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

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

Ligand: zotiraciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.
Published in: J Med Chem

Ligand: zemprocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Patent): Tricyclic janus kinase 1 inhibitors, and compositions and methods thereof

Ligand: XL019 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.65999984741211 pIC50
Reference (Journal): SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: WXFL10203614 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Janus kinase inhibitor

Ligand: upadacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2019)
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Patent): Jak1 selective inhibitor and uses thereof

Ligand: TYK2 inhibitor 14l (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 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: yes
Median affinity: 7.110000133514404 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: tinengotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pIC50
Reference (Patent): Multi-kinase inhibitor compound, and crystal form and use thereof

Ligand: solcitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 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: 9.470000267028809 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: no
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis.
Published in: J Immunol

Ligand: safimaltib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Bipyrazole derivatives as jak inhibitors

Ligand: ruxolitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: yes
Median affinity:  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: yes
Median affinity:  pIC50
Reference (Journal): Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.
Published in: Blood

Ligand: ruxolitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: rovadicitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Patent): Pyrrolopyrimidine compound

Ligand: ropsacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Published in: J Med Chem

Ligand: RGB-286638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Published in: Leukemia

Ligand: RG-1530 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.539999961853027 pKd
Reference (Journal): Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.
Published in: Cell Cycle

Ligand: repotrectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 8.979999542236328 pIC50
Reference (Journal): Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations.
Published in: Cancer Discov

Ligand: PF-956980 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 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: 7.639999866485596 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: pacritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022)
Primary target: yes
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
Published in: J Med Chem

Ligand: oclacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.760000228881836 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: 10.510000228881836 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: 8.850000381469727 pIC50
Reference (Journal): Momelotinib inhibits ACVR1/ALK2, decreases hepcidin production, and ameliorates anemia of chronic disease in rodents.
Published in: Blood

Ligand: momelotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023), Japan (2024)
Primary target: yes
Median affinity: 7.739999771118164 pIC50
Reference (Journal): CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Published in: Leukemia

Ligand: lorpucitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pIC50
Reference (Patent): Small molecule inhibitors of the JAK family of kinases

Ligand: londamocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.909999847412109 pIC50
Reference (Patent): Jak1 selective inhibitors

Ligand: LASW1393 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 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: JNJ-7706621 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.340000152587891 pKd
Reference (Journal): Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Published in: J Med Chem

Ligand: JNJ-7706621 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.96999979019165 pIC50
Reference (Journal): Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.
Published in: ACS Med Chem Lett

Ligand: JNJ-7706621 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.340000152587891 pKd
Reference (Journal): Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.
Published in: ACS Med Chem Lett

Ligand: JAK inhibitor I (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: JAK inhibitor 20a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.53000020980835 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: 8.449999809265137 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 II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): The specificity of JAK3 kinase inhibitors.
Published in: Blood

Ligand: JAK3 inhibitor 34 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.179999828338623 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: 5.519999980926514 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: yes
Median affinity: 10 pKi
Reference (Patent): Naphthyridine compounds as jak kinase inhibitors

Ligand: ivarmacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Patent): Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof

Ligand: itacnosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Patent): Jak2 and alk2 inhibitors and methods for their use

Ligand: itacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Piperidin-4-yl azetidine derivatives as jak1 inhibitors.

Ligand: ilginatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.140000343322754 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: HG-10-102-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.489999771118164 pKi
Reference (Journal): Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.
Published in: J Med Chem

Ligand: gusacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Patent): Pyrimido- pyridazinone compounds and use thereof

Ligand: GSK2646264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Published in: Bioorg Med Chem Lett

Ligand: golidocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.820000171661377 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: girocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): JAK1 selective inhibitors and uses thereof

Ligand: GDC-0214 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pKi
Reference (Journal): Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Published in: Sci Transl Med

Ligand: gandotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F.
Published in: Blood Cancer J

Ligand: filgotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2020)
Primary target: no
Median affinity: 5.619999885559082 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: filgotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2020)
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Published in: J Immunol

Ligand: fedratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.
Published in: Cancer Cell

Ligand: fedratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: yes
Median affinity: 8.520000457763672 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: emzeltrectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor

Ligand: deuruxolitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Patent): Treatment of hair loss disorders with deuterated jak inhibitors

Ligand: delgocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020)
Primary target: no
Median affinity: 8.770000457763672 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: yes
Median affinity: 8.59000015258789 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: decernotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: decernotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: compound 8l [PMID: 36053746] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Discovery of Novel Imidazo[4,5-<i>c</i>]quinoline Derivatives to Treat Inflammatory Bowel Disease (IBD) by Inhibiting Multiple Proinflammatory Signaling Pathways and Restoring Intestinal Homeostasis.
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: 8.079999923706055 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 25ap [PMID: 37796543] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.739999771118164 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 1d [PMID: 21493067] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 19a [PMID: 24359159] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.
Published in: J Med Chem

Ligand: compound 18e [PMID: 31670517] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.
Published in: J Med Chem

Ligand: compound 13 [PMID: 35653642] (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.170000076293945 pKd
Reference (Journal): Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
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: 8.520000457763672 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: compound 11 [PMID: 35653642] (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.46999979019165 pKd
Reference (Journal): Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Published in: J Med Chem

Ligand: compound 11 [PMID: 35653642] (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pKd
Reference (Journal): Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Published in: J Med Chem

Ligand: cerdulatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 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: CEP-33779 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pIC50
Reference (Journal): A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.
Published in: J Med Chem

Ligand: CEE321 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 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: 7.110000133514404 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-911543 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.
Published in: Leukemia

Ligand: BIIB068 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.340000152587891 pKd
Reference (Journal): Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Published in: J Med Chem

Ligand: baricitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2017), FDA (2018)
Primary target: yes
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Published in: J Med Chem

Ligand: baricitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2017), FDA (2018)
Primary target: yes
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
Published in: J Immunol

Ligand: AZD1480 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2.
Published in: J Biol Chem

Ligand: AZ960 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.350000381469727 pKi
Reference (Journal): Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2.
Published in: J Biol Chem

Ligand: AT-9283 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.920000076293945 pIC50
Reference (Journal): Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Published in: J Med Chem

Ligand: AC430 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Optically active pyrazolylaminoquinazoline, and pharmaceutical compositions and methods of use thereof

Ligand: abrocitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: UK, Japan & EMA (2021), FDA (2022)
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Published in: J Med Chem