Target family: TTK family (type: enzyme)
Target: TTK protein kinase

Ligand: Ro3280 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.289999961853027 pKd
Reference (Journal): Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
Published in: Bioorg Med Chem Lett

Ligand: compound 34h [PMID: 27055065] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
Published in: J Med Chem

Ligand: compound 34h [PMID: 27055065] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Inhibitor compounds

Ligand: compound 27f [PMID: 25625617] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.550000190734863 pIC50
Reference (Journal): Discovery of imidazo[1,2-b]pyridazine derivatives: selective and orally available Mps1 (TTK) kinase inhibitors exhibiting remarkable antiproliferative activity.
Published in: J Med Chem

Ligand: compound 20 [PMID: 30998356] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 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: BOS172722 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.960000038146973 pKi
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: BOS172722 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 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: BAY1217389 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity.
Published in: Mol Cancer Ther

Ligand: AZ3146 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex.
Published in: J Cell Biol

Ligand: GNE-7915 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.28000020980835 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: luvixasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
Published in: ACS Med Chem Lett

Ligand: MPI-0479605 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pIC50
Reference (Journal): Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.
Published in: Mol Cancer Ther

Ligand: MPS1-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Published in: Nat Chem Biol

Ligand: NMS-P715 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.739999771118164 pIC50
Reference (Journal): Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: empesertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity.
Published in: Mol Cancer Ther