General
Preferred name
PF-4191834
Synonyms
PF-04191834 ()
PF04191834 ()
Pf-04191834 ()
P&D ID
PD047703
CAS
1029317-21-2
Tags
available
drug candidate
Drug indication
osteoarthritis, knee
Asthma
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 PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain[1].
PRICE 64
DESCRIPTION PF-4191834 is an orally available, novel, selective non-redox 5-lipoxygenase (ALOX5) inhibitor with potential antiinflammatory and analgesic activity . (GtoPdb)
DESCRIPTION PF-04191834 is an inhibitor of the 5-Lipoxygenase (5-LOX), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain. (Enamine Bioactive Compounds)
DESCRIPTION PF04191834 is a novel, potent and selective non-redox 5-lipoxygenase(5-LOX) inhibitor with an IC50 value of 229 +/- 20 nM. It inhibits 5-LOX in human blood cells with an IC80 value of 370 +/- 20 nM. It exhibits good potency in enzyme- and cell-based assays, as well as in a rat model of acute inflammation. It demonstrated approximately 300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and shows no activity toward the cyclooxygenase enzymes. It is effective in inflammation and pain. (BOC Sciences Bioactive Compounds)
DESCRIPTION PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834 (TargetMol Bioactive Compound Library)
Compound Sets
15
BOC Sciences Bioactive Compounds
pf04191834-cas-1029317-21-2-item-474983
ChEMBL Drugs
CHEMBL4297416
Concise Guide to Pharmacology 2017/18
9054
Concise Guide to Pharmacology 2019/20
9054
Concise Guide to Pharmacology 2021/22
9054
Concise Guide to Pharmacology 2023/24
9054
Drug Repurposing Hub
DrugBank
DB11645
DrugMAP
DM3DWKN
Enamine Bioactive Compounds
EBC-501076
EUbOPEN Chemogenomics Library
EUB0001857
Guide to Pharmacology
9054
MedChem Express Bioactive Compound Library
HY-117048
ReFrame library
TargetMol Bioactive Compound Library
T16503
External IDs
16
Properties
(calculated by RDKit )
Molecular Weight
393.15
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
3.77
TPSA
70.14
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Lipoxygenase
5-Lipoxygenase
5-LOX
MOA
Lipoxygenase inhibitor
Pathway
Metabolic Enzyme/Protease
Metabolism
Solubility
10 mM in DMSO
Recommended Cell Concentration
None
Source data