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Assay Detail

CHEMBL4606603

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

Binding
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
4
Total Activities
4
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
Ki 4 7.33 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129198 JNJ-7777120 1 7.90
CHEMBL14690 CLOBENPROPIT 1 7.40
CHEMBL260374 THIOPERAMIDE 1 7.20
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE 4.0 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129198 JNJ-7777120 Ki = 12.59 nM 7.90
CHEMBL14690 CLOBENPROPIT Ki = 39.81 nM 7.40
CHEMBL260374 THIOPERAMIDE Ki = 63.1 nM 7.20
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE Ki = 158.49 nM 6.80