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Assay Detail

CHEMBL4337400

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Binding
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

[<sup>3</sup>H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H<sub>4</sub> Receptors.
Bartole E, Littmann T, Tanaka M, Ozawa T, Buschauer A, Bernhardt G.
J Med Chem (2019) 62 : 8338 -8356
PubMed 31469288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.58 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454158 1 8.38
CHEMBL4443126 1 8.16
CHEMBL4455324 1 7.84
CHEMBL4439142 1 7.73
CHEMBL90 HISTAMINE 4.0 1 7.47
CHEMBL4437371 1 7.40
CHEMBL4518374 1 7.37
CHEMBL4445423 1 7.05
CHEMBL4543119 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454158 EC50 = 4.169 nM 8.38
CHEMBL4443126 EC50 = 6.918 nM 8.16
CHEMBL4455324 EC50 = 14.45 nM 7.84
CHEMBL4439142 EC50 = 18.62 nM 7.73
CHEMBL90 HISTAMINE EC50 = 33.88 nM 7.47
CHEMBL4437371 EC50 = 39.81 nM 7.40
CHEMBL4518374 EC50 = 42.66 nM 7.37
CHEMBL4445423 EC50 = 89.13 nM 7.05
CHEMBL4543119 EC50 = 138.04 nM 6.86