Assay Detail

CHEMBL947354

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Binding

Displacement of radiolabeled cimetidine from human histamine H2 receptor

ChEMBL ↗

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Target

Histamine H2 receptor (CHEMBL1941) ↗

Open DB target context

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Histamine H2 receptor (CHEMBL1941) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histamine H2 receptor

CHEMBL1941

Anchored from Assay target.

Protein identity Histamine H2 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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histamine H2 receptor (CHEMBL1941) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.
J Med Chem (2008) 51 : 7094 -7098
PubMed 18983139 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.75	6.75
Ki	1	6.77	6.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL30	CIMETIDINE	4.0	2	6.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL30	CIMETIDINE	Ki	=	170.0	nM	6.77
CHEMBL30	CIMETIDINE	IC50	=	180.0	nM	6.75