Target family: Interleukin-1 receptor-associated kinase (IRAK) family (type: enzyme)
Target: interleukin 1 receptor associated kinase 4

Ligand: BAY1830839 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of IRAK4 Inhibitors <b>BAY1834845</b> (Zabedosertib) and <b>BAY1830839</b>.
Published in: J Med Chem

Ligand: BIO-7488 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pIC50
Reference (Journal): The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-<i>N</i>-(6-methylpyrazolo[1,5-<i>a</i>]pyrimidin-3-yl)imidazo[1,2-<i>a</i>]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
Published in: J Med Chem

Ligand: BIO-8169 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Discovery of BIO-8169&#x2500;A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
Published in: J Med Chem

Ligand: compound 1 [WO2012007375] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Patent): Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators.

Ligand: compound 7 [WO2012007375] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Patent): Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators.

Ligand: edecesertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Pyrrolo[1,2-b] pyridazine derivatives

Ligand: emavusertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.
Published in: ACS Med Chem Lett

Ligand: GLPG2534 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.1899995803833 pIC50
Reference (Journal): IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases.
Published in: Sci Transl Med

Ligand: GLPG2534 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Journal): IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases.
Published in: Sci Transl Med

Ligand: ND-2158 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pKi
Reference (Journal): Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders.
Published in: J Med Chem

Ligand: PF-06426779 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Patent): Bicyclic-fused heteroaryl or aryl compounds and their use as IRAK4 inhibitors

Ligand: Takinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease.
Published in: Cell Chem Biol

Ligand: zabedosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Discovery of IRAK4 Inhibitors <b>BAY1834845</b> (Zabedosertib) and <b>BAY1830839</b>.
Published in: J Med Chem

Ligand: zabedosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.96999979019165 pIC50
Reference (Patent): New substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs

Ligand: zomiradomide (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Methods of treating mutant lymphomas

Ligand: IRAK-1/4 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Published in: Bioorg Med Chem Lett

Ligand: IRAK4 inhibitor 4b [PMID: 18474425] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): IRAK-4 inhibitors. Part 1: a series of amides.
Published in: Bioorg Med Chem Lett

Ligand: IRAK4 inhibitor rac-45 [PMID: 18501603] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines.
Published in: Bioorg Med Chem Lett

Ligand: ND-2110 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.119999885559082 pKi
Reference (Journal): Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders.
Published in: J Med Chem