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Assay Detail

CHEMBL5228263

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Binding
Displacement of [3H]CB34 from TSPO receptor in rat brain cortex membrane by liquid scintillation spectrometer method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Exploring Translocator Protein (TSPO) Medicinal Chemistry: An Approach for Targeting Radionuclides and Boron Atoms to Mitochondria.
Giordani A, Menziani MC, Moresco RM, Matarrese M, Paolino M, Saletti M, Giuliani G, Anzini M, Cappelli A.
J Med Chem (2021) 64 : 9649 -9676
PubMed 34254805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.07 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325820 1 8.66
CHEMBL481537 PK-11195 1 8.08
CHEMBL120668 1 8.06
CHEMBL121674 1 8.01
CHEMBL120763 1 7.96
CHEMBL331928 1 7.92
CHEMBL332775 1 7.42
CHEMBL325701 1 7.19
CHEMBL122301 1 5.83
CHEMBL119566 1 5.57
CHEMBL332801 1 5.18
CHEMBL120398 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325820 IC50 = 2.2 nM 8.66
CHEMBL481537 PK-11195 IC50 = 8.4 nM 8.08
CHEMBL120668 IC50 = 8.7 nM 8.06
CHEMBL121674 IC50 = 9.8 nM 8.01
CHEMBL120763 IC50 = 11.0 nM 7.96
CHEMBL331928 IC50 = 12.0 nM 7.92
CHEMBL332775 IC50 = 38.0 nM 7.42
CHEMBL325701 IC50 = 64.0 nM 7.19
CHEMBL122301 IC50 = 1490.0 nM 5.83
CHEMBL119566 IC50 = 2700.0 nM 5.57
CHEMBL332801 IC50 = 6600.0 nM 5.18
CHEMBL120398 IC50 = 11500.0 nM 4.94