Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T82383 | Target Info | |||
| Target Name | Tyrosine-protein kinase UFO (AXL) | ||||
| Synonyms |
UFO; Tyrosine-protein kinase receptor UFO; AXL oncogene
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| Target Type | Successful Target | ||||
| Gene Name | AXL | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Gilteritinib | Drug Info | IC50 = 0.29 nM | [1] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 2 (KDR) | Successful Target | ||||
| UniProt ID | VGFR2_HUMAN | |||||
| Gene Name | KDR | |||||
| Synonyms |
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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| Representative Drug(s) | MGCD265 | Drug Info | IC50 = 1 nM | [2] | ||
| Co-Target Name | Proto-oncogene c-Met (MET) | Successful Target | ||||
| UniProt ID | MET_HUMAN | |||||
| Gene Name | MET | |||||
| Synonyms |
Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase
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| Representative Drug(s) | MGCD265 | Drug Info | IC50 = 1 nM | [2] | ||
| Co-Target Name | Smoothened homolog (SMO) | Successful Target | ||||
| UniProt ID | SMO_HUMAN | |||||
| Gene Name | SMO | |||||
| Synonyms |
Smo-D473H; SMOH; Protein Gx
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| Representative Drug(s) | MGCD265 | Drug Info | Ki = 41.7 nM | [3] | ||
| Co-Target Name | Aurora kinase A (AURKA) | Clinical trial Target | ||||
| UniProt ID | AURKA_HUMAN | |||||
| Gene Name | AURKA | |||||
| Synonyms |
hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
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| Representative Drug(s) | TP-0903 | Drug Info | IC50 = 3 nM | [4] | ||
| Co-Target Name | Aurora kinase B (AURKB) | Clinical trial Target | ||||
| UniProt ID | AURKB_HUMAN | |||||
| Gene Name | AURKB | |||||
| Synonyms |
Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
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| Representative Drug(s) | TP-0903 | Drug Info | IC50 = 12.4 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608. | ||||
| REF 3 | Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-58. | ||||
| REF 4 | Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912. | ||||
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