Assay Detail

CHEMBL4358957

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Binding

Displacement of [3H]2-BFI from I2IR in Swiss mouse brain cortex incubated for 45 mins by liquid scintillation spectrometry

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

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	Mus musculus
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease.

Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, de Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallàs M, Callado LF, Escolano C.
J Med Chem (2020) 63 : 3610 -3633
PubMed 32150414 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	6.05	6.41

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4450506	—	—	1	6.41
CHEMBL10316	IDAZOXAN	3.0	1	5.68

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4450506	—	Ki	=	389.05	nM	6.41
CHEMBL10316	IDAZOXAN	Ki	=	2089.3	nM	5.68