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Assay Detail

CHEMBL653041

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

Binding
Binding affinity against peripheral benzodiazepine receptor( PBR).
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem.
Anzini M, Cappelli A, Vomero S, Giorgi G, Langer T, Bruni G, Romeo MR, Basile AS.
J Med Chem (1996) 39 : 4275 -4284
PubMed 8863805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.36 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481537 PK-11195 1 8.74
CHEMBL135870 1 8.72
CHEMBL135869 1 8.49
CHEMBL137689 1 8.41
CHEMBL54349 ALPIDEM 4.0 1 8.15
CHEMBL134590 1 7.40
CHEMBL334887 1 6.82
CHEMBL136030 1 6.54
CHEMBL135408 1 5.80
CHEMBL137730 1 4.48
CHEMBL335923 1 -
CHEMBL334761 1 -
CHEMBL2111919 1 -
CHEMBL133313 1 -
CHEMBL335388 1 -
CHEMBL338738 1 -
CHEMBL335049 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481537 PK-11195 IC50 = 1.8 nM 8.74
CHEMBL135870 IC50 = 1.9 nM 8.72
CHEMBL135869 IC50 = 3.2 nM 8.49
CHEMBL137689 IC50 = 3.9 nM 8.41
CHEMBL54349 ALPIDEM IC50 = 7.0 nM 8.15
CHEMBL134590 IC50 = 40.0 nM 7.40
CHEMBL334887 IC50 = 150.0 nM 6.82
CHEMBL136030 IC50 = 290.0 nM 6.54
CHEMBL135408 IC50 = 1600.0 nM 5.80
CHEMBL137730 IC50 = 33000.0 nM 4.48
CHEMBL335923 IC50 > 1000.0 nM -
CHEMBL334761 IC50 > 1000.0 nM -
CHEMBL2111919 IC50 > 1000.0 nM -
CHEMBL133313 IC50 > 1000.0 nM -
CHEMBL335388 IC50 > 1000.0 nM -
CHEMBL338738 IC50 > 1000.0 nM -
CHEMBL335049 IC50 > 1000.0 nM -