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Assay Detail

CHEMBL4606570

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

Binding
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL5657)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H3 and H4 Receptors.
Bartole E, Grätz L, Littmann T, Wifling D, Seibel U, Buschauer A, Bernhardt G.
J Med Chem (2020) 63 : 5297 -5311
PubMed 32420741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.43 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260374 THIOPERAMIDE 1 7.55
CHEMBL4635634 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260374 THIOPERAMIDE EC50 = 28.18 nM 7.55
CHEMBL4635634 EC50 = 50.12 nM 7.30