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Assay Detail

CHEMBL5392889

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Binding
Binding affinity to histamine H3 receptor (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 4 8.45 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129542 JNJ-5207852 1 9.20
CHEMBL462605 PITOLISANT 4.0 1 8.60
CHEMBL268229 1 8.40
CHEMBL11919 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129542 JNJ-5207852 Ki = 0.631 nM 9.20
CHEMBL462605 PITOLISANT Ki = 2.512 nM 8.60
CHEMBL268229 Ki = 3.981 nM 8.40
CHEMBL11919 Ki = 25.12 nM 7.60