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Assay Detail

CHEMBL927398

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

Binding
Binding affinity to beta amyloid plaque in human Alzheimer's disease brain tissue
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Brain
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 N-methyl and S-methyl 11C-labeled 6-methylthio-2-(4'-N,N-dimethylamino)phenylimidazo[1,2-a]pyridines as radioligands for imaging beta-amyloid plaques in Alzheimer's disease.
Cai L, Liow JS, Zoghbi SS, Cuevas J, Baetas C, Hong J, Shetty HU, Seneca NM, Brown AK, Gladding R, Temme SS, Herman MM, Innis RB, Pike VW.
J Med Chem (2008) 51 : 148 -158
PubMed 18078311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.27 8.10
Kd 1 8.14 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93124 PITTSBURGH COMPOUND B UNLABELLED 2.0 1 8.14
CHEMBL252766 1 8.10
CHEMBL78012 1 8.05
CHEMBL252765 1 7.10
CHEMBL252969 1 6.69
CHEMBL254850 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93124 PITTSBURGH COMPOUND B UNLABELLED Kd = 7.23 nM 8.14
CHEMBL252766 Ki = 7.93 nM 8.10
CHEMBL78012 Ki = 8.95 nM 8.05
CHEMBL252765 Ki = 80.0 nM 7.10
CHEMBL252969 Ki = 205.0 nM 6.69
CHEMBL254850 Ki = 377.0 nM 6.42