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Assay Detail

CHEMBL5392891

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

Binding
Displacement of [3H]NAMH from human C-terminal Nluc-tagged Halo tag fused between T229/F348 residue histamine H3 receptor expressed in HEK293-A cells incubated for 2 hrs by scintillation counter analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H<sub>3</sub> Receptor.
Mönnich D, Nagl M, Forster L, Rosier N, Igel P, Pockes S.
ACS Med Chem Lett (2023) 14 : 1589 -1595
PubMed 37974943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.80 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268229 1 8.30
CHEMBL11919 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268229 Ki = 5.012 nM 8.30
CHEMBL11919 Ki = 50.12 nM 7.30