Target family: Receptor interacting protein kinase (RIPK) family (type: enzyme)
Target: receptor interacting serine/threonine kinase 1

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.320000171661377 pKd
Reference (Journal): Identification of the Raf kinase inhibitor TAK-632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3.
Published in: Br J Pharmacol

Ligand: SZM679 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pKd
Reference (Journal): Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.
Published in: J Med Chem

Ligand: SZM594 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pKd
Reference (Journal): Identification of the Raf kinase inhibitor TAK-632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3.
Published in: Br J Pharmacol

Ligand: SIR1-365 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): RIP1 Inhibitors

Ligand: RIPK3 inhibitor 42 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKd
Reference (Journal): <i>N</i>-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[<i>d</i>]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships, and in Vivo Efficacy.
Published in: J Med Chem

Ligand: RIPK3 inhibitor 18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.260000228881836 pIC50
Reference (Journal): Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
Published in: ACS Med Chem Lett

Ligand: RIPK1 inhibitor 22b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.
Published in: J Med Chem

Ligand: RIPK1 inhibitor 22b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.359999656677246 pKd
Reference (Journal): Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.
Published in: J Med Chem

Ligand: RIPA-56 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.
Published in: J Med Chem

Ligand: ponatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1.
Published in: Cell Rep

Ligand: PN10 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.050000190734863 pIC50
Reference (Journal): Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1.
Published in: Cell Rep

Ligand: oditrasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Kinase inhibitors and uses thereof

Ligand: necrostatin-1s (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.429999828338623 pKd
Reference (Journal): Phosphoinositide-3-OH kinase-dependent regulation of glycogen synthase kinase 3 and protein kinase B/AKT by the integrin-linked kinase.
Published in: Proc Natl Acad Sci USA

Ligand: necrostatin-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.309999942779541 pIC50
Reference (Journal): Identification of RIP1 kinase as a specific cellular target of necrostatins.
Published in: Nat Chem Biol

Ligand: GSK963 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase.
Published in: Cell Death Discov

Ligand: GSK'547 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Heterocyclic amides as kinase inhibitors for use in the treatment cancer

Ligand: GSK3145095 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Published in: ACS Med Chem Lett

Ligand: GSK3145095 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Published in: ACS Med Chem Lett

Ligand: GSK2982772 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Published in: J Med Chem

Ligand: GNE684 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.159999847412109 pKi
Reference (Journal): RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Published in: Cell Death Differ

Ligand: GNE684 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pKi
Reference (Journal): RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Published in: Cell Death Differ

Ligand: GNE684 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pKi
Reference (Journal): RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Published in: Cell Death Differ

Ligand: flizasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pKi
Reference (Patent): Bicyclic compounds for use as rip1 kinase inhibitors

Ligand: eclitasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Compounds, compositions and methods

Ligand: compound 27 [PMID: 24900635] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Published in: ACS Med Chem Lett

Ligand: compound 21 [PMID: 24900635] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Published in: ACS Med Chem Lett

Ligand: 6E11 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.400000095367432 pKd
Reference (Journal): 6E11, a highly selective inhibitor of Receptor-Interacting Protein Kinase 1, protects cells against cold hypoxia-reoxygenation injury.
Published in: Sci Rep