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Assay Detail

CHEMBL3755809

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Binding
Displacement of [3H]Nalpha-methylhistamine from human histamine 3 receptor expressed in Sf9 cell membranes by liquid scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.
Hammer SG, Gobleder S, Naporra F, Wittmann HJ, Elz S, Heinrich MR, Strasser A.
Bioorg Med Chem Lett (2016) 26 : 292 -300
PubMed 26718844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.28 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752085 1 5.60
CHEMBL3752270 1 5.22
CHEMBL494093 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752085 Ki = 2511.89 nM 5.60
CHEMBL3752270 Ki = 6025.6 nM 5.22
CHEMBL494093 Ki = 9772.37 nM 5.01