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Assay Detail

CHEMBL4606566

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

Binding
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 2 7.06 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635634 1 7.81
CHEMBL260374 THIOPERAMIDE 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635634 IC50 = 15.49 nM 7.81
CHEMBL260374 THIOPERAMIDE IC50 = 489.78 nM 6.31