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Assay Detail

CHEMBL4337198

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Binding
Inhibition of human histamine H3 receptor
6
Total Activities
6
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

Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Rodríguez-Soacha DA, Scheiner M, Decker M.
Eur J Med Chem (2019) 180 : 690 -706
PubMed 31401465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.00 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173258 1 7.97
CHEMBL14638 CIPROXIFAN 1 7.34
CHEMBL3323035 1 7.12
CHEMBL1929421 1 7.08
CHEMBL3747907 1 6.89
CHEMBL3323053 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173258 Ki = 10.8 nM 7.97
CHEMBL14638 CIPROXIFAN Ki = 46.0 nM 7.34
CHEMBL3323035 Ki = 76.2 nM 7.12
CHEMBL1929421 Ki = 84.2 nM 7.08
CHEMBL3747907 Ki = 128.0 nM 6.89
CHEMBL3323053 Ki = 2500.0 nM 5.60