GSK-189254A

Investigational

CNC(=O)C1=CC=C(OC2=CC=C3CCN(CCC3=C2)C4CCC4)N=C1

InChIKey=WROHEWWOCPRMIA-UHFFFAOYSA-N

InChI=1S/C21H25N3O2/c1-22-21(25)17-6-8-20(23-14-17)26-19-7-5-15-9-11-24(18-3-2-4-18)12-10-16(15)13-19/h5-8,13-14,18H,2-4,9-12H2,1H3,(H,22,25)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H3 receptor 44 Target ID: CHEMBL264 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17327487	Antagonist 2778		9.6 null [pKi]

PubMed

Title	Date	PubMed
Soraprazan: setting new standards in inhibition of gastric acid secretion.	2007 Jun	17369284
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.	2007 Jun	17327487
When reversible ligands do not reverse, and other modelers' dilemmas.	2010 Jul	20554739
Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET.	2010 Jul	20554726
Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems.	2010 Oct 1	20682302
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.	2011 Jul 14	21634396

Patents

Substance Class	Chemical Created by `admin` on `Sat Dec 16 07:01:28 UTC 2023` Edited by `admin` on `Sat Dec 16 07:01:28 UTC 2023`
Record UNII	5T4TX6CO53
Record Status	`Validated (UNII)`
Record Version

Name

Type

Language

GSK-189254A

Common Name

English

GSK-189254 FREE BASE

Code

English

6-((3-CYCLOBUTYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPIN-7-YL)OXY)-N-METHYL-3-PYRIDINECARBOXAMIDE

Systematic Name

English

GSK-189254

Code

English

Code System Code Type Description

SMS_ID

300000042429