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Assay Detail

CHEMBL973551

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

Binding
Displacement of [3H]clonidine from Imidazoline receptor 1 in Sprague-Dawley rat kidney membrane
10
Total Activities
10
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

Nischarin (CHEMBL5221)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.
Gentili F, Cardinaletti C, Vesprini C, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Mattioli L, Perfumi M, Hudson A, Pigini M.
J Med Chem (2008) 51 : 5130 -5134
PubMed 18661965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.16 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508960 1 5.54
CHEMBL506350 1 5.45
CHEMBL525531 1 5.40
CHEMBL506016 1 5.37
CHEMBL498476 1 5.16
CHEMBL498261 1 5.14
CHEMBL450405 1 5.13
CHEMBL448918 1 4.62
CHEMBL497458 1 4.59
CHEMBL452401 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508960 IC50 = 2877.0 nM 5.54
CHEMBL506350 IC50 = 3569.0 nM 5.45
CHEMBL525531 IC50 = 3998.0 nM 5.40
CHEMBL506016 IC50 = 4255.0 nM 5.37
CHEMBL498476 IC50 = 6891.0 nM 5.16
CHEMBL498261 IC50 = 7301.0 nM 5.14
CHEMBL450405 IC50 = 7360.0 nM 5.13
CHEMBL448918 IC50 = 23890.0 nM 4.62
CHEMBL497458 IC50 = 25812.0 nM 4.59
CHEMBL452401 IC50 = 211600.0 nM -