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Assay Detail

CHEMBL1817088

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Binding
Inhibition of human H3 receptor
1
Total Activities
1
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 and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Hudkins RL, Raddatz R, Tao M, Mathiasen JR, Aimone LD, Becknell NC, Prouty CP, Knutsen LJ, Yazdanian M, Moachon G, Ator MA, Mallamo JP, Marino MJ, Bacon ER, Williams M.
J Med Chem (2011) 54 : 4781 -4792
PubMed 21634396 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.77 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476323 MK-0249 2.0 1 8.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476323 MK-0249 Ki = 1.7 nM 8.77