Assay Detail

CHEMBL4415153

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Binding

Inhibition of Guinea Pig Ileum H3R

ChEMBL ↗

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Target

Histamine H3 receptor (CHEMBL5076) ↗

Open DB target context

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Histamine H3 receptor (CHEMBL5076) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histamine H3 receptor

CHEMBL5076

Anchored from Assay target.

Protein identity Histamine H3 receptor

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	Cavia porcellus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histamine H3 receptor (CHEMBL5076) ↗

Type	SINGLE PROTEIN
Organism	Cavia porcellus

Publication

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Vanda D, Zajdel P, Soural M.
Eur J Med Chem (2019) 181 : 111569 -111569
PubMed 31404862 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	8.86	9.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL462605	PITOLISANT	4.0	1	9.80
CHEMBL3700336	LML-134	2.0	1	7.92

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL462605	PITOLISANT	Ki	=	0.16	nM	9.80
CHEMBL3700336	LML-134	Ki	=	12.0	nM	7.92