Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T51883 | Target Info | |||
| Target Name | Serine/threonine-protein kinase Raf (RAF) | ||||
| Synonyms |
Proto-oncogene Raf
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| Target Type | Clinical trial Target | ||||
| Gene Name | ARAF; BRAF; RAF1 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Serine/threonine-protein kinase B-raf (BRAF) | Successful Target | ||||
| UniProt ID | BRAF_HUMAN | |||||
| Gene Name | BRAF | |||||
| Synonyms |
V-Raf murine sarcoma viral oncogene homolog B1; RAFB1; Proto-oncogene B-Raf; P94; BRAF1; BRAF(V599E); BRAF serine/threonine kinase; B-raf protein; B-Raf
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 1.5 nM | [1] | ||
| Co-Target Name | Fyn tyrosine protein kinase (FYN) | Successful Target | ||||
| UniProt ID | FYN_HUMAN | |||||
| Gene Name | FYN | |||||
| Synonyms |
Tyrosine-protein kinase Fyn; Src-like kinase; SLK; Proto-oncogene tyrosine-protein kinase Fyn; Proto-oncogene c-Fyn; Proto-oncogene Syn; Fyn p59-Fyn; Fyn Protooncogene Syn
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 91 nM | [2] | ||
| Co-Target Name | Proto-oncogene c-Src (SRC) | Successful Target | ||||
| UniProt ID | SRC_HUMAN | |||||
| Gene Name | SRC | |||||
| Synonyms |
pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 310 nM | [2] | ||
| Co-Target Name | Tyrosine-protein kinase ABL1 (ABL) | Successful Target | ||||
| UniProt ID | ABL1_HUMAN | |||||
| Gene Name | ABL1 | |||||
| Synonyms |
p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 380 nM | [2] | ||
| Co-Target Name | Proto-oncogene c-RAF (c-RAF) | Clinical trial Target | ||||
| UniProt ID | RAF1_HUMAN | |||||
| Gene Name | RAF1 | |||||
| Synonyms |
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 3.8 nM | Click to Show More | [1] | |
| 2 | RO-5126766 | Drug Info | IC50 = 56 nM | [3] | ||
| Co-Target Name | Ephrin type-A receptor 2 (EPHA2) | Clinical trial Target | ||||
| UniProt ID | EPHA2_HUMAN | |||||
| Gene Name | EPHA2 | |||||
| Synonyms |
Tyrosine-protein kinase receptor ECK; Epithelial cell kinase; EphA2receptor; ECK
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 20 nM | [2] | ||
| Co-Target Name | Stress-activated protein kinase (p38) | Clinical trial Target | ||||
| UniProt ID | MK11_HUMAN; MK12_HUMAN; MK13_HUMAN; MK14_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
p38) Stress-activated protein kinase; P38 MAPK; P38 MAP kinase; Mitogen-activated protein kinase p38
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 61 nM | [2] | ||
| Co-Target Name | MAPK/ERK kinase kinase 1 (MAP3K1) | Clinical trial Target | ||||
| UniProt ID | M3K1_HUMAN | |||||
| Gene Name | MAP3K1 | |||||
| Synonyms |
Mitogenactivated protein kinase kinase kinase 1; Mitogen-activated protein kinase kinase kinase 1; MEKK1; MEKK 1; MEKK; MEK kinase 1; MAPKKK1
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 98 nM | [2] | ||
| Co-Target Name | Ephrin type-B receptor 4 (EPHB4) | Clinical trial Target | ||||
| UniProt ID | EPHB4_HUMAN | |||||
| Gene Name | EPHB4 | |||||
| Synonyms |
Tyrosine-protein kinase TYRO11; TYRO11; MYK1; Hepatoma transmembrane kinase; HTK
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 100 nM | [2] | ||
| Co-Target Name | GTPase KRas (KRAS) | Clinical trial Target | ||||
| UniProt ID | RASK_HUMAN | |||||
| Gene Name | KRAS | |||||
| Synonyms |
c-Ki-ras; c-K-ras; RASK2; Ki-Ras; KRAS2; K-Ras 2
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 150 nM | [2] | ||
| Co-Target Name | ERK activator kinase 1 (MEK1) | Clinical trial Target | ||||
| UniProt ID | MP2K1_HUMAN | |||||
| Gene Name | MAP2K1 | |||||
| Synonyms |
PRKMK1; Mitogen-activated protein kinase kinase 1; MKK1; MEK 1; MAPKK 1; MAPK/ERKkinase 1; MAPK/ERK kinase 1; MAP kinase kinase 1; Dual specificity mitogen-activated protein kinase kinase 1
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| Representative Drug(s) | RO-5126766 | Drug Info | IC50 = 160 nM | [3] | ||
| Co-Target Name | Jun N terminal kinase (JNK) | Clinical trial Target | ||||
| UniProt ID | MK08_HUMAN; MK09_HUMAN; MK10_HUMAN | |||||
| Gene Name | MAPK8; MAPK9; MAPK10 | |||||
| Synonyms |
c-Jun N-terminal kinase; Stress-activated protein kinase JNK; SAPK1; PRKM; MAP kinase; JNK
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 470 nM | [2] | ||
| Co-Target Name | Tyrosine-protein kinase CSK (CSK) | Patented-recorded Target | ||||
| UniProt ID | CSK_HUMAN | |||||
| Gene Name | CSK | |||||
| Synonyms |
Protein-tyrosine kinase CYL; C-Src kinase
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 290 nM | [2] | ||
| Co-Target Name | IL-1 receptor-associated kinase 1 (IRAK1) | Patented-recorded Target | ||||
| UniProt ID | IRAK1_HUMAN | |||||
| Gene Name | IRAK1 | |||||
| Synonyms |
Interleukin-1 receptor-associated kinase 1; IRAK-1; IRAK
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 390 nM | [2] | ||
| Co-Target Name | MLK-related kinase (MLTK) | Literature-reported Target | ||||
| UniProt ID | M3K20_HUMAN | |||||
| Gene Name | MAP3K20 | |||||
| Synonyms |
ZAK; Sterile alpha motif- and leucine zipper-containing kinase AZK; Mixed lineage kinase-related kinase; Mitogen-activated protein kinase kinase kinase MLT; Mitogen-activated protein kinase kinase kinase 20; MRK; MLTK; MLK-like mitogen-activated protein triple kinase; Leucine zipper- and sterile alpha motif-containing kinase; Human cervical cancer suppressor gene 4 protein; HCCS4; HCCS-4
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 39 nM | [2] | ||
| Co-Target Name | Eukaryotic translation initiation factor 2-alpha kinase 4 (EIF2AK4) | Literature-reported Target | ||||
| UniProt ID | E2AK4_HUMAN | |||||
| Gene Name | EIF2AK4 | |||||
| Synonyms |
eIF-2-alpha kinase GCN2; KIAA1338; GCN2-like protein; GCN2
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 450 nM | [2] | ||
| Co-Target Name | ERK activator kinase 5 (MAP2K5) | Literature-reported Target | ||||
| UniProt ID | MP2K5_HUMAN | |||||
| Gene Name | MAP2K5 | |||||
| Synonyms |
PRKMK5; Mitogen-activatedprotein kinase kinase 5; MKK5; MEK5; MEK 5; MAPKK 5; MAPK/ERK kinase 5; MAP kinase kinase5; MAP kinase kinase 5; Dual specificity mitogen-activated protein kinase kinase 5
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 800 nM | [2] | ||
| Co-Target Name | Serine/threonine-protein kinase A-Raf (ARAF) | Co-Target | ||||
| UniProt ID | ARAF_HUMAN | |||||
| Gene Name | ARAF | |||||
| Synonyms |
Proto-oncogene A-Raf; Proto-oncogene A-Raf-1; Proto-oncogene Pks
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 1.2 nM | [1] | ||
| Co-Target Name | Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5) | Co-Target | ||||
| UniProt ID | M4K5_HUMAN | |||||
| Gene Name | MAP4K5 | |||||
| Synonyms |
Kinase homologous to SPS1/STE20; KHS; MAPK/ERK kinase kinase kinase 5; MEK kinase kinase 5; MEKKK 5
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| Representative Drug(s) | LY3009120 | Drug Info | IC50 = 970 nM | [2] | ||
| References | Top | ||||
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| REF 1 | Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. Eur J Med Chem. 2019 Feb 1;163:243-255. | ||||
| REF 2 | Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J Med Chem. 2015 May 28;58(10):4165-79. | ||||
| REF 3 | Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14. | ||||
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