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Assay Detail

CHEMBL5104248

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

Binding
Displacement of [3H]-flunitrazepam from TSPO receptor in Wistar rat brain without cerebellum incubated for 90 mins by liquid scintillation counter analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

An update into the medicinal chemistry of translocator protein (TSPO) ligands.
Barresi E, Robello M, Costa B, Da Pozzo E, Baglini E, Salerno S, Da Settimo F, Martini C, Taliani S.
Eur J Med Chem (2021) 209 : 112924 -112924
PubMed 33081988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.50 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193551 1 9.30
CHEMBL481537 PK-11195 1 8.94
CHEMBL54349 ALPIDEM 4.0 1 8.10
CHEMBL5191240 1 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193551 Ki = 0.5 nM 9.30
CHEMBL481537 PK-11195 Ki = 1.14 nM 8.94
CHEMBL54349 ALPIDEM Ki = 7.9 nM 8.10
CHEMBL5191240 Ki = 22.2 nM 7.65