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Assay Detail

CHEMBL4137782

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

Binding
Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
Bautista-Aguilera ÓM, Budni J, Mina F, Medeiros EB, Deuther-Conrad W, Entrena JM, Moraleda I, Iriepa I, López-Muñoz F, Marco-Contelles J.
J Med Chem (2018) 61 : 6937 -6943
PubMed 29969030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.97 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173258 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173258 Ki = 10.8 nM 7.97