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BAY-439 | BAY-439 : Inhibitor of PLA2G5
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PLA2G5
  • Kd:214 nM
  • IC50:7 nM
  • IC50:61 nM
up to 300 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity withing the target family: BAY-439 presents a selectivity window with 110-fold selectivi ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
BAY-439 was shown to be inactive on 4 enzymes (PLCβ3, PLCδ1, PLCγ1, PLCζ1) up to the highest concen ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Eurofins Bayer Safety Screen (77 targets) at 10 µM: Closest off-targets: human SLC6A3 (82 % inhibiti ...

Potency
Cellular
In Vitro

PLA2G5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6c00488

In Vivo Validations

Rat
Dose: 0.5 mg/Kg IV, 3 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 6.9 h IV, 6.0 h PO
Systemic clearance: 0.04 L/h/Kg
Bioavailability: 50%
Volume of Distribution at Steady-State: 0.2 L/Kg

DOI Reference: 10.1021/acs.jmedchem.6c00488

Negative Control Compounds

BAY-163
Notes: Biochemical assay: PLA2G5 human (IC50 > 25 µM), mouse/rat (IC50 > 20 µM), human PLA2G4A (IC50 >40 µM), PLA2G7 (IC50 > 40 µM), PLA2G2A (IC50 = 24.1 µM), PLA2G10 (IC50 = 14.3 µM); Nuvisan Phospholipase C panel: human PLCB3/PLCD1/PLCG1 / PLCZ1 (all IC50 >20 µM); Binding (SPR): human PLA2G5 (KD > 10 µM); Eurofins Bayer Safety Screen (77 targets) at 10 µM: Closest off-targets: human SLC6A3 (52 % inhibition), ADRA2C (54 % inhibition), Adenosine transporter (88 % inhibition) Kinase panel (378 kinases) at 10 μM: Closest off-target is DYRK1A (52 % inhibition)

Orthogonal Probes def

DARAPLADIB

Chemical Information

Molecular Formula C21H24N4O2
SMILEs CCNc1cc(C#Cc2ccc(OC3CCN(C(N)=O)CC3)cc2)ccn1
InChI InChI=1S/C21H24N4O2/c1-2-23-20-15-17(9-12-24-20)4-3-16-5-7-18(8-6-16)27-19-10-13-25(14-11-19)21(22)26/h5-9,12,15,19H,2,10-11,13-14H2,1H3,(H2,22,26)(H,23,24)
Molecular weight 364.19 Da
AlogP 2.8351000000000015
HBond acceptors 6
HBond donors 3
Atoms 51

Expert Reviews

by SERP
(on 25 Jun 2026)
Cellular Use Rating
In Model Organisms
The recommended maximum concentration of up to 300 nM in cellular assays is scientifically reasonable, considering the observed off-target profile and the cellular enzymatic assay IC50 values (61 nM). However,...
by SERP
(on 7 Jul 2026)
Cellular Use Rating
In Model Organisms
BAY-439 is a highly potent, selective, and soluble probe for hPLA2-G5. It enables the study of the biology of PLA2-G5 in cells. Since the probe exhibits unprecedented selectivity against other Phospholipase...
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