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Assay Detail

CHEMBL760163

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Binding
In vitro inhibition of [11C]2 binding to Peripheral benzodiazepine receptor (PBR) in rat brain
6
Total Activities
6
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 Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain.
Zhang MR, Maeda J, Ogawa M, Noguchi J, Ito T, Yoshida Y, Okauchi T, Obayashi S, Suhara T, Suzuki K.
J Med Chem (2004) 47 : 2228 -2235
PubMed 15084121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.14 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292092 1 10.11
CHEMBL63064 1 9.80
CHEMBL63065 1 9.77
CHEMBL481537 PK-11195 1 9.08
CHEMBL72521 1 8.32
CHEMBL443526 1 7.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292092 Ki = 0.078 nM 10.11
CHEMBL63064 Ki = 0.16 nM 9.80
CHEMBL63065 Ki = 0.17 nM 9.77
CHEMBL481537 PK-11195 Ki = 0.83 nM 9.08
CHEMBL72521 Ki = 4.8 nM 8.32
CHEMBL443526 Ki = 18.1 nM 7.74