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Assay Detail

CHEMBL1921324

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

Functional
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
2
Total Activities
2
Compounds Tested
1
Activity Types
0
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 8.59 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915540 ADRIFORANT 2.0 1 8.89
CHEMBL129198 JNJ-7777120 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915540 ADRIFORANT IC50 = 1.3 nM 8.89
CHEMBL129198 JNJ-7777120 IC50 = 5.3 nM 8.28