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Assay Detail

CHEMBL948371

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

Binding
Displacement of [3H]PK11195 from peripheral benzodiazepine receptor in rat kidney membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
Fookes CJ, Pham TQ, Mattner F, Greguric I, Loc'h C, Liu X, Berghofer P, Shepherd R, Gregoire MC, Katsifis A.
J Med Chem (2008) 51 : 3700 -3712
PubMed 18557607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.33 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469681 1 8.43
CHEMBL469682 1 8.39
CHEMBL512306 DPA-714 2.0 1 8.25
CHEMBL469680 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469681 Ki = 3.7 nM 8.43
CHEMBL469682 Ki = 4.1 nM 8.39
CHEMBL512306 DPA-714 Ki = 5.6 nM 8.25
CHEMBL469680 Ki = 5.8 nM 8.24