Target family: Type II RTKs: Insulin receptor family (type: catalytic_receptor)
Target: Insulin-like growth factor I receptor

Ligand: AG 1024 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 4.739999771118164 pIC50
Reference (Journal): Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins.
Published in: Endocrinology

Ligand: AZD3463 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Webpage): AZD3463.

Ligand: BMS-536924 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Published in: J Med Chem

Ligand: BMS-754807 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Published in: J Med Chem

Ligand: brigatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 7.610000133514404 pIC50
Reference (Journal): Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Published in: J Med Chem

Ligand: ceritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014), EMA (2015)
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Published in: J Med Chem

Ligand: compound 19a [PMID: 30503936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.679999828338623 pIC50
Reference (Journal): Discovery of N<sup>1</sup>-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N<sup>3</sup>-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment.
Published in: Eur J Med Chem

Ligand: fexagratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pIC50
Reference (Webpage): AZD4547.

Ligand: GSK1511931 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.
Published in: Bioorg Med Chem Lett

Ligand: GSK-1838705A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers.
Published in: Mol Cancer Ther

Ligand: insulin-like growth factor 1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2005)
Primary target: no
Median affinity:  -

Ligand: GSK-1838705A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: insulin-like growth factor 2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: istiratumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors.
Published in: Mol Cancer Ther

Ligand: linsitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor.
Published in: Future Med Chem

Ligand: NVP-AEW541 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.399999618530273 pIC50
Reference (Journal): In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.
Published in: Cancer Cell

Ligand: NVP-TAE 226 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo.
Published in: Mol Cancer Ther

Ligand: picropodophyllin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth.
Published in: Cancer Res

Ligand: PQ401 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6 pIC50
Reference (Journal): Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth.
Published in: Mol Cancer Ther

Ligand: teprotumumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity: 12.15999984741211 pKd
Reference (Patent): Antibodies against insulin-like growth factor i receptor and uses thereof

Ligand: teprotumumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity: 9.25 pKd
Reference (Patent): Antibodies against insulin-like growth factor i receptor and uses thereof