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Assay Detail

CHEMBL859957

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

Binding
Displacement of [11C](R)-PK1119 from Sprague-Dawley rat brain PBR
5
Total Activities
5
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

[2-11C]isopropyl-, [1-11C]ethyl-, and [11C]methyl-labeled phenoxyphenyl acetamide derivatives as positron emission tomography ligands for the peripheral benzodiazepine receptor: radiosynthesis, uptake, and in vivo binding in brain.
Zhang MR, Ogawa M, Maeda J, Ito T, Noguchi J, Kumata K, Okauchi T, Suhara T, Suzuki K.
J Med Chem (2006) 49 : 2735 -2742
PubMed 16640334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 9.83 10.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205971 1 10.13
CHEMBL63064 1 10.02
CHEMBL381602 1 10.01
CHEMBL205767 1 9.72
CHEMBL481537 PK-11195 1 9.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205971 Ki = 0.074 nM 10.13
CHEMBL63064 Ki = 0.095 nM 10.02
CHEMBL381602 Ki = 0.098 nM 10.01
CHEMBL205767 Ki = 0.19 nM 9.72
CHEMBL481537 PK-11195 Ki = 0.54 nM 9.27