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Assay Detail

CHEMBL4036800

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Binding
Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
3
Total Activities
3
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

Systematic Data Mining Reveals Synergistic H3R/MCHR1 Ligands.
Schaller D, Hagenow S, Alpert G, Naß A, Schulz R, Bermudez M, Stark H, Wolber G.
ACS Med Chem Lett (2017) 8 : 648 -653
PubMed 28626527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.98 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196573 1 7.97
CHEMBL214957 1 6.68
CHEMBL584538 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196573 Ki = 10.6 nM 7.97
CHEMBL214957 Ki = 208.0 nM 6.68
CHEMBL584538 Ki = 516.7 nM 6.29