Target family: Leucine-rich repeat kinase (LRRK) family (type: enzyme)
Target: leucine rich repeat kinase 2

Ligand: BOS172722 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N<sup>2</sup>-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N<sup>8</sup>-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
Published in: J Med Chem

Ligand: compound 20 [PMID: 30998356] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy.
Published in: J Med Chem

Ligand: DCLK1-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.159999847412109 pIC50
Reference (Journal): Discovery of a selective inhibitor of doublecortin like kinase 1.
Published in: Nat Chem Biol

Ligand: EB-42486 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pIC50
Reference (Journal): Selective Inhibitors of G2019S-LRRK2 Kinase Activity.
Published in: J Med Chem

Ligand: EB-42486 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.96999979019165 pIC50
Reference (Journal): Selective Inhibitors of G2019S-LRRK2 Kinase Activity.
Published in: J Med Chem

Ligand: GNE-0877 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 pKi
Reference (Journal): Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Published in: J Med Chem

Ligand: GNE-7915 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Published in: J Med Chem

Ligand: GNE-7915 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9 pKi
Reference (Journal): Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Published in: J Med Chem

Ligand: GNE-9605 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Published in: J Med Chem

Ligand: GSK2646264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Published in: Bioorg Med Chem Lett

Ligand: HG-10-102-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pKi
Reference (Journal): Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.
Published in: J Med Chem

Ligand: HG-10-102-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.610000133514404 pIC50
Reference (Journal): Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2)
Published in: chemrxiv

Ligand: HG-10-102-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.909999847412109 pIC50
Reference (Journal): Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2)
Published in: chemrxiv

Ligand: JAK3 inhibitor VI (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50

Ligand: JH-XII-03-02 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Development of a highly potent and selective degrader of LRRK2.
Published in: Bioorg Med Chem Lett

Ligand: LRRK2-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pKi
Reference (Journal): The development of CNS-active LRRK2 inhibitors using property-directed optimisation.
Published in: Bioorg Med Chem Lett

Ligand: LRRK2-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
Published in: Nat Chem Biol

Ligand: MLI-2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.1899995803833 pIC50
Reference (Journal): Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Published in: J Med Chem

Ligand: NIK inhibitor 12f (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.019999980926514 pIC50
Reference (Journal): Identification of <i>N</i>-Phenyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine Derivatives as Novel, Potent, and Selective NF-κB Inducing Kinase (NIK) Inhibitors for the Treatment of Psoriasis.
Published in: J Med Chem

Ligand: NIK SMI1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.610000133514404 pKi
Reference (Journal): NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Published in: Nat Commun

Ligand: PF-06447475 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor.
Published in: J Med Chem

Ligand: PF-06454589 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor.
Published in: J Med Chem

Ligand: TTT-3002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Kinase inhibitors arrest neurodegeneration in cell and C. elegans models of LRRK2 toxicity.
Published in: Hum Mol Genet

Ligand: URMC-099 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Published in: J Med Chem

Ligand: XL01126 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: XMD-12 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.
Published in: ACS Chem Biol