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Assay Detail

CHEMBL1114779

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

Binding
Displacement of [3H]Ro5-4864 from TSPO in rat kidney mitochondrial membrane
7
Total Activities
4
Compounds Tested
2
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

Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.
Taliani S, Da Pozzo E, Bellandi M, Bendinelli S, Pugliesi I, Simorini F, La Motta C, Salerno S, Marini AM, Da Settimo F, Cosimelli B, Greco G, Novellino E, Martini C.
J Med Chem (2010) 53 : 4085 -4093
PubMed 20438080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.45 7.64
IC50 3 7.31 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286346 RO-54864 1 7.64
CHEMBL1097176 2 7.42
CHEMBL1099012 2 7.42
CHEMBL1097503 2 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286346 RO-54864 Ki = 23.0 nM 7.64
CHEMBL1097176 Ki = 37.9 nM 7.42
CHEMBL1099012 Ki = 37.6 nM 7.42
CHEMBL1099012 IC50 = 42.2 nM 7.38
CHEMBL1097176 IC50 = 45.6 nM 7.34
CHEMBL1097503 Ki = 49.5 nM 7.30
CHEMBL1097503 IC50 = 59.7 nM 7.22