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Assay Detail

CHEMBL3878788

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Binding
Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by microbeta liquid scintillation counting method
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease.
Kim T, Yang HY, Park BG, Jung SY, Park JH, Park KD, Min SJ, Tae J, Yang H, Cho S, Cho SJ, Song H, Mook-Jung I, Lee J, Pae AN.
Eur J Med Chem (2017) 125 : 1172 -1192
PubMed 27855359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.01 8.88
Ki 2 7.85 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481537 PK-11195 2 8.88
CHEMBL3948914 2 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481537 PK-11195 IC50 = 1.32 nM 8.88
CHEMBL481537 PK-11195 Ki = 8.85 nM 8.05
CHEMBL3948914 Ki = 22.8 nM 7.64
CHEMBL3948914 IC50 = 74.3 nM 7.13