General
Preferred name
GLPG-0974
Synonyms
GLPG 0974 ()
GLPG0974 ()
P&D ID
PD048653
CAS
1391076-61-1
Tags
available
drug candidate
probe
Drug indication
Abortion
Ulcerative colitis
Drug Status
investigational
Max Phase
2.0
Probe info
Probe type
experimental probe
P&D approved
Probe selectivity
protein-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
0
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)
MOA
Selective antagonist
DESCRIPTION
GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
PRICE
192
DESCRIPTION
GLPG0974 was a lead clinical development candidate. It acts as an antagonist of the free fatty acid receptor 2 (FFA2) . FFA2 is a GPCR involved in the mediation of inflammatory responses.
(GtoPdb)
MOA
Antagonist
(Chemical Probes.org)
DESCRIPTION
GLPG 0974 is a potent FFA2 antagonist (IC50 = 9 nM) with selectivity for FFA2 over FFA3. It was shown that GLPG 0974 inhibited acetate-induced human neutrophil migration in plasma or buffer, and also suppressed FFA2-induced expression of CD11b activation-specific epitope (AE) in human whole blood.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Potent and selective GPR139 agonist
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
20
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Chemical Probes.org
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
DrugBank
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
19
Molecular Weight
484.12
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
3
cLogP
5.05
TPSA
77.92
Fraction CSP3
0.32
Chiral centers
1.0
Largest ring
6.0
QED
0.48
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
FFA2
Free Fatty Acid Receptor
FFAR2
Primary Target
Free Fatty Acid Receptors
MOA
Antagonist
GPR43 antagonist
Member status
member
Orthogonal probe
(S)-4-CMTB
Pathway
GPCR/G protein
Endocrinology/Hormones
Target class
GPCR
Target subclass
Free fatty acid receptor
Recommended Cell Concentration
1 uM
Source data
