Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T99089 | Target Info | |||
| Target Name | Serine/threonine-protein kinase B-raf (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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| Target Type | Successful Target | ||||
| Gene Name | BRAF | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | CEP-32496 | Drug Info | Ki = 187.8 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) | Vemurafenib | Drug Info | IC50 = 360 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) | Vemurafenib | Drug Info | IC50 = 48 nM | Click to Show More | [3] | |
| 2 | Dabrafenib | Drug Info | IC50 = 150 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) | Vemurafenib | Drug Info | IC50 = 23 nM | [4] | ||
| Co-Target Name | Receptor-interacting serine/threonine-protein kinase 3 (RIPK3) | Co-Target | ||||
| UniProt ID | RIPK3_HUMAN | |||||
| Gene Name | RIPK3 | |||||
| Synonyms |
RIP-like protein kinase 3; Receptor-interacting protein 3; RIP-3
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| Representative Drug(s) | Dabrafenib | Drug Info | IC50 = 2 nM | [5] | ||
| 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) | Vemurafenib | Drug Info | IC50 = 2.1 nM | Click to Show More | [6] | |
| 2 | Dabrafenib | Drug Info | IC50 = 26 nM | [2] | ||
| Co-Target Name | Serine/threonine-protein kinase RIPK2 (RIPK2) | Co-Target | ||||
| UniProt ID | RIPK2_HUMAN | |||||
| Gene Name | RIPK2 | |||||
| Synonyms |
Receptor-interacting serine/threonine-protein kinase 2; CARD-containing interleukin-1 beta-converting enzyme-associated kinase; CARD-containing IL-1 beta ICE-kinase; RIP-like-interacting CLARP kinase; Receptor-interacting protein 2; RIP-2; Tyrosine-protein kinase RIPK2
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| Representative Drug(s) | Dabrafenib | Drug Info | IC50 = 77 nM | [5] | ||
| References | Top | ||||
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| REF 1 | 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 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 | Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41. | ||||
| REF 4 | Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-alpha Motif Kinase (ZAK) Inhibitors. J Med Chem. 2017 Jul 13;60(13):5927-32. | ||||
| REF 5 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. J Med Chem. 2020 Feb 27;63(4):1490-1510. | ||||
| REF 6 | Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. Eur J Med Chem. 2019 Feb 1;163:243-255. | ||||
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