Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62460 | Target Info | |||
| Target Name | Janus kinase 1 (JAK-1) | ||||
| Synonyms |
Tyrosine-protein kinase JAK1; JAK1B; JAK1A
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| Target Type | Successful Target | ||||
| Gene Name | JAK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Janus kinase 2 (JAK-2) | Successful Target | ||||
| UniProt ID | JAK2_HUMAN | |||||
| Gene Name | JAK2 | |||||
| Synonyms |
Tyrosine-protein kinase JAK2
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| Representative Drug(s) | Ruxolitinib | Drug Info | IC50 = 0.056 nM | Click to Show More | [1] | |
| 2 | Baricitinib | Drug Info | IC50 = 0.8 nM | [3] | ||
| 3 | ASP-015K | Drug Info | IC50 = 5 nM | [2] | ||
| 4 | Cerdulatinib | Drug Info | IC50 = 6 nM | [5] | ||
| 5 | Upadacitinib | Drug Info | IC50 = 8 nM | [6] | ||
| 6 | GLPG-0634 | Drug Info | IC50 = 25 nM | [2] | ||
| Co-Target Name | Janus kinase 3 (JAK-3) | Successful Target | ||||
| UniProt ID | JAK3_HUMAN | |||||
| Gene Name | JAK3 | |||||
| Synonyms |
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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| Representative Drug(s) | ASP-015K | Drug Info | IC50 = 0.71 nM | Click to Show More | [2] | |
| 2 | Ruxolitinib | Drug Info | IC50 = 2.8 nM | [4] | ||
| 3 | Cerdulatinib | Drug Info | IC50 = 8 nM | [5] | ||
| 4 | Baricitinib | Drug Info | IC50 = 25 nM | [3] | ||
| 5 | GLPG-0634 | Drug Info | IC50 = 810 nM | [8] | ||
| Co-Target Name | Fms-like tyrosine kinase 3 (FLT-3) | Successful Target | ||||
| UniProt ID | FLT3_HUMAN | |||||
| Gene Name | FLT3 | |||||
| Synonyms |
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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| Representative Drug(s) | GLPG-0634 | Drug Info | IC50 = 338 nM | [7] | ||
| Co-Target Name | TYK2 tyrosine kinase (TYK2) | Successful Target | ||||
| UniProt ID | TYK2_HUMAN | |||||
| Gene Name | TYK2 | |||||
| Synonyms |
Non-receptor tyrosine-protein kinase TYK2
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| Representative Drug(s) | Ruxolitinib | Drug Info | IC50 = 0.4 nM | Click to Show More | [9] | |
| 2 | ASP-015K | Drug Info | IC50 = 4.8 nM | [2] | ||
| 3 | Baricitinib | Drug Info | IC50 = 8.7 nM | [3] | ||
| 4 | GLPG-0634 | Drug Info | IC50 = 116 nM | [2] | ||
| Co-Target Name | Histone deacetylase 6 (HDAC6) | Clinical trial Target | ||||
| UniProt ID | HDAC6_HUMAN | |||||
| Gene Name | HDAC6 | |||||
| Synonyms |
KIAA0901; JM21; HD6
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| Representative Drug(s) | Ruxolitinib | Drug Info | IC50 = 15 nM | [10] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 3 (FLT-4) | Clinical trial Target | ||||
| UniProt ID | VGFR3_HUMAN | |||||
| Gene Name | FLT4 | |||||
| Synonyms |
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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| Representative Drug(s) | GLPG-0634 | Drug Info | IC50 = 274 nM | [7] | ||
| Co-Target Name | Macrophage colony-stimulating factor 1 receptor (CSF1R) | Clinical trial Target | ||||
| UniProt ID | CSF1R_HUMAN | |||||
| Gene Name | CSF1R | |||||
| Synonyms |
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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| Representative Drug(s) | GLPG-0634 | Drug Info | IC50 = 489 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. J Med Chem. 2017 Oct 26;60(20):8336-57. | ||||
| REF 2 | Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. J Med Chem. 2015 Sep 24;58(18):7596-602. | ||||
| REF 3 | Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors. J Med Chem. 2016 Jan 28;59(2):733-49. | ||||
| REF 4 | Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors. Bioorg Med Chem Lett. 2016 Apr 1;26(7):1803-8. | ||||
| REF 5 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. J Med Chem. 2018 Nov 21;61(22):9811-40. | ||||
| REF 6 | Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances. J Med Chem. 2018 Oct 25;61(20):9030-9058. | ||||
| REF 7 | Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem. 2014 Nov 26;57(22):9323-42. | ||||
| REF 8 | Design, synthesis and evaluation of ( R)-3-(7-(methyl(7 H-pyrrolo[2,3- d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor. Medchemcomm. 2018 Jan 15;9(3):477-489. | ||||
| REF 9 | Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1116-21. | ||||
| REF 10 | Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. J Med Chem. 2019 Apr 25;62(8):3898-3923. | ||||
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