Assay Detail

CHEMBL3855979

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Binding

Displacement of [3H]idazoxan from I2 receptor imidazoline binding site in rabbit kidney membranes after 45 mins by gamma counting method

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Oryctolagus cuniculus
Tissue	Kidney
Subcellular	Membrane
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

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	2	8.10	8.72

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL275970	TRACIZOLINE	—	1	8.72
CHEMBL13881	PHENAMAZOLINE	2.0	1	7.48

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL275970	TRACIZOLINE	Ki	=	1.905	nM	8.72
CHEMBL13881	PHENAMAZOLINE	Ki	=	33.11	nM	7.48