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Assay Detail

CHEMBL2045349

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

Binding
Displacement of [18F]-amyvid from amyloid-beta aggregates in alzheimer's disease patient brain homogenates after 1 hr
13
Total Activities
13
Compounds Tested
1
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

Multidentate (18)F-polypegylated styrylpyridines as imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA).
Zha Z, Choi SR, Ploessl K, Lieberman BP, Qu W, Hefti F, Mintun M, Skovronsky D, Kung HF.
J Med Chem (2011) 54 : 8085 -8098
PubMed 22011144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.33 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2042122 FLUTEMETAMOL F 18 4.0 1 9.13
CHEMBL207456 PITTSBURGH COMPOUND B 2.0 1 9.06
CHEMBL78012 1 8.89
CHEMBL566752 FLORBETABEN F18 4.0 1 8.65
CHEMBL2042123 1 8.64
CHEMBL1774461 FLORBETAPIR F 18 4.0 1 8.54
CHEMBL381642 1 8.50
CHEMBL2042124 1 8.49
CHEMBL2042245 1 8.41
CHEMBL2042125 1 8.11
CHEMBL2042246 1 7.15
CHEMBL2042247 1 6.33
CHEMBL2042248 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2042122 FLUTEMETAMOL F 18 Ki = 0.74 nM 9.13
CHEMBL207456 PITTSBURGH COMPOUND B Ki = 0.87 nM 9.06
CHEMBL78012 Ki = 1.29 nM 8.89
CHEMBL566752 FLORBETABEN F18 Ki = 2.22 nM 8.65
CHEMBL2042123 Ki = 2.3 nM 8.64
CHEMBL1774461 FLORBETAPIR F 18 Ki = 2.87 nM 8.54
CHEMBL381642 Ki = 3.18 nM 8.50
CHEMBL2042124 Ki = 3.24 nM 8.49
CHEMBL2042245 Ki = 3.86 nM 8.41
CHEMBL2042125 Ki = 7.71 nM 8.11
CHEMBL2042246 Ki = 71.2 nM 7.15
CHEMBL2042247 Ki = 468.0 nM 6.33
CHEMBL2042248 Ki > 1000.0 nM -