Target family: Janus kinase (JakA) family (type: enzyme)
Target: tyrosine kinase 2

Ligand: zotiraciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.
Published in: Leukemia

Ligand: zemprocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Patent): Tricyclic janus kinase 1 inhibitors, and compositions and methods thereof

Ligand: zasocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Tyk2 inhibitors and uses thereof

Ligand: upadacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2019)
Primary target: no
Median affinity: 5.329999923706055 pIC50
Reference (Patent): Jak1 selective inhibitor and uses thereof

Ligand: TYK2 inhibitor 18 [WO2023227946] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Patent): Tyk2 inhibitors and uses thereof

Ligand: TYK2 inhibitor 14l (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery of 3-(4-(2-((1 H-Indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1 H-pyrazol-1-yl)propanenitrile Derivatives as Selective TYK2 Inhibitors for the Treatment of Inflammatory Bowel Disease
Published in: Journal of Medicinal Chemistry

Ligand: tofacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2017)
Primary target: no
Median affinity: 6.309999942779541 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: solcitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pIC50
Reference (Patent): Novel compound useful for the treatment of degenerative and inflammatory diseases

Ligand: SJ988497 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.270000457763672 pKd
Reference (Journal): Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia.
Published in: Blood

Ligand: SAR-20347 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.
Published in: Biochim Biophys Acta

Ligand: SAR-20347 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.220000267028809 pIC50

Ligand: ruxolitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 9.260000228881836 pIC50
Reference (Journal): Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Published in: J Med Chem

Ligand: ruxolitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: ropsacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Published in: J Med Chem

Ligand: PF-956980 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Monomeric Targeted Protein Degraders.
Published in: J Med Chem

Ligand: PF-06263276 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.53000020980835 pIC50
Reference (Journal): Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Published in: J Med Chem

Ligand: peficitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019)
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model.
Published in: J Pharmacol Sci

Ligand: oclacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pIC50
Reference (Patent): Pyrrolo[2,3-d]pyrimidine compounds

Ligand: nezulcitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Patent): DIMETHYL AMINO AZETIDINE AMIDES AS JAK INHIBITORS

Ligand: momelotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023), Japan (2024)
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Momelotinib inhibits ACVR1/ALK2, decreases hepcidin production, and ameliorates anemia of chronic disease in rodents.
Published in: Blood

Ligand: lorpucitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.130000114440918 pIC50
Reference (Patent): Small molecule inhibitors of the JAK family of kinases

Ligand: LASW1393 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.
Published in: J Med Chem

Ligand: JAK inhibitor I (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: JAK inhibitor 20a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
Published in: J Med Chem

Ligand: JAK inhibitor 17b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
Published in: J Med Chem

Ligand: JAK3 inhibitor 34 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Published in: J Med Chem

Ligand: JAK3 inhibitor 32 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Published in: J Med Chem

Ligand: izencitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Patent): Naphthyridine compounds as jak kinase inhibitors

Ligand: ilginatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms.
Published in: Blood Cancer J

Ligand: golidocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.550000190734863 pIC50
Reference (Journal): Discovery of (2<i>R</i>)-<i>N</i>-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1<i>H</i>-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Published in: J Med Chem

Ligand: GDC-0214 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Published in: Sci Transl Med

Ligand: filgotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2020)
Primary target: no
Median affinity: 6.940000057220459 pIC50
Reference (Journal): Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Published in: J Immunol

Ligand: filgotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2020)
Primary target: no
Median affinity: 5.590000152587891 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: fedratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
Published in: Bioorg Med Chem Lett

Ligand: deucravacitinib (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022), EMA (2023)
Primary target: yes
Median affinity: 10.699999809265137 pKi
Reference (Journal): Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Published in: J Med Chem

Ligand: deucravacitinib (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022), EMA (2023)
Primary target: yes
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Published in: J Med Chem

Ligand: delgocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020)
Primary target: no
Median affinity: 7.849999904632568 pKi
Reference (Journal): Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo.
Published in: Inflamm Res

Ligand: delgocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020)
Primary target: no
Median affinity: 7.239999771118164 pIC50
Reference (Journal): Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
Published in: J Med Chem

Ligand: compound 6 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem

Ligand: compound 30 [PMID: 37057760] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.110000133514404 pIC50
Reference (Journal): Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
Published in: J Med Chem

Ligand: compound 29 [Moslin et al., 2017] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Identification of imidazo[1,2-<i>b</i>]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Published in: Medchemcomm

Ligand: compound 25ap [PMID: 37796543] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Published in: J Med Chem

Ligand: compound 13 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem

Ligand: compound 13ac [PMID: 33256400] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pIC50
Reference (Journal): <i>N</i>-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
Published in: J Med Chem

Ligand: cerdulatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer.
Published in: J Pharmacol Exp Ther

Ligand: CEE321 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Published in: J Med Chem

Ligand: brepocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).
Published in: J Med Chem

Ligand: BMS-986202 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.699999809265137 pKi
Reference (Journal): Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Published in: J Med Chem

Ligand: BMS-986202 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.720000267028809 pIC50
Reference (Journal): Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Published in: J Med Chem

Ligand: BMS-911543 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.179999828338623 pIC50
Reference (Journal): Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.
Published in: Leukemia

Ligand: baricitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2017), FDA (2018)
Primary target: no
Median affinity: 7.210000038146973 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem