Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T19760 | Target Info | |||
| Target Name | Mixed lineage kinase 1 (MAP3K9) | ||||
| Synonyms |
PRKE1; Mitogen-activated protein kinase kinase kinase 9; MLK1
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| Target Type | Clinical trial Target | ||||
| Gene Name | MAP3K9 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | CEP1347 | Drug Info | IC50 = 43 nM | [1] | ||
| 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) | CEP1347 | Drug Info | IC50 = 39 nM | [1] | ||
| Co-Target Name | Protein delta homolog 1 (DLK1) | Clinical trial Target | ||||
| UniProt ID | DLK1_HUMAN | |||||
| Gene Name | DLK1 | |||||
| Synonyms |
pG2; DLK-1
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| Representative Drug(s) | CEP1347 | Drug Info | IC50 = 114 nM | [2] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 1 (FLT-1) | Clinical trial Target | ||||
| UniProt ID | VGFR1_HUMAN | |||||
| Gene Name | FLT1 | |||||
| Synonyms |
Vascular permeability factor receptor; VEGFR1; VEGFR-1; VEGF-1 receptor; Tyrosine-protein kinase receptor FLT; Tyrosine-protein kinase FRT; Fms-like tyrosine kinase 1; FRT; FLT
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| Representative Drug(s) | CEP1347 | Drug Info | IC50 = 209 nM | [1] | ||
| Co-Target Name | Mixed lineage kinase 2 (MAP3K10) | Literature-reported Target | ||||
| UniProt ID | M3K10_HUMAN | |||||
| Gene Name | MAP3K10 | |||||
| Synonyms |
Protein kinase MST; Mitogen-activated protein kinase kinase kinase 10; MST; MLK2
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| Representative Drug(s) | CEP1347 | Drug Info | IC50 = 2 nM | [3] | ||
| Co-Target Name | Mixed lineage kinase 3 (MAP3K11) | Literature-reported Target | ||||
| UniProt ID | M3K11_HUMAN | |||||
| Gene Name | MAP3K11 | |||||
| Synonyms |
Src-homology 3 domain-containing proline-rich kinase; SPRK; SH3 domain-containing proline-rich kinase; Protein-tyrosine kinase PTK1; PTK1; Mixed-lineage protein kinase 3; Mitogen-activated protein kinase kinase kinase 11; MLK3
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| Representative Drug(s) | CEP1347 | Drug Info | IC50 = 6 nM | [3] | ||
| References | Top | ||||
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| REF 1 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9. | ||||
| REF 2 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-87. | ||||
| REF 3 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48. | ||||
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