Target family: PIM family (type: enzyme)
Target: Pim-1 proto-oncogene, serine/threonine kinase

Ligand: compound 20 [PMID: 22136433] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pIC50
Reference (Journal): 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Published in: J Med Chem

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: compound 2 [PMID: 22560567] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.480000019073486 pIC50
Reference (Journal): Discovery of XL413, a potent and selective CDC7 inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: CX-5011 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pIC50
Reference (Journal): Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.
Published in: Biochemistry

Ligand: CX-5279 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.070000171661377 pIC50
Reference (Journal): Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.
Published in: Biochemistry

Ligand: CX-6258 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 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: 10.520000457763672 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: leucettine L41 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 pIC50
Reference (Journal): Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Published in: J Med Chem

Ligand: LGB321 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 12 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: 8.300000190734863 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: 11.220000267028809 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: 6.699999809265137 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: AZD1208 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.770000457763672 pKi
Reference (Journal): Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Published in: ACS Med Chem Lett

Ligand: Akt inhibitor X (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pIC50
Reference (Journal): More than just a GPCR ligand: structure-based discovery of thioridazine derivatives as Pim-1 kinase inhibitors.
Published in: Medchemcomm

Ligand: XL413 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.380000114440918 pIC50
Reference (Journal): Discovery of XL413, a potent and selective CDC7 inhibitor.
Published in: Bioorg Med Chem Lett