Target family: Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family (type: catalytic_receptor)
Target: ALK receptor tyrosine kinase

Ligand: alectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2017), Japan (unknown)
Primary target: yes
Median affinity: 8.720000267028809 pIC50
Reference (Journal): Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Published in: Bioorg Med Chem

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

Ligand: belizatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.4399995803833 pKd
Reference (Journal): The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
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: yes
Median affinity:  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: brigatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: yes
Median affinity: 10.050000190734863 pKi
Reference (Journal): Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.
Published in: Proc Natl Acad Sci USA

Ligand: brigatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.
Published in: Proc Natl Acad Sci USA

Ligand: CEP-37440 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pIC50
Reference (Journal): Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
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: yes
Median affinity: 9.699999809265137 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 15 [PMID: 24900237] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
Published in: ACS Med Chem Lett

Ligand: compound 17 [PMID: 34176264] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.869999885559082 pIC50
Reference (Journal): Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK).
Published in: J Med Chem

Ligand: compound 25b [PMID: 22564207] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.720000267028809 pIC50
Reference (Journal): Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Published in: J Med Chem

Ligand: compound 5g [PMID: 20483621] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Published in: Bioorg Med Chem

Ligand: compound 5m [PMID: 20483621] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Published in: Bioorg Med Chem

Ligand: compound 5n [PMID: 20483621] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Published in: Bioorg Med Chem

Ligand: compound 8e [PMID: 24432909] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Published in: J Med Chem