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Assay Detail

CHEMBL4337316

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

Binding
Displacement of [3H]PK11195 from wild-type human TSPO expressed in HEK293 cells after 90 mins by scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL5742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.
Cheng HWA, Sokias R, Werry EL, Ittner LM, Reekie TA, Du J, Gao Q, Hibbs DE, Kassiou M.
J Med Chem (2019) 62 : 8235 -8248
PubMed 31419132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.67 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4459176 1 8.49
CHEMBL416715 (R)PK-11195 1 7.87
CHEMBL4439049 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4459176 Ki = 3.2 nM 8.49
CHEMBL416715 (R)PK-11195 Ki = 13.6 nM 7.87
CHEMBL4439049 Ki = 217.3 nM 6.66