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Assay Detail

CHEMBL4337406

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

Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL4468)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8.49 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454158 1 10.30
CHEMBL4443126 1 9.21
CHEMBL4439142 1 9.19
CHEMBL4543119 1 8.93
CHEMBL4445423 1 8.86
CHEMBL4455324 1 8.75
CHEMBL4437371 1 7.64
CHEMBL4518374 1 7.03
CHEMBL90 HISTAMINE 4.0 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454158 EC50 = 0.05012 nM 10.30
CHEMBL4443126 EC50 = 0.6166 nM 9.21
CHEMBL4439142 EC50 = 0.6457 nM 9.19
CHEMBL4543119 EC50 = 1.175 nM 8.93
CHEMBL4445423 EC50 = 1.38 nM 8.86
CHEMBL4455324 EC50 = 1.778 nM 8.75
CHEMBL4437371 EC50 = 22.91 nM 7.64
CHEMBL4518374 EC50 = 93.33 nM 7.03
CHEMBL90 HISTAMINE EC50 = 295.12 nM 6.53