General
Preferred name
GSK189254
Synonyms
6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide ()
GSK-189254 ()
GSK189254A ()
GSK 189254 ()
GSK189254 (free base) ()
P&D ID
PD086011
CAS
720690-73-3
Tags
available
drug candidate
Drug indication
Narcolepsy
Cognitive impairment
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
PRICE 101
DESCRIPTION Potent and selective H3 histamine receptor inverse agonist. Radioligand 11C-GSK189254 can be used to quantify H3 receptor availability in humans in vivo using PET. (GtoPdb)
DESCRIPTION GSK189254A is a novel, potent and selective histamine H3 receptor antagonist. (Enamine Bioactive Compounds)
DESCRIPTION GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3). (TargetMol Bioactive Compound Library)
Compound Sets
16
Cayman Chemical Bioactives
36705
ChEMBL Drugs
CHEMBL517140
Concise Guide to Pharmacology 2021/22
10736
Concise Guide to Pharmacology 2023/24
10736
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DMKXPOL
Enamine Bioactive Compounds
EBC-07631
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS100200
Guide to Pharmacology
10736
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL517140
MedChem Express Bioactive Compound Library
HY-14111
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
TargetMol Bioactive Compound Library
TQ0066
External IDs
15
Properties
(calculated by RDKit )
Molecular Weight
351.19
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
2
cLogP
3.76
TPSA
57.95
Fraction CSP3
0.43
Chiral centers
0.0
Largest ring
7.0
QED
0.67
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Member status
member
MOA
Histamine H3 Receptor Inverse Agonists
Histamine H3 Receptor Antagonists
Histamine Receptor antagonist
Target
Histamine Receptor
Human H3 receptor
Mouse H3 receptor
Source data