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Assay Detail

CHEMBL2409975

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

Binding
Displacement of [125I]IMPY from amyloid beta (1 to 42) (unknown origin) after 3 hrs by gamma counting
8
Total Activities
8
Compounds Tested
1
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

Structure-Activity Relationships and in Vivo Evaluation of Quinoxaline Derivatives for PET Imaging of β-Amyloid Plaques.
Yoshimura M, Ono M, Matsumura K, Watanabe H, Kimura H, Cui M, Nakamoto Y, Togashi K, Okamoto Y, Ihara M, Takahashi R, Saji H.
ACS Med Chem Lett (2013) 4 : 596 -600
PubMed 24900717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.31 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2407616 1 9.05
CHEMBL78012 1 8.14
CHEMBL1908919 FLORBETAPIR 4.0 1 7.89
CHEMBL2407615 1 7.80
CHEMBL2407623 1 6.96
CHEMBL2407624 1 6.62
CHEMBL2407625 1 6.12
CHEMBL2407626 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2407616 Ki = 0.895 nM 9.05
CHEMBL78012 Ki = 7.21 nM 8.14
CHEMBL1908919 FLORBETAPIR Ki = 12.8 nM 7.89
CHEMBL2407615 Ki = 15.7 nM 7.80
CHEMBL2407623 Ki = 111.0 nM 6.96
CHEMBL2407624 Ki = 242.0 nM 6.62
CHEMBL2407625 Ki = 758.0 nM 6.12
CHEMBL2407626 Ki = 1180.0 nM 5.93