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Assay Detail

CHEMBL4606602

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

Binding
Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
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 3 7.97 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT 1 8.60
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE 4.0 1 8.00
CHEMBL260374 THIOPERAMIDE 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 2.512 nM 8.60
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE Ki = 10.0 nM 8.00
CHEMBL260374 THIOPERAMIDE Ki = 50.12 nM 7.30