General
Preferred name
FILGOTINIB
Synonyms
G-146034, GLPG-0634, G-146034_101, Filgotinib hydrochloride ()
GLPG0634 ()
Filgotinib（GLPG0643) ()
Filgotinib??GLPG0643) ()
GLPG0634 (maleate) ()
GLPG-0634 ()
Filgotinib (maleate) ()
G-146034 ()
G146034 ()
GS-6034 FREE BASE ()
Filgotinib (GLPG0634) ()
G146034_101 ()
G-146034_101 ()
FILGOTINIB HYDROCHLORIDE ()
GS-6034 ()
Jyseleca ()
FILGOTINIB MALEATE ()
Filgotinib-d4 ()
P&D ID
PD010273
CAS
1206161-97-8
1206101-20-3
1802998-75-9
2041095-50-3
Tags
available
drug
drug candidate
probe
Approved by
PMDA
EMA
First approval
2020
Drug indication
Cutaneous lupus erythematosus
Rheumatoid arthritis
Crohn disease
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
5
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
Filgotinib is one of a number of JAK inhibitors available with varying selectivity within the JAK family and across other kinases. I recommend using more than one JAK inhibitor as a tool in cellular assays. Filgotinib is reported to have geater functional selectivity for JAK1 over JAK2 in cells but biochemical selectivity is only about three-fold. Mouse pharmacokinetic data are not found in the literature. Mar 30 2017 - 8:19pm; The probe appears to show a significant degree of selectivity of JAK1 in cellular assays. I would hence recommend this compound as a fairly selective probe for JAK1 but not for the other kinases listed as targets (JAK2, JAK3, TYK2). The compounds appears to be very selective but has "only" been screened against 170 kinases. Screening of a wider panel would build even more confidence that this compound does not inhibit other kinases. The pharmokineted (PK) data clearly show that the compound is suitable for rat and dog in vivo experiments. It may be suitable for mouse in vivo experiments as well, but I could not find any mouse PK data. I thus recommend assessing PK in mice before using it in mice. Apr 12 2017 - 12:41pm; Filgotinib is an orally available, selective JAK1 inhibitor and is one of the best JAK inhibitors at this moment. However, the in vitro selectivity index to JAK2 is only 2.8, and the results should be interpreted with caution. Jun 16 2017 - 2:07pm
DESCRIPTION
Filgotinib is a selective and orally acive JAK1 inhibitor . It is being developed in a collaboration between Gilead Sciences and Galapagos for the treatment of inflammatory indications including psoriatic arthritis, ankylosing spondylitis, Crohn's disease, ulcerative colitis and rheumatoid arthritis. It is proposed as a once daily drug, that is predicted to cause fewer toxicity issues and adverse effects than existing JAK1 inhibitors.
(GtoPdb)
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Filgotinib is a potent and selective JAK1 inhibitor exhibiting 30-fold selectivity over JAK2. It was shown to inhibit Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro. Filgotinib has the potential for the treatment of rheumatoid arthritis and possibly other immune-inflammatory diseases.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
35
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
JUMP-MOA Compound Set
JUMP-Target 1 Compound Set
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
425.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
3
cLogP
1.98
TPSA
96.67
Fraction CSP3
0.38
Chiral centers
0.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
JAK1
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Chromatin/Epigenetic
JAK/STAT Signaling
Stem Cells
Anti-infection
Epigenetics
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
Target
JAK2
JAK3
TYK2
JAK1, JAK2, JAK3, TYK2
HIV
JAK
Member status
member
MOA
JAK inhibitor
Target class
Protein kinase
Kinase
Orthogonal probe
Baricitinib
Target subclass
TK
Recommended Cell Concentration
1 µM
Source data
