GSK256066

Inhibitor of PDE4B

Structure

Information

  • PDE4B
  • Inhibitor
  • 0.1-10 nM
  • Reviewer recommended concentration: Cellular activity range includes 0.01 nM, solubility may be limiting at higher concentrations

In Vitro Validations

Uniprot ID: Q07343
Target Class: Nucleic acid metabolism
Target SubClass: Phosphodiesterase
Potency: IC50
Potency Value: 0.079 nM
Potency Assay: Scintillation Proximity Assay (SPA)
PDB ID for probe-target interaction (3D structure): 3GWT
Structure-activity relationship: yes
Target aliases:
cAMP-specific 3',5'-cyclic phosphodiesterase 4B, P ...

DOI Reference: 10.1016/j.bmcl.2009.04.012

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

>1000-fold selective versus PDEs 1–3 and 5–7

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Good in vitro tool, but limited delivery methods as in vivo tool.

(last updated: 30 Nov 2021 )