Compound name
PITOLISANT
Protein family
GPCR
Target name
HRH3
Affinity biochemical (nM)
2.6
Affinity on-target cellular (nM)
12.02
Compound EUbOPEN ID
EUB0000475aCl
SMILES
[H]Cl.ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1
InChIKey
XLFKECRRMPOAQS-UHFFFAOYSA-N
NCBI gene ID
11255
UniProt ID
Q9Y5N1
Synonyms
GPCR97
Mode of action
Inverse agonist
Affinity biochemical definition
Ki
Affinity biochemical assay type
Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in CHO-K1 cells
Affinity Biochemical Source Knowledge
18774720
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Affinity on-target cellular relation
=