMBL86903 1 6.09
CHEMBL160858 1 6.01
CHEMBL158180 1 5.97
CHEMBL160928 1 5.91
CHEMBL157198 1 5.85
CHEMBL160554 1 5.82
CHEMBL84726 1 5.80
CHEMBL157197 1 5.70
CHEMBL87622 1 5.69
CHEMBL156749 1 5.62
CHEMBL156925 1 5.56
CHEMBL345250 1 5.46
CHEMBL434072 1 5.37
CHEMBL160288 1 5.25
CHEMBL159208 1 5.07
CHEMBL160509 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL156050 IC50 = 15.0 nM 7.82
CHEMBL351561 IC50 = 21.0 nM 7.68
CHEMBL160582 IC50 = 44.0 nM 7.36
CHEMBL348412 IC50 = 64.0 nM 7.19
CHEMBL405426 IC50 = 81.0 nM 7.09
CHEMBL156445 IC50 = 88.0 nM 7.06
CHEMBL346580 IC50 = 171.0 nM 6.77
CHEMBL345415 IC50 = 181.0 nM 6.74
CHEMBL160939 IC50 = 219.0 nM 6.66
CHEMBL345205 IC50 = 383.0 nM 6.42
CHEMBL434469 IC50 = 384.0 nM 6.42
CHEMBL160541 IC50 = 439.0 nM 6.36
CHEMBL348079 IC50 = 608.0 nM 6.22
CHEMBL346123 IC50 = 681.0 nM 6.17
CHEMBL86903 IC50 = 807.0 nM 6.09
CHEMBL160858 IC50 = 968.0 nM 6.01
CHEMBL158180 IC50 = 1073.0 nM 5.97
CHEMBL160928 IC50 = 1245.0 nM 5.91
CHEMBL157198 IC50 = 1413.0 nM 5.85
CHEMBL160554 IC50 = 1514.0 nM 5.82
CHEMBL84726 IC50 = 1587.0 nM 5.80
CHEMBL157197 IC50 = 1992.0 nM 5.70
CHEMBL87622 IC50 = 2063.0 nM 5.69
CHEMBL156749 IC50 = 2380.0 nM 5.62
CHEMBL156925 IC50 = 2742.0 nM 5.56
CHEMBL345250 IC50 = 3510.0 nM 5.46
CHEMBL434072 IC50 = 4234.0 nM 5.37
CHEMBL160288 IC50 = 5593.0 nM 5.25
CHEMBL159208 IC50 = 8547.0 nM 5.07
CHEMBL160509 IC50 = 19308.0 nM 4.71
CHEMBL14 CARBACHOL IC50 = 33000.0 nM 4.48