ATP-competitive inhibitor of PAK1, PAK2, PAK3
Protein target names: PAK1, PAK2, PAK3
Mechanism of action: ATP-competitive inhibitor
In Vitro Validations
Uniprot ID: Q13153
Target Class: Protein kinase
Target SubClass: STE
Potency Value: 3.7 nM
Potency Assay: Measuring the phosphorylation of a FRET peptide substrate (Ser/Thr19) labeled with Coumarin and Fluorescein
PDB ID for probe-target interaction (3D structure): 5DEY
Structure-activity relationship: SAR described in "Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety, ACS Med. Chem. Lett. 2015, 6, 1241" and Chemically diverse Group I PAK inhibitors impart acute cardiovascular toxicity with a narrow therapeutic window, J. Med. Chem. 2016, 59, 5520. SAR assay used is described above.
Serine/threonine-protein kinase PAK 1, PAK1, PAK1_ ...
In Cell Validations
In Vivo Data
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