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Assay Detail

CHEMBL1675411

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

Binding
Displacement of [3H]PiB from human amyloid beta (1-42) at 100 nM after 180 mins by liquid scintillation counter
14
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amyloid-beta precursor protein (CHEMBL2487)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 11C-labeled imidazo[2,1-b]benzothiazoles (IBTs) as PET tracers for imaging β-amyloid plaques in Alzheimer's disease.
Yousefi BH, Manook A, Drzezga A, von Reutern B, Schwaiger M, Wester HJ, Henriksen G.
J Med Chem (2011) 54 : 949 -956
PubMed 21275403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 12 - -
Ki 2 8.07 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1671878 2 8.24
CHEMBL93124 PITTSBURGH COMPOUND B UNLABELLED 2.0 2 7.89
CHEMBL1672888 1 -
CHEMBL1672889 1 -
CHEMBL1672890 1 -
CHEMBL1672891 1 -
CHEMBL1672892 1 -
CHEMBL1672893 1 -
CHEMBL1672894 1 -
CHEMBL1672895 1 -
CHEMBL1672896 1 -
CHEMBL1672897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1671878 Ki = 5.8 nM 8.24
CHEMBL93124 PITTSBURGH COMPOUND B UNLABELLED Ki = 13.0 nM 7.89
CHEMBL93124 PITTSBURGH COMPOUND B UNLABELLED Inhibition = 83.0 % -
CHEMBL1672888 Inhibition = 82.0 % -
CHEMBL1672889 Inhibition = 91.0 % -
CHEMBL1672890 Inhibition = 91.0 % -
CHEMBL1672891 Inhibition = 64.0 % -
CHEMBL1672892 Inhibition = 91.0 % -
CHEMBL1672893 Inhibition = 91.0 % -
CHEMBL1672894 Inhibition = 86.0 % -
CHEMBL1672895 Inhibition = 74.0 % -
CHEMBL1671878 Inhibition = 97.0 % -
CHEMBL1672896 Inhibition = 48.0 % -
CHEMBL1672897 Inhibition = 73.0 % -