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Assay Detail

CHEMBL4606554

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

Binding
Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
4
Total Activities
4
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

UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H3 and H4 Receptors.
Bartole E, Grätz L, Littmann T, Wifling D, Seibel U, Buschauer A, Bernhardt G.
J Med Chem (2020) 63 : 5297 -5311
PubMed 32420741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.64 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4641846 1 8.37
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE 4.0 1 7.73
CHEMBL4644353 1 7.43
CHEMBL4634086 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4641846 Ki = 4.266 nM 8.37
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE Ki = 18.62 nM 7.73
CHEMBL4644353 Ki = 37.15 nM 7.43
CHEMBL4634086 Ki = 93.33 nM 7.03