General
Preferred name
GW-3965
Synonyms
GW 3965 hydrochloride ()
GW3965 ()
GW3965 hydrochloride ()
GW3965 HCl ()
GW 3965 ()
GW3965 (hydrochloride) ()
GW 3965 (hydrochloride) ()
P&D ID
PD015563
CAS
405911-09-3
405911-17-3
Tags
available
probe
drug candidate
Drug indication
Major depressive disorder
Drug Status
experimental
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
30
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT
GW3965 has been widely used as a chemical probe for the liver X receptors, alpha and beta. GW3965 is commonly employed in parallel with another LXR agonist such as T1317. T1317 is approximately 10-fold more potent in agonizing the LXRs in cells but suffers from the liability of activity at a handful of other nuclear receptors, notably PXR. GW3965 has properties amenable for in vivo usage. Aug 7 2017 - 3:59pm; GW3965 is a selective non-steroidal agonist for the LXRa and LXRb receptors. GW3965 is suitable for in vivo use in mouse models where a 10mg/kg oral dose exceeds the LXR EC50. A complementary, structurally orthogonal tool is LXR-623, which could be used in parallel to confirm outcomes. Aug 11 2017 - 1:42pm; This appears to be a robust and credible probe for the investigation of LXR biology, though the primary literature reference is somewhat sparse in terms of utilization and limitation. It will be important for the community to report new findings using this probe to fully validate its applicability. Aug 18 2017 - 4:24pm; A 2020 publication shows that T0901317 exert unspecific effects on pancreatic β-cell function DOI: 10.1007/s12020-020-02241-4 Jul 9 2020 - 1:27pm
DESCRIPTION
GW3965 is a synthetic agonist of the liver X receptors (LXRs) α and β.
(GtoPdb)
MOA
Agonist
(Chemical Probes.org)
DESCRIPTION
Potent and selective RARgamma agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Orally active liver X receptor (LXR) agonist
(Tocriscreen Plus)
DESCRIPTION
Orally active liver X receptor (LXR) agonist
(Tocriscreen Total)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
4
Organisms
3
Compound Sets
23
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
JUMP-MOA Compound Set
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
NURSA ligand set
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
36
Molecular Weight
581.19
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
13
Ring Count
4
Aromatic Ring Count
4
cLogP
8.09
TPSA
49.77
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
6.0
QED
0.16
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Nuclear Receptors
Target
LXR
hLXR??
LXR??/SRC1?LiSA
NR1H2, NR1H3
NR1H3, NR1H2
Liver X Receptor
Pathway
Metabolic Enzyme/Protease
Metabolism
Vitamin D Related/Nuclear Receptor
Primary Target
LXR-like Receptors
MOA
Agonist
Liver X Receptor (LXR) Agonists
ABCA1 Expression Enhancers
LXR agonist
Member status
member
Target subclass
NR1 Subfamily
NR1 Subfamily, NR1 Subfamily
Orthogonal probe
T0901317
Target class
NHR, NHR
Recommended Cell Concentration
None
Source data
