Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: transforming growth factor beta receptor 1

Ligand: compound 15b [PMID: 16539403] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Published in: J Med Chem

Ligand: galunisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.25 pIC50

Ligand: galunisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.760000228881836 pIC50
Reference (Journal): Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Published in: Oncotarget

Ligand: H. polygyrus TGF-β mimic (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.460000038146973 pKd
Reference (Journal): A structurally distinct TGF-β mimic from an intestinal helminth parasite potently induces regulatory T cells.
Published in: Nat Commun

Ligand: LY2109761 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.420000076293945 pKi
Reference (Journal): LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis.
Published in: Mol Cancer Ther

Ligand: SB-431542 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.03000020980835 pIC50
Reference (Journal): Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
Published in: J Med Chem

Ligand: SD-208 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.28000020980835 pIC50
Reference (Journal): Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: TGF-beta RI inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.269999980926514 pIC50
Reference (Journal): Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.
Published in: Eur J Med Chem

Ligand: TGF-beta RI kinase inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.570000171661377 pIC50
Reference (Journal): Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Published in: J Med Chem

Ligand: vactosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.
Published in: J Med Chem

Ligand: zilurgisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Patent): Aminopyridine derivatives and their use as selective alk-2 inhibitors

Ligand: LDN-214117 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Published in: J Med Chem