Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T08391 | Target Info | |||
| Target Name | Janus kinase 2 (JAK-2) | ||||
| Synonyms |
Tyrosine-protein kinase JAK2
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| Target Type | Successful Target | ||||
| Gene Name | JAK2 | ||||
| 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) | Drug Info | Ki = 0.09 nM | Click to Show More | [1] | ||
| 2 | Drug Info | IC50 = 0.99 nM | [2] | |||
| 3 | Momelotinib | Drug Info | IC50 = 11 nM | [8] | ||
| 4 | Cerdulatinib | Drug Info | IC50 = 12 nM | [7] | ||
| 5 | BMS-911543 | Drug Info | IC50 = 75 nM | [12] | ||
| 6 | Fedratinib | Drug Info | IC50 = 100 nM | [13] | ||
| Co-Target Name | Histone deacetylase 1 (HDAC1) | Successful Target | ||||
| UniProt ID | HDAC1_HUMAN | |||||
| Gene Name | HDAC1 | |||||
| Synonyms |
RPD3L1; HD1
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 2 nM | [3] | ||
| 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 | Click to Show More | [4] | ||
| 2 | Cerdulatinib | Drug Info | IC50 = 8 nM | [7] | ||
| 3 | Drug Info | IC50 = 25 nM | [2] | |||
| 4 | Momelotinib | Drug Info | IC50 = 155 nM | [8] | ||
| 5 | BMS-911543 | Drug Info | IC50 = 360 nM | [12] | ||
| 6 | Pacritinib | Drug Info | IC50 = 520 nM | [6] | ||
| 7 | Fedratinib | Drug Info | IC50 = 1000 nM | [13] | ||
| Co-Target Name | Tropomyosin-related kinase A (TrkA) | Successful Target | ||||
| UniProt ID | NTRK1_HUMAN | |||||
| Gene Name | NTRK1 | |||||
| Synonyms |
gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
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| Representative Drug(s) | AZD1480 | Drug Info | IC50 = 3 nM | [5] | ||
| 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) | Pacritinib | Drug Info | IC50 = 6 nM | Click to Show More | [6] | |
| 2 | Fedratinib | Drug Info | IC50 = 15 nM | [9] | ||
| 3 | Pacritinib | Drug Info | IC50 = 23 nM | [10] | ||
| 4 | SB-1578 | Drug Info | IC50 = 60 nM | [11] | ||
| Co-Target Name | Signal transducer and activator of transcription 3 (STAT3) | Successful Target | ||||
| UniProt ID | STAT3_HUMAN | |||||
| Gene Name | STAT3 | |||||
| Synonyms |
Acute-phase response factor; APRF
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| Representative Drug(s) | AZD1480 | Drug Info | IC50 = 23 nM | [5] | ||
| Co-Target Name | Proto-oncogene c-Ret (RET) | Successful Target | ||||
| UniProt ID | RET_HUMAN | |||||
| Gene Name | RET | |||||
| Synonyms |
RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret
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| Representative Drug(s) | Fedratinib | Drug Info | IC50 = 48 nM | [9] | ||
| 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 | Click to Show More | [14] | ||
| 2 | Drug Info | IC50 = 8.7 nM | [2] | |||
| 3 | Pacritinib | Drug Info | IC50 = 50 nM | [6] | ||
| 4 | BMS-911543 | Drug Info | IC50 = 66 nM | [12] | ||
| 5 | Fedratinib | Drug Info | IC50 = 150 nM | [13] | ||
| 6 | SB-1578 | Drug Info | IC50 = 230 nM | [11] | ||
| Co-Target Name | Histone deacetylase 2 (HDAC2) | Clinical trial Target | ||||
| UniProt ID | HDAC2_HUMAN | |||||
| Gene Name | HDAC2 | |||||
| Synonyms |
HD2
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 3 nM | [3] | ||
| Co-Target Name | Histone deacetylase 3 (HDAC3) | Clinical trial Target | ||||
| UniProt ID | HDAC3_HUMAN | |||||
| Gene Name | HDAC3 | |||||
| Synonyms |
SMAP45; RPD32; RPD3-2; HD3
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 3 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) | ITF2357 | Drug Info | Ki = 4.2 nM | Click to Show More | [15] | |
| 2 | Drug Info | IC50 = 15 nM | [16] | |||
| Co-Target Name | Cyclin-dependent kinase 9 (CDK9) | Clinical trial Target | ||||
| UniProt ID | CDK9_HUMAN | |||||
| Gene Name | CDK9 | |||||
| Synonyms |
Tat-associated kinase complex catalytic subunit; TAK; Similar to cyclin-dependent kinase 9; Serine/threonine-protein kinase PITALRE; Cyclin-dependent protein kinase Cdk9; Cell division protein kinase 9; Cell division cycle 2-like protein kinase 4; CDC2L4; CDC2-related kinase; C-2K
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| Representative Drug(s) | SB-1578 | Drug Info | IC50 = 36 nM | [11] | ||
| 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) | SB-1578 | Drug Info | IC50 = 69 nM | [11] | ||
| Co-Target Name | Bromodomain-containing protein 4 (BRD4) | Clinical trial Target | ||||
| UniProt ID | BRD4_HUMAN | |||||
| Gene Name | BRD4 | |||||
| Synonyms |
Protein HUNK1; HUNK1
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| Representative Drug(s) | Fedratinib | Drug Info | IC50 = 290 nM | [9] | ||
| Co-Target Name | Bromodomain testis-specific protein (BRDT) | Clinical trial Target | ||||
| UniProt ID | BRDT_HUMAN | |||||
| Gene Name | BRDT | |||||
| Synonyms |
Cancer/testis antigen 9; CT9
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| Representative Drug(s) | Fedratinib | Drug Info | IC50 = 340 nM | [9] | ||
| Co-Target Name | Histone deacetylase 8 (HDAC8) | Patented-recorded Target | ||||
| UniProt ID | HDAC8_HUMAN | |||||
| Gene Name | HDAC8 | |||||
| Synonyms |
Histone deacetylase-8; HDACL1; HD8; CDA07
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 39 nM | [3] | ||
| Co-Target Name | Histone deacetylase 7 (HDAC7) | Patented-recorded Target | ||||
| UniProt ID | HDAC7_HUMAN | |||||
| Gene Name | HDAC7 | |||||
| Synonyms |
Histone deacetylase 7A; HDAC7A; HD7a; HD7
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 240 nM | [15] | ||
| Co-Target Name | Histone deacetylase 9 (HDAC9) | Patented-recorded Target | ||||
| UniProt ID | HDAC9_HUMAN | |||||
| Gene Name | HDAC9 | |||||
| Synonyms |
MITR; MEF2-interacting transcription repressor MITR; KIAA0744; Histone deacetylase-related protein; Histone deacetylase 7B; HDRP; HDAC7B; HDAC7; HD9; HD7b
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 390 nM | [3] | ||
| Co-Target Name | Histone deacetylase 5 (HDAC5) | Patented-recorded Target | ||||
| UniProt ID | HDAC5_HUMAN | |||||
| Gene Name | HDAC5 | |||||
| Synonyms |
KIAA0600; HD5; Antigen NY-CO-9
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| Representative Drug(s) | ITF2357 | Drug Info | Ki = 600 nM | [15] | ||
| Co-Target Name | Signal transducer and activator of transcription 5A (STAT5A) | Co-Target | ||||
| UniProt ID | STA5A_HUMAN | |||||
| Gene Name | STAT5A | |||||
| Representative Drug(s) | AZD1480 | Drug Info | IC50 = 25 nM | [5] | ||
| Co-Target Name | Cytochrome P450 1A2 (CYP1A2) | Co-Target | ||||
| UniProt ID | CP1A2_HUMAN | |||||
| Gene Name | CYP1A2 | |||||
| Synonyms |
Cholesterol 25-hydroxylase; Hydroperoxy icosatetraenoate dehydratase; CYPIA2; Cytochrome P(3)450; Cytochrome P450 4; Cytochrome P450-P3
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| Representative Drug(s) | BMS-911543 | Drug Info | IC50 = 1000 nM | [12] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 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 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 3 | Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243. | ||||
| 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 | Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. J Med Chem. 2011 Jan 13;54(1):262-76. | ||||
| REF 6 | 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. J Med Chem. 2011 Jul 14;54(13):4638-58. | ||||
| REF 7 | Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. J Med Chem. 2018 Nov 21;61(22):9811-40. | ||||
| REF 8 | Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. | ||||
| REF 9 | Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40. | ||||
| REF 10 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. Eur J Med Chem. 2019 Sep 15;178:468-483. | ||||
| REF 11 | Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthritis. J Med Chem. 2012 Mar 22;55(6):2623-40. | ||||
| REF 12 | Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. | ||||
| REF 13 | Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7454-7. | ||||
| REF 14 | Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1116-21. | ||||
| REF 15 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). Bioorg Med Chem. 2015 Aug 15;23(16):5151-5. | ||||
| REF 16 | 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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