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Target Report Card

Target Name and Classification

Target ID CHEMBL1906
Target Type SINGLE PROTEIN
Preferred Name Serine/threonine-protein kinase RAF
Synonyms Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase | RAF | RAF1 | Raf-1 | cRaf
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tkl protein kinase group > tkl protein kinase raf family

Target Components

Component Description Relationship Accession
RAF proto-oncogene serine/threonine-protein kinase SINGLE PROTEIN P04049

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111351 Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) PROTEIN FAMILY
CHEMBL3883317 B-raf/RAF proto-oncogene serine/threonine-protein kinase PROTEIN FAMILY
CHEMBL3885566 Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase PROTEIN FAMILY
CHEMBL3559685 RAF serine/threonine protein kinase PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1200485 SORAFENIB TOSYLATE Serine/threonine-protein kinase RAF inhibitor 4 FDA
CHEMBL1946170 REGORAFENIB Serine/threonine-protein kinase RAF inhibitor 4 Expert
CHEMBL3545027 XL-281 Serine/threonine-protein kinase RAF inhibitor 2 Other Other PubMed PubMed
CHEMBL3545082 RG-7376 Serine/threonine-protein kinase RAF inhibitor 1 PubMed
CHEMBL3545195 LY-3009120 Serine/threonine-protein kinase RAF inhibitor 1 PubMed
CHEMBL3545263 LGX-806 Serine/threonine-protein kinase RAF inhibitor 1
CHEMBL3545296 ARQ-736 Serine/threonine-protein kinase RAF inhibitor 1 DOI Other PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000132155
Ensembl ENSG00000132155
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005741 (mitochondrial outer membrane)
GO:0005794 (Golgi apparatus)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0016607 (nuclear speck)
GO:0031143 (pseudopodium)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004709 (MAP kinase kinase kinase activity)
GO:0005057 (receptor signaling protein activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008179 (adenylate cyclase binding)
GO:0010856 (adenylate cyclase activator activity)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019899 (enzyme binding)
GO:0031267 (small GTPase binding)
GO:0031434 (mitogen-activated protein kinase kinase binding)
GO:0042802 (identical protein binding)
GO:0046872 (metal ion binding)
GO:0046982 (protein heterodimerization activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000186 (activation of MAPKK activity)
GO:0001666 (response to hypoxia)
GO:0001678 (cellular glucose homeostasis)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0002223 (stimulatory C-type lectin receptor signaling pathway)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0007165 (signal transduction)
GO:0007190 (activation of adenylate cyclase activity)
GO:0007275 (multicellular organism development)
GO:0007507 (heart development)
GO:0008283 (cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0009968 (negative regulation of signal transduction)
GO:0016310 (phosphorylation)
GO:0030154 (cell differentiation)
GO:0030168 (platelet activation)
GO:0030878 (thyroid gland development)
GO:0031333 (negative regulation of protein complex assembly)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0034220 (ion transmembrane transport)
GO:0035019 (somatic stem cell population maintenance)
GO:0035023 (regulation of Rho protein signal transduction)
GO:0035556 (intracellular signal transduction)
GO:0035773 (insulin secretion involved in cellular response to glucose stimulus)
GO:0035994 (response to muscle stretch)
GO:0042060 (wound healing)
GO:0042981 (regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043154 (negative regulation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0045104 (intermediate filament cytoskeleton organization)
GO:0045595 (regulation of cell differentiation)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048011 (neurotrophin TRK receptor signaling pathway)
GO:0048538 (thymus development)
GO:0060324 (face development)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071550 (death-inducing signaling complex assembly)
GO:1902042 (negative regulation of extrinsic apoptotic signaling pathway via death domain receptors)
GO:2000145 (regulation of cell motility)
Wikipedia C-Raf

Target Cross References - Protein

canSAR P04049
CGD LEOPARD syndrome 2; Noonan syndrome 5
Human Protein Atlas ENSG00000132155
IntAct P04049
Guide to Pharmacology 2184
Open Targets ENSG00000132155
PharmGKB PA34183
Pharos P04049 (Tclin)
Reactome R-HSA-2672351 (Stimuli-sensing channels.)
R-HSA-392517 (Rap1 signalling.)
R-HSA-430116 (GP1b-IX-V activation signalling.)
R-HSA-442742 (CREB phosphorylation through the activation of Ras.)
R-HSA-5621575 (CD209 (DC-SIGN) signaling.)
R-HSA-5673000 (RAF activation.)
R-HSA-5674135 (MAP2K and MAPK activation.)
R-HSA-5674499 (Negative feedback regulation of MAPK pathway.)
R-HSA-5675221 (Negative regulation of MAPK pathway.)
R-HSA-6802946 (Signaling by moderate kinase activity BRAF mutants.)
R-HSA-6802948 (Signaling by high-kinase activity BRAF mutants.)
R-HSA-6802949 (Signaling by RAS mutants.)
R-HSA-6802952 (Signaling by BRAF and RAF fusions.)
R-HSA-6802955 (Paradoxical activation of RAF signaling by kinase inactive BRAF.)
UniProt B0LPH8 B2R5N3 P04049 Q15278 Q9UC20

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR002219 (PE/DAG-bd.)
IPR003116 (RBD_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020454 (DAG/PE-bd.)
IPR029071 (Ubiquitin-like_domsf.)
Pfam PF00130 (C1_1)
PF02196 (RBD)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1C1Y 1GUA 3CU8 3IQJ 3IQU 3IQV 3KUC 3KUD 3NKX 3O8I 3OMV 4FJ3 4G0N 4G3X 4IEA 4IHL
CREDO 1C1Y 1GUA 3CU8 3IQJ 3IQU 3IQV 3KUC 3KUD 3NKX 3O8I 3OMV 4FJ3 4G0N 4G3X 4IEA 4IHL
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