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Assay Detail

CHEMBL5057269

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

Functional
Antagonist activity at histamine H3 receptor (unknown origin)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Histamine H<sub>3</sub> receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation.
Falkenstein M, Reiner-Link D, Zivkovic A, Gering I, Willbold D, Stark H.
Bioorg Med Chem (2021) 50 : 116462 -116462
PubMed 34695709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.65 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527011 1 8.70
CHEMBL462605 PITOLISANT 4.0 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527011 Ki = 1.995 nM 8.70
CHEMBL462605 PITOLISANT Ki = 2.512 nM 8.60