Assay Detail

CHEMBL3097146

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Binding

Displacement of [3H]-R-alpha-ethylhistamine from rat histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry

ChEMBL ↗

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Target

Histamine H3 receptor (CHEMBL4124) ↗

Open DB target context

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Histamine H3 receptor (CHEMBL4124) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histamine H3 receptor

CHEMBL4124

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	Rattus norvegicus
Cell Type	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histamine H3 receptor (CHEMBL4124) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.

Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD.
Bioorg Med Chem Lett (2013) 23 : 6890 -6896
PubMed 24269482 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	3	9.32	9.83

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3092650	GSK239512	2.0	1	9.83
CHEMBL517140	GSK189254	2.0	1	9.17
CHEMBL1783890	—	—	1	8.95

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3092650	GSK239512	Ki	=	0.1479	nM	9.83
CHEMBL517140	GSK189254	Ki	=	0.6761	nM	9.17
CHEMBL1783890	—	Ki	=	1.122	nM	8.95