Target family: PAKA subfamily (type: enzyme)
Target: p21 (RAC1) activated kinase 1

Ligand: compound 4 [PMID: 24432870] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Published in: ACS Med Chem Lett

Ligand: BJG-05-039 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 pIC50
Reference (Journal): Development and Utility of a PAK1-Selective Degrader.
Published in: J Med Chem

Ligand: compound 1 [PMID: 20005102] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Published in: Bioorg Med Chem Lett

Ligand: compound 3 [PMID: 26191365] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pKd
Reference (Journal): Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Published in: ACS Med Chem Lett

Ligand: compound 4 [PMID: 24432870] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Published in: J Med Chem

Ligand: FRAX486 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.079999923706055 pIC50
Reference (Journal): Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486.
Published in: Proc Natl Acad Sci USA

Ligand: FRAX597 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.
Published in: J Biol Chem

Ligand: Il-94 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.429999828338623 pKi
Reference (Journal): PAK1: A Therapeutic Target for Cancer Treatment.
Published in: ACS Med Chem Lett

Ligand: IPA-3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.599999904632568 pIC50
Reference (Journal): An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase.
Published in: Chem Biol

Ligand: PF-3758309 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Published in: J Med Chem

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm