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Assay Detail

CHEMBL3296477

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

Binding
Displacement of [3H]PK11195 from TSPO in rat C6 cell membrane after 90 mins by radioligand binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, Characterization, and in Vitro Evaluation of a New TSPO-Selective Bifunctional Chelate Ligand.
Denora N, Margiotta N, Laquintana V, Lopedota A, Cutrignelli A, Losacco M, Franco M, Natile G.
ACS Med Chem Lett (2014) 5 : 685 -689
PubMed 24944744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.27 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481537 PK-11195 1 9.40
CHEMBL339816 1 8.80
CHEMBL3287610 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481537 PK-11195 Ki = 0.4 nM 9.40
CHEMBL339816 Ki = 1.6 nM 8.80
CHEMBL3287610 Ki = 239.0 nM 6.62