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Assay Detail

CHEMBL1655210

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

Binding
Displacement of [11C]PBR28 from TSPO in rat kidney mitochondrial membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.
Pike VW, Taliani S, Lohith TG, Owen DR, Pugliesi I, Da Pozzo E, Hong J, Zoghbi SS, Gunn RN, Parker CA, Rabiner EA, Fujita M, Innis RB, Martini C, Da Settimo F.
J Med Chem (2011) 54 : 366 -373
PubMed 21133364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.54 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53430 1 9.43
CHEMBL294625 1 8.85
CHEMBL299487 1 8.37
CHEMBL431938 1 8.12
CHEMBL56058 1 7.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53430 Ki = 0.37 nM 9.43
CHEMBL294625 Ki = 1.4 nM 8.85
CHEMBL299487 Ki = 4.28 nM 8.37
CHEMBL431938 Ki = 7.5 nM 8.12
CHEMBL56058 Ki = 12.2 nM 7.91