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Assay Detail

CHEMBL650802

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

Binding
Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.
Dalpiaz A, Bertolasi V, Borea PA, Nacci V, Fiorini I, Campiani G, Mennini T, Manzoni C, Novellino E, Greco G.
J Med Chem (1995) 38 : 4730 -4738
PubMed 7473601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.65 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288551 1 8.05
CHEMBL116087 1 7.52
CHEMBL286909 1 7.02
CHEMBL358133 1 5.50
CHEMBL142639 1 5.16
CHEMBL317219 1 -
CHEMBL284371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288551 Ki = 9.0 nM 8.05
CHEMBL116087 Ki = 30.0 nM 7.52
CHEMBL286909 Ki = 95.0 nM 7.02
CHEMBL358133 Ki = 3150.0 nM 5.50
CHEMBL142639 Ki = 7000.0 nM 5.16
CHEMBL317219 Ki > 10.0 nM -
CHEMBL284371 Ki > 10.0 nM -