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Assay Detail

CHEMBL5531265

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

Functional
Antagonist activity at human Histamine H3 receptor expressed in human SK-N-MC cell membrane assessed as inhibition constant incubated for 60 mins in presence of [3H]-N-methylhistamine by liquid scintillation counter
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Steroid-Based Histamine H<sub>3</sub> Receptor Antagonists/Inverse Agonists.
Ledneczki I, Tapolcsányi P, Gábor E, Éles J, Barabás J, Béni Z, Varga B, Balázs O, Román V, Fodor L, Szikra J, Vastag M, Lévay G, Schmidt É, Lendvai B, Greiner I, Kiss B, Némethy Z, Mahó S.
J Med Chem (2024) 67 : 3643 -3667
PubMed 38393759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527011 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527011 Ki = 1.995 nM 8.70