Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T87554 | Target Info | |||
Target Name | HUMAN janus kinase 2 (JAK-2) | ||||
Synonyms |
Tyrosine-protein kinase JAK2
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Gene Name | JAK2 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Drug Info | Ki = 0.09 nM | [1] | |||
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) | Drug Info | IC50 = 2.8 nM | [2] | |||
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) | Drug Info | IC50 = 0.4 nM | [3] | |||
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) | Drug Info | IC50 = 15 nM | [4] | |||
Co-Target Name | Tyrosine protein kinase JAK1-Tyrosine protein kinase JAK3 complex (JAK1-JAK3) | Co-Target | ||||
UniProt ID | JAK3_HUMAN-JAK1_HUMAN | |||||
Gene Name | JAK1-JAK3 | |||||
Representative Drug(s) | Drug Info | IC50 = 23 nM | [5] |
References | Top | ||||
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REF 1 | Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. J Med Chem. 2012 Nov 26;55(22):10090-107. | ||||
REF 2 | 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 3 | Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1116-21. | ||||
REF 4 | 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. | ||||
REF 5 | Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome. Bioorg Med Chem Lett. 2013 May 1;23(9):2793-800. |
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