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GSK256066 | Inhibitor of PDE4B
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
PDE4B
  • IC50:0.079 nM
  • IC50:0.01 nM
  • IC50:0.12 nM
Inhibitor
Cellular activity range includes 0.01 nM, solubility may be limiting at higher concentrations
0.1-10 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
>1000-fold selective versus PDEs 1–3 and 5–7

Potency
Cellular
In Vitro

PDE4B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2009.04.012

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 1.1 h (IV)
Systemic clearance: 39 mL/min/kg
Fb : 0% (PO)

DOI Reference: 10.1016/j.bmcl.2009.04.012

Dose:
Route of delivery: Intratracheal
Volume of Distribution at Steady-State: 0.8 L/kg

DOI Reference: 10.1016/j.bmcl.2009.04.012

Negative Control Compounds

cpd 3

Orthogonal Probes def

R(-)Rolipram

Chemical Information

Molecular Formula C27H26N4O5S
SMILEs COc1cccc(Nc2c(C(N)=O)cnc3c(C)cc(S(=O)(=O)c4cccc(C(=O)N(C)C)c4)cc23)c1
InChI InChI=1S/C27H26N4O5S/c1-16-11-21(37(34,35)20-10-5-7-17(12-20)27(33)31(2)3)14-22-24(16)29-15-23(26(28)32)25(22)30-18-8-6-9-19(13-18)36-4/h5-15H,1-4H3,(H2,28,32)(H,29,30)
Molecular weight 518.16 Da
AlogP 3.92892
HBond acceptors 9
HBond donors 3
Atoms 63

Vendors

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Expert Reviews

by SERP
(on 30 Nov 2021)
Cellular Use Rating
In Model Organisms
Good in vitro tool, but limited delivery methods as in vivo tool.
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