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Assay Detail

CHEMBL4138528

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

Binding
Displacement of [3H]PK11195 from human wild type TSPO expressed in HEK293T cell membranes after 90 mins by scintillation counting method
10
Total Activities
10
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

Translocator protein (CHEMBL5742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination.
Sokias R, Werry EL, Chua SW, Reekie TA, Munoz L, Wong ECN, Ittner LM, Kassiou M.
Medchemcomm (2017) 8 : 202 -210
PubMed 30108706 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.54 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513922 EMAPUNIL 2.0 1 8.19
CHEMBL480041 1 7.71
CHEMBL4165898 1 7.59
CHEMBL481537 PK-11195 1 7.54
CHEMBL4173816 1 7.54
CHEMBL4173118 1 7.52
CHEMBL4164932 1 7.50
CHEMBL4177167 1 7.50
CHEMBL4169328 1 7.26
CHEMBL4161842 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513922 EMAPUNIL Ki = 6.4 nM 8.19
CHEMBL480041 Ki = 19.5 nM 7.71
CHEMBL4165898 Ki = 25.4 nM 7.59
CHEMBL481537 PK-11195 Ki = 29.2 nM 7.54
CHEMBL4173816 Ki = 28.9 nM 7.54
CHEMBL4173118 Ki = 30.1 nM 7.52
CHEMBL4164932 Ki = 31.5 nM 7.50
CHEMBL4177167 Ki = 31.6 nM 7.50
CHEMBL4169328 Ki = 54.3 nM 7.26
CHEMBL4161842 Ki = 91.6 nM 7.04