Assay Detail

CHEMBL1921323

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Functional

Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation

ChEMBL ↗

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Target

Histamine H4 receptor (CHEMBL3759) ↗

Open DB target context

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Histamine H4 receptor (CHEMBL3759) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histamine H4 receptor

CHEMBL3759

Anchored from Assay target.

Protein identity Histamine H4 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	Functional
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histamine H4 receptor (CHEMBL3759) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.

Mowbray CE, Bell AS, Clarke NP, Collins M, Jones RM, Lane CA, Liu WL, Newman SD, Paradowski M, Schenck EJ, Selby MD, Swain NA, Williams DH.
Bioorg Med Chem Lett (2011) 21 : 6596 -6602
PubMed 21920751 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.49	8.31

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1915540	ADRIFORANT	2.0	1	8.31
CHEMBL129198	JNJ-7777120	—	1	6.66

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1915540	ADRIFORANT	IC50	=	4.9	nM	8.31
CHEMBL129198	JNJ-7777120	IC50	=	221.4	nM	6.66