Target family: Other PIKK family kinases (type: enzyme)
Target: protein kinase, DNA-activated, catalytic subunit

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family.
Published in: Bioorg Med Chem Lett

Ligand: torin 2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Published in: J Med Chem

Ligand: PP121 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Published in: Nat Chem Biol

Ligand: PIK-75 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.
Published in: Cell

Ligand: PI-103 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.
Published in: Mol Cancer Ther

Ligand: peposertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Patent): Arylquinazolines

Ligand: NU-7441 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
Published in: Bioorg Med Chem Lett

Ligand: NU-7026 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.639999866485596 pIC50
Reference (Journal): 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).
Published in: Bioorg Med Chem Lett

Ligand: lartesertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.21999979019165 pIC50
Reference (Patent): Imidazolonylquinoline compounds and therapeutic uses thereof

Ligand: KU-0060648 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.
Published in: J Med Chem

Ligand: DNA-PK inhibitor V (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.570000171661377 pIC50
Reference (Journal): Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.
Published in: J Biol Chem

Ligand: DNA-PK inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family.
Published in: Bioorg Med Chem Lett

Ligand: compound 82 [PMID: 21332118] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
Published in: J Med Chem

Ligand: BAY-8400 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.090000152587891 pIC50
Reference (Journal): BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Published in: J Med Chem

Ligand: AZD7648 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.039999961853027 pIC50
Reference (Journal): The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-<i>a</i>]pyridin-6-yl)amino]-9-(tetrahydro-2<i>H</i>-pyran-4-yl)-7,9-dihydro-8<i>H</i>-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.
Published in: J Med Chem

Ligand: AZD7648 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.199999809265137 pIC50
Reference (Journal): The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-<i>a</i>]pyridin-6-yl)amino]-9-(tetrahydro-2<i>H</i>-pyran-4-yl)-7,9-dihydro-8<i>H</i>-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.
Published in: J Med Chem