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Assay Detail

CHEMBL3855950

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

Binding
Displacement of [125I]-p-iodoclonidine from I1 receptor imidazoline binding site in Sprague-Dawley rat kidney cell membranes after 30 mins by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nischarin (CHEMBL5221)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Combined Interactions with I1-, I2-Imidazoline Binding Sites and α2-Adrenoceptors To Manage Opioid Addiction.
Giusepponi ME, Cifani C, Micioni Di Bonaventura MV, Mattioli L, Hudson A, Diamanti E, Del Bello F, Giannella M, Mammoli V, Paoletti CD, Piergentili A, Pigini M, Quaglia W.
ACS Med Chem Lett (2016) 7 : 956 -961
PubMed 27774136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.97 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337862 1 8.85
CHEMBL3904276 1 8.70
CHEMBL3961335 1 8.40
CHEMBL51358 1 8.12
CHEMBL3892351 1 8.08
CHEMBL1439667 1 7.75
CHEMBL3920069 1 7.62
CHEMBL3939078 1 7.16
CHEMBL3911124 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337862 Ki = 1.413 nM 8.85
CHEMBL3904276 Ki = 1.995 nM 8.70
CHEMBL3961335 Ki = 3.981 nM 8.40
CHEMBL51358 Ki = 7.586 nM 8.12
CHEMBL3892351 Ki = 8.318 nM 8.08
CHEMBL1439667 Ki = 17.78 nM 7.75
CHEMBL3920069 Ki = 23.99 nM 7.62
CHEMBL3939078 Ki = 69.18 nM 7.16
CHEMBL3911124 Ki = 97.72 nM 7.01