Target family: PIM family (type: enzyme)
Target: Pim-2 proto-oncogene, serine/threonine kinase

Ligand: compound 28 [PMID: 30624936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.
Published in: J Med Chem

Ligand: CX-6258 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Published in: ACS Med Chem Lett

Ligand: dapolsertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Novel benzimidazole derivatives as kinase inhibitors

Ligand: GDC-0339 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Published in: J Med Chem

Ligand: LGB321 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 11.680000305175781 pKi
Reference (Journal): Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers.
Published in: Clin Cancer Res

Ligand: nuvisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pKi
Reference (Journal): A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas.
Published in: Neoplasia

Ligand: PIM447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.739999771118164 pKi
Reference (Journal): Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Published in: J Med Chem

Ligand: ruboxistaurin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: SGI-1776 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Published in: J Med Chem

Ligand: uzansertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.
Published in: PLoS ONE