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Assay Detail

CHEMBL748171

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

Binding
Compound was evaluated for inhibition of [3H]cis-methyldioxolane binding to label agonist sites (RCMD) in rat neocortex
25
Total Activities
25
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

A rationale for the design and synthesis of m1 selective muscarinic agonists.
Tecle H, Mirzadegan T, Moos W, Moreland D, Pavia M, Schwarz R, Davis R
Bioorg Med Chem Lett (1992) 2 : 821 -826
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.65 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314737 OXADIAZOLE 1 9.52
CHEMBL315676 1 8.46
CHEMBL168545 1 8.44
CHEMBL354738 1 8.40
CHEMBL14 CARBACHOL 4.0 1 8.17
CHEMBL83074 1 8.10
CHEMBL352908 1 7.90
CHEMBL85678 1 7.74
CHEMBL313918 1 7.66
CHEMBL74300 1 7.60
CHEMBL169011 1 7.50
CHEMBL166537 1 7.46
CHEMBL312823 1 7.46
CHEMBL168561 1 7.41
CHEMBL168639 1 7.36
CHEMBL166423 1 7.34
CHEMBL84893 1 7.34
CHEMBL166782 1 7.32
CHEMBL168991 1 7.26
CHEMBL352832 1 7.08
CHEMBL354259 1 7.06
CHEMBL166593 1 7.04
CHEMBL167015 1 6.96
CHEMBL167438 1 6.92
CHEMBL170903 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314737 OXADIAZOLE IC50 = 0.3 nM 9.52
CHEMBL315676 IC50 = 3.5 nM 8.46
CHEMBL168545 IC50 = 3.6 nM 8.44
CHEMBL354738 IC50 = 4.0 nM 8.40
CHEMBL14 CARBACHOL IC50 = 6.7 nM 8.17
CHEMBL83074 IC50 = 8.0 nM 8.10
CHEMBL352908 IC50 = 12.5 nM 7.90
CHEMBL85678 IC50 = 18.2 nM 7.74
CHEMBL313918 IC50 = 22.0 nM 7.66
CHEMBL74300 IC50 = 25.0 nM 7.60
CHEMBL169011 IC50 = 32.0 nM 7.50
CHEMBL166537 IC50 = 35.0 nM 7.46
CHEMBL312823 IC50 = 35.0 nM 7.46
CHEMBL168561 IC50 = 39.0 nM 7.41
CHEMBL168639 IC50 = 44.0 nM 7.36
CHEMBL166423 IC50 = 46.0 nM 7.34
CHEMBL84893 IC50 = 46.0 nM 7.34
CHEMBL166782 IC50 = 48.0 nM 7.32
CHEMBL168991 IC50 = 55.0 nM 7.26
CHEMBL352832 IC50 = 83.0 nM 7.08
CHEMBL354259 IC50 = 88.0 nM 7.06
CHEMBL166593 IC50 = 91.0 nM 7.04
CHEMBL167015 IC50 = 111.0 nM 6.96
CHEMBL167438 IC50 = 120.0 nM 6.92
CHEMBL170903 IC50 > 100.0 nM -