Assay Detail

CHEMBL3097149

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

Binding

Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in human cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

Histamine H3 receptor (CHEMBL264) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

Histamine H3 receptor (CHEMBL264) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histamine H3 receptor

CHEMBL264

Anchored from Assay target.

Protein identity Histamine H3 receptor

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histamine H3 receptor (CHEMBL264) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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	9.73	9.92

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3092650	GSK239512	2.0	1	9.92
CHEMBL1783890	—	—	1	9.67
CHEMBL517140	GSK189254	2.0	1	9.59

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3092650	GSK239512	Ki	=	0.1202	nM	9.92
CHEMBL1783890	—	Ki	=	0.2138	nM	9.67
CHEMBL517140	GSK189254	Ki	=	0.257	nM	9.59