Page last updated: 2024-08-07 15:36:15

RAF proto-oncogene serine/threonine-protein kinase

A RAF proto-oncogene serine/threonine-protein kinase that is encoded in the genome of human. [PMID:20703093, PRO:KER]

Synonyms

EC 2.7.11.1;
Proto-oncogene c-RAF;
cRaf;
Raf-1

Research

Bioassay Publications (71)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (2.82)18.2507
2000's27 (38.03)29.6817
2010's35 (49.30)24.3611
2020's7 (9.86)2.80

Compounds (107)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
pd 98059Homo sapiens (human)IC502.800011
3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-oneHomo sapiens (human)IC500.077011
sb 239063Homo sapiens (human)IC5025.025022
zm 336372Homo sapiens (human)IC503.448255
staurosporineHomo sapiens (human)IC502.102555
birb 796Homo sapiens (human)IC501.266733
sb 203580Homo sapiens (human)IC500.757544
sorafenibHomo sapiens (human)IC500.13332932
sorafenibHomo sapiens (human)Ki0.006011
7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazineHomo sapiens (human)IC50100.000011
s 1033Homo sapiens (human)IC501.100011
Src Inhibitor-1Homo sapiens (human)IC50100.000011
u 0126Homo sapiens (human)IC500.290011
dasatinibHomo sapiens (human)IC500.164011
aldisineHomo sapiens (human)IC502.500011
su 11248Homo sapiens (human)IC5010.000011
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-oneHomo sapiens (human)IC5010.000011
gw-5074Homo sapiens (human)IC500.007844
oroidinHomo sapiens (human)IC502.500011
gw2974Homo sapiens (human)IC5049.000011
pd 184352Homo sapiens (human)IC500.012011
sb 242235Homo sapiens (human)IC500.050011
osi 930Homo sapiens (human)IC500.041011
3,5-bis(2-fluorobenzylidene)piperidin-4-oneHomo sapiens (human)IC5024.000011
npi 2358Homo sapiens (human)IC508.900010
l-779,450Homo sapiens (human)IC500.001411
regorafenibHomo sapiens (human)IC500.002022
chir-265Homo sapiens (human)IC500.609522
az-628Homo sapiens (human)IC500.380011
GDC-0879Homo sapiens (human)Ki0.000511
4-(4-(3-adamantan-1-ylureido)cyclohexyloxy)benzoic acidHomo sapiens (human)IC5010.000011
ro5126766Homo sapiens (human)IC500.056022
nvp-bhg712Homo sapiens (human)IC500.395010
t-tucbHomo sapiens (human)IC5010.000011
plx 4720Homo sapiens (human)IC500.006511
plx 4720Homo sapiens (human)Ki0.003311
thiouredopyrenetrisulfonateHomo sapiens (human)IC5010.000011
plx4032Homo sapiens (human)IC503.454766
dabrafenibHomo sapiens (human)IC500.150011
tak-632Homo sapiens (human)IC500.015655
cep-32496Homo sapiens (human)IC500.146011
ly3009120Homo sapiens (human)IC500.023044
ly3009120Homo sapiens (human)Ki0.000122
hymenialdisineHomo sapiens (human)IC500.006011
sb-590885Homo sapiens (human)Ki0.001722
debromohymenialdisineHomo sapiens (human)IC500.881011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
sb 202190Homo sapiens (human)Kd1.900011
imatinibHomo sapiens (human)Kd1.700022
staurosporineHomo sapiens (human)Kd10.000022
gefitinibHomo sapiens (human)Kd10.000022
lestaurtinibHomo sapiens (human)Kd10.000022
vatalanibHomo sapiens (human)Kd10.000022
ruboxistaurinHomo sapiens (human)Kd10.000022
canertinibHomo sapiens (human)Kd10.000022
birb 796Homo sapiens (human)Kd10.000022
cyc 202Homo sapiens (human)Kd10.000011
sb 203580Homo sapiens (human)Kd0.980022
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd10.000022
lapatinibHomo sapiens (human)Kd10.000022
sorafenibHomo sapiens (human)Kd0.230033
pd 173955Homo sapiens (human)Kd0.023011
s 1033Homo sapiens (human)Kd3.900011
bms 387032Homo sapiens (human)Kd10.000022
tandutinibHomo sapiens (human)Kd10.000033
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd0.570022
zd 6474Homo sapiens (human)Kd10.000022
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd10.000022
bosutinibHomo sapiens (human)Kd10.000011
su 11248Homo sapiens (human)Kd10.000033
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd10.000022
ekb 569Homo sapiens (human)Kd10.000011
axitinibHomo sapiens (human)Kd10.000011
pd 184352Homo sapiens (human)Kd10.000011
bms345541Homo sapiens (human)Kd10.000011
midostaurinHomo sapiens (human)Kd10.000033
ki 20227Homo sapiens (human)Kd10.000011
cp 724714Homo sapiens (human)Kd10.000011
pi103Homo sapiens (human)Kd3.700022
hki 272Homo sapiens (human)Kd10.000011
tofacitinibHomo sapiens (human)Kd10.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd10.000011
masitinibHomo sapiens (human)Kd10.000011
pazopanibHomo sapiens (human)Kd0.900022
azd 6244Homo sapiens (human)Kd10.000011
su 14813Homo sapiens (human)Kd10.000022
bibw 2992Homo sapiens (human)Kd10.000011
tg100-115Homo sapiens (human)Kd10.000011
pha 665752Homo sapiens (human)Kd10.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd0.840011
brivanibHomo sapiens (human)Kd10.000011
at 7519Homo sapiens (human)Kd10.000011
bi 2536Homo sapiens (human)Kd10.000011
nvp-ast487Homo sapiens (human)Kd0.930022
kw 2449Homo sapiens (human)Kd10.000011
abt 869Homo sapiens (human)Kd10.000022
gw 2580Homo sapiens (human)Kd10.000022
crizotinibHomo sapiens (human)Kd10.000011
chir-265Homo sapiens (human)Kd0.390022
motesanibHomo sapiens (human)Kd0.880022
mln8054Homo sapiens (human)Kd10.000022
GDC-0879Homo sapiens (human)Kd0.006611
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd10.000022
nvp-tae684Homo sapiens (human)Kd10.000011
fedratinibHomo sapiens (human)Kd10.000011
gsk690693Homo sapiens (human)Kd10.000011
gdc 0941Homo sapiens (human)Kd10.000011
plx 4720Homo sapiens (human)Kd0.170011
sgx 523Homo sapiens (human)Kd10.000011
quizartinibHomo sapiens (human)Kd10.000022
incb-018424Homo sapiens (human)Kd10.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
plx4032Homo sapiens (human)EC500.601011
gsk 1363089Homo sapiens (human)Kd4.400011
cep-32496Homo sapiens (human)Kd0.039022
chir 258Homo sapiens (human)Kd10.000022
nintedanibHomo sapiens (human)Kd10.000011
pp242Homo sapiens (human)Kd10.000011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
plx4032Homo sapiens (human)INH0.048011
dabrafenibHomo sapiens (human)INH0.006011

Enables

This protein enables 9 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
protein serine/threonine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
enzyme bindingmolecular functionBinding to an enzyme, a protein with catalytic activity. [GOC:jl]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
metal ion bindingmolecular functionBinding to a metal ion. [GOC:ai]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
MAP kinase kinase kinase activitymolecular functionCatalysis of the phosphorylation and activation of a MAP kinase kinase; each MAP kinase kinase can be phosphorylated by any of several MAP kinase kinase kinases. [PMID:9561267]

Located In

This protein is located in 7 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
mitochondrial outer membranecellular componentThe outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai]
Golgi apparatuscellular componentA membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
pseudopodiumcellular componentA temporary protrusion or retractile process of a cell, associated with flowing movements of the protoplasm, and serving for locomotion and feeding. [ISBN:0198506732]

Active In

This protein is active in 2 target(s):

TargetCategoryDefinition
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
mitochondrioncellular componentA semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732]

Involved In

This protein is involved in 34 target(s):

TargetCategoryDefinition
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
signal transductionbiological processThe cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11]
activation of adenylate cyclase activitybiological processAny process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai]
negative regulation of cell population proliferationbiological processAny process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators]
insulin receptor signaling pathwaybiological processThe series of molecular signals generated as a consequence of the insulin receptor binding to insulin. [GOC:ceb]
extrinsic apoptotic signaling pathway via death domain receptorsbiological processThe series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with a ligand binding to a death domain receptor on the cell surface, and ends when the execution phase of apoptosis is triggered. [GOC:mah, GOC:mtg_apoptosis]
Schwann cell developmentbiological processThe process aimed at the progression of a Schwann cell over time, from initial commitment of the cell to a specific fate, to the fully functional differentiated cell. Schwann cells are found in the peripheral nervous system, where they insulate neurons and axons, and regulate the environment in which neurons function. [GOC:dgh, GOC:ef]
thyroid gland developmentbiological processThe process whose specific outcome is the progression of the thyroid gland over time, from its formation to the mature structure. The thyroid gland is an endoderm-derived gland that produces thyroid hormone. [GOC:dgh]
negative regulation of protein-containing complex assemblybiological processAny process that stops, prevents, or reduces the frequency, rate or extent of protein complex assembly. [GOC:mah]
positive regulation of peptidyl-serine phosphorylationbiological processAny process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah]
somatic stem cell population maintenancebiological processAny process by which an organism retains a population of somatic stem cells, undifferentiated cells in the embryo or adult which can undergo unlimited division and give rise to cell types of the body other than those of the germ-line. [GOC:bf, ISBN:0582227089]
regulation of Rho protein signal transductionbiological processAny process that modulates the frequency, rate or extent of Rho protein signal transduction. [GOC:bf]
insulin secretion involved in cellular response to glucose stimulusbiological processThe regulated release of proinsulin from secretory granules (B granules) in the B cells of the pancreas; accompanied by cleavage of proinsulin to form mature insulin, in response to a glucose stimulus. [GOC:bf, GOC:yaf, PMID:8492079]
response to muscle stretchbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a myofibril being extended beyond its slack length. [GOC:BHF, GOC:vk, PMID:14583192]
ERBB2-ERBB3 signaling pathwaybiological processThe series of molecular signals initiated by binding of a ligand to a ERBB3 receptor on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and ERBB3. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB3. ERBB3 also has impaired kinase activity and relies on ERBB2 for activation and signal transmission. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589]
wound healingbiological processThe series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788]
myelinationbiological processThe process in which myelin sheaths are formed and maintained around neurons. Oligodendrocytes in the brain and spinal cord and Schwann cells in the peripheral nervous system wrap axons with compact layers of their plasma membrane. Adjacent myelin segments are separated by a non-myelinated stretch of axon called a node of Ranvier. [GOC:dgh, GOC:mah]
regulation of apoptotic processbiological processAny process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
negative regulation of apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of a cysteine-type endopeptidase activity involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of MAPK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators]
type B pancreatic cell proliferationbiological processThe multiplication or reproduction of pancreatic B cells, resulting in the expansion of an pancreatic B cell population. Pancreatic B cell are cells of the pancreas that secrete insulin. [GOC:jl, GOC:yaf]
intermediate filament cytoskeleton organizationbiological processA process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising intermediate filaments and their associated proteins. [GOC:ai]
regulation of cell differentiationbiological processAny process that modulates the frequency, rate or extent of cell differentiation, the process in which relatively unspecialized cells acquire specialized structural and functional features. [GOC:go_curators]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
insulin-like growth factor receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb]
neurotrophin TRK receptor signaling pathwaybiological processThe series of molecular signals initiated by neurotrophin binding to its receptor on the surface of a target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:ceb, GOC:jc, GOC:signaling, PMID:12065629, Wikipedia:Trk_receptor]
thymus developmentbiological processThe process whose specific outcome is the progression of the thymus over time, from its formation to the mature structure. The thymus is a symmetric bi-lobed organ involved primarily in the differentiation of immature to mature T cells, with unique vascular, nervous, epithelial, and lymphoid cell components. [GOC:add, ISBN:0781735149]
face developmentbiological processThe biological process whose specific outcome is the progression of a face from an initial condition to its mature state. The face is the ventral division of the head. [GOC:dph]
type II interferon-mediated signaling pathwaybiological processThe series of molecular signals initiated by interferon-gamma binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. Interferon gamma is the only member of the type II interferon found so far. [GOC:add, GOC:dph, GOC:signaling, PMID:28901902]
death-inducing signaling complex assemblybiological processA process of protein complex assembly in which the arrangement and bonding together of the set of components that form the protein complex is mediated by a death domain (DD) interaction, as part of the extrinsic apoptotic signaling pathway. [GOC:amm, GOC:mtg_apoptosis, InterPro:IPR000488]
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsbiological processAny process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway via death domain receptors. [GOC:TermGenie, PMID:17245429]
regulation of cell motilitybiological processAny process that modulates the frequency, rate or extent of cell motility. [GOC:mah]
MAPK cascadebiological processAn intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267]