Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T23172 | Target Info | |||
| Target Name | Janus kinase 3 (JAK-3) | ||||
| Synonyms |
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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| Target Type | Successful Target | ||||
| Gene Name | JAK3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Janus kinase 1 (JAK-1) | Successful Target | ||||
| UniProt ID | JAK1_HUMAN | |||||
| Gene Name | JAK1 | |||||
| Synonyms |
Tyrosine-protein kinase JAK1; JAK1B; JAK1A
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| Representative Drug(s) | Tofacitinib | Drug Info | IC50 = 0.5 nM | Click to Show More | [1] | |
| 2 | ASP-015K | Drug Info | IC50 = 3.9 nM | [3] | ||
| 3 | VX-509 | Drug Info | IC50 = 11 nM | [3] | ||
| 4 | Cerdulatinib | Drug Info | IC50 = 12 nM | [4] | ||
| 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) | Tofacitinib | Drug Info | IC50 = 0.5 nM | Click to Show More | [2] | |
| 2 | ASP-015K | Drug Info | IC50 = 5 nM | [3] | ||
| 3 | Cerdulatinib | Drug Info | IC50 = 6 nM | [4] | ||
| 4 | VX-509 | Drug Info | IC50 = 13 nM | [3] | ||
| Co-Target Name | Tyrosine-protein kinase BTK (ATK) | Successful Target | ||||
| UniProt ID | BTK_HUMAN | |||||
| Gene Name | BTK | |||||
| Synonyms |
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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| Representative Drug(s) | Ritlecitinib | Drug Info | IC50 = 607 nM | [5] | ||
| 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) | Tofacitinib | Drug Info | IC50 = 3.6 nM | Click to Show More | [6] | |
| 2 | ASP-015K | Drug Info | IC50 = 4.8 nM | [3] | ||
| 3 | VX-509 | Drug Info | IC50 = 11 nM | [3] | ||
| Co-Target Name | T-cell-specific kinase (ITK) | Clinical trial Target | ||||
| UniProt ID | ITK_HUMAN | |||||
| Gene Name | ITK | |||||
| Synonyms |
Tyrosine kinase ITK; Inducible T cell kinase; EMT
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| Representative Drug(s) | Ritlecitinib | Drug Info | Ki = 26.9 nM | [5] | ||
| Co-Target Name | Tyrosine-protein kinase BMX (BMX) | Patented-recorded Target | ||||
| UniProt ID | BMX_HUMAN | |||||
| Gene Name | BMX | |||||
| Synonyms |
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
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| Representative Drug(s) | Ritlecitinib | Drug Info | Ki = 545 nM | [5] | ||
| Co-Target Name | Tyrosine-protein kinase Tec (PSCTK4) | Patented-recorded Target | ||||
| UniProt ID | TEC_HUMAN | |||||
| Gene Name | TEC | |||||
| Synonyms |
Tec protein tyrosine kinase
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| Representative Drug(s) | Ritlecitinib | Drug Info | IC50 = 592 nM | [5] | ||
| Co-Target Name | Tyrosine-protein kinase TXK (TXK) | Literature-reported Target | ||||
| UniProt ID | TXK_HUMAN | |||||
| Gene Name | TXK | |||||
| Synonyms |
Resting lymphocyte kinase; RLK; Protein-tyrosine kinase 4; PTK4
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| Representative Drug(s) | Ritlecitinib | Drug Info | Ki = 131 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold. J Med Chem. 2018 Jun 28;61(12):5350-66. | ||||
| REF 2 | Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors. Bioorg Med Chem. 2019 Apr 15;27(8):1646-1657. | ||||
| REF 3 | Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. J Med Chem. 2015 Sep 24;58(18):7596-602. | ||||
| REF 4 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. J Med Chem. 2018 Nov 21;61(22):9811-40. | ||||
| REF 5 | Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. J Med Chem. 2017 Mar 9;60(5):1971-1993. | ||||
| REF 6 | Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group. Bioorg Med Chem. 2014 Feb 1;22(3):1156-62. | ||||
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