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Assay Detail

CHEMBL4606571

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

Binding
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
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
Kd 4 7.44 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635634 2 7.78
CHEMBL4642520 2 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635634 Kd = 16.5 nM 7.78
CHEMBL4635634 Kd = 17.78 nM 7.75
CHEMBL4642520 Kd = 77.62 nM 7.11
CHEMBL4642520 Kd = 79.5 nM 7.10