Target family: Dyrk1 subfamily (type: enzyme)
Target: dual specificity tyrosine phosphorylation regulated kinase 1A

Ligand: cirtuvivint (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Methods of treating cartilage disorders through inhibition of clk and dyrk

Ligand: compound 17 [PMID: 23642479] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
Published in: Bioorg Med Chem Lett

Ligand: compound 2-2c [PMID: 32003560] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.
Published in: J Med Chem

Ligand: compound 3b [PMID: 23454515] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.550000190734863 pIC50
Reference (Journal): Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
Published in: Eur J Med Chem

Ligand: compound 68 [PMID: 24900699] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.800000190734863 pIC50
Reference (Journal): Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease.
Published in: ACS Med Chem Lett

Ligand: compound 72 [WO2013026806] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.65999984741211 pIC50
Reference (Patent): Dyrk1 inhibitors and uses thereof.

Ligand: epigallocatechin-3-gallate (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.480000019073486 pIC50
Reference (Journal): DYRK1A Protein, A Promising Therapeutic Target to Improve Cognitive Deficits in Down Syndrome.
Published in: Brain Sci

Ligand: GNF2133 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 pIC50
Reference (Journal): Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Published in: J Med Chem

Ligand: GNF4877 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Inhibition of DYRK1A and GSK3B induces human β-cell proliferation.
Published in: Nat Commun

Ligand: harmine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation.
Published in: FEBS J

Ligand: KH-CB19 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pIC50
Reference (Journal): Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Published in: Chem Biol

Ligand: leucettine L41 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 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: lorecivivint (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.570000171661377 pIC50
Reference (Journal): A small-molecule inhibitor of the Wnt pathway (SM04690) as a potential disease modifying agent for the treatment of osteoarthritis of the knee.
Published in: Osteoarthr Cartil

Ligand: ML315 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
Published in: Bioorg Med Chem Lett

Ligand: (S)-CR8 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.
Published in: J Med Chem