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SummaryStructural detailsExperimental detailsFunctional detailsSequence NeighborHistoryDownloads

9O0U

Crystal structure of CRAF/MEK1 complex with PLX4720 and CH5126766

Functional Information from GO Data
ChainGOidnamespacecontents
B0000165biological_processMAPK cascade
B0000166molecular_functionnucleotide binding
B0000187biological_processobsolete activation of MAPK activity
B0003056biological_processregulation of vascular associated smooth muscle contraction
B0004672molecular_functionprotein kinase activity
B0004674molecular_functionprotein serine/threonine kinase activity
B0004708molecular_functionMAP kinase kinase activity
B0004712molecular_functionprotein serine/threonine/tyrosine kinase activity
B0004713molecular_functionprotein tyrosine kinase activity
B0005078molecular_functionMAP-kinase scaffold activity
B0005515molecular_functionprotein binding
B0005524molecular_functionATP binding
B0005634cellular_componentnucleus
B0005737cellular_componentcytoplasm
B0005739cellular_componentmitochondrion
B0005769cellular_componentearly endosome
B0005770cellular_componentlate endosome
B0005783cellular_componentendoplasmic reticulum
B0005794cellular_componentGolgi apparatus
B0005813cellular_componentcentrosome
B0005829cellular_componentcytosol
B0005874cellular_componentmicrotubule
B0005886cellular_componentplasma membrane
B0005925cellular_componentfocal adhesion
B0005938cellular_componentcell cortex
B0006935biological_processchemotaxis
B0006979biological_processresponse to oxidative stress
B0007165biological_processsignal transduction
B0007528biological_processneuromuscular junction development
B0008285biological_processnegative regulation of cell population proliferation
B0010508biological_processpositive regulation of autophagy
B0010628biological_processpositive regulation of gene expression
B0010629biological_processnegative regulation of gene expression
B0014044biological_processSchwann cell development
B0014069cellular_componentpostsynaptic density
B0016020cellular_componentmembrane
B0016301molecular_functionkinase activity
B0016740molecular_functiontransferase activity
B0019901molecular_functionprotein kinase binding
B0030182biological_processneuron differentiation
B0030295molecular_functionprotein kinase activator activity
B0030335biological_processpositive regulation of cell migration
B0030424cellular_componentaxon
B0030425cellular_componentdendrite
B0031267molecular_functionsmall GTPase binding
B0031435molecular_functionmitogen-activated protein kinase kinase kinase binding
B0032402biological_processmelanosome transport
B0032839cellular_componentdendrite cytoplasm
B0032872biological_processregulation of stress-activated MAPK cascade
B0032968biological_processpositive regulation of transcription elongation by RNA polymerase II
B0034111biological_processnegative regulation of homotypic cell-cell adhesion
B0036064cellular_componentciliary basal body
B0038127biological_processERBB signaling pathway
B0038133biological_processERBB2-ERBB3 signaling pathway
B0042552biological_processmyelination
B0043204cellular_componentperikaryon
B0043410biological_processpositive regulation of MAPK cascade
B0043539molecular_functionprotein serine/threonine kinase activator activity
B0044877molecular_functionprotein-containing complex binding
B0045893biological_processpositive regulation of DNA-templated transcription
B0045933biological_processpositive regulation of muscle contraction
B0047496biological_processvesicle transport along microtubule
B0048009biological_processinsulin-like growth factor receptor signaling pathway
B0048313biological_processGolgi inheritance
B0048471cellular_componentperinuclear region of cytoplasm
B0048678biological_processresponse to axon injury
B0048812biological_processneuron projection morphogenesis
B0051384biological_processresponse to glucocorticoid
B0070328biological_processtriglyceride homeostasis
B0070371biological_processERK1 and ERK2 cascade
B0070372biological_processregulation of ERK1 and ERK2 cascade
B0070374biological_processpositive regulation of ERK1 and ERK2 cascade
B0071902biological_processpositive regulation of protein serine/threonine kinase activity
B0090170biological_processregulation of Golgi inheritance
B0090398biological_processcellular senescence
B0097110molecular_functionscaffold protein binding
B0098696biological_processregulation of neurotransmitter receptor localization to postsynaptic specialization membrane
B0098978cellular_componentglutamatergic synapse
B0106310molecular_functionprotein serine kinase activity
B1903298biological_processnegative regulation of hypoxia-induced intrinsic apoptotic signaling pathway
B2000641biological_processregulation of early endosome to late endosome transport
B2001171biological_processpositive regulation of ATP biosynthetic process
D0000165biological_processMAPK cascade
D0000166molecular_functionnucleotide binding
D0000187biological_processobsolete activation of MAPK activity
D0003056biological_processregulation of vascular associated smooth muscle contraction
D0004672molecular_functionprotein kinase activity
D0004674molecular_functionprotein serine/threonine kinase activity
D0004708molecular_functionMAP kinase kinase activity
D0004712molecular_functionprotein serine/threonine/tyrosine kinase activity
D0004713molecular_functionprotein tyrosine kinase activity
D0005078molecular_functionMAP-kinase scaffold activity
D0005515molecular_functionprotein binding
D0005524molecular_functionATP binding
D0005634cellular_componentnucleus
D0005737cellular_componentcytoplasm
D0005739cellular_componentmitochondrion
D0005769cellular_componentearly endosome
D0005770cellular_componentlate endosome
D0005783cellular_componentendoplasmic reticulum
D0005794cellular_componentGolgi apparatus
D0005813cellular_componentcentrosome
D0005829cellular_componentcytosol
D0005874cellular_componentmicrotubule
D0005886cellular_componentplasma membrane
D0005925cellular_componentfocal adhesion
D0005938cellular_componentcell cortex
D0006935biological_processchemotaxis
D0006979biological_processresponse to oxidative stress
D0007165biological_processsignal transduction
D0007528biological_processneuromuscular junction development
D0008285biological_processnegative regulation of cell population proliferation
D0010508biological_processpositive regulation of autophagy
D0010628biological_processpositive regulation of gene expression
D0010629biological_processnegative regulation of gene expression
D0014044biological_processSchwann cell development
D0014069cellular_componentpostsynaptic density
D0016020cellular_componentmembrane
D0016301molecular_functionkinase activity
D0016740molecular_functiontransferase activity
D0019901molecular_functionprotein kinase binding
D0030182biological_processneuron differentiation
D0030295molecular_functionprotein kinase activator activity
D0030335biological_processpositive regulation of cell migration
D0030424cellular_componentaxon
D0030425cellular_componentdendrite
D0031267molecular_functionsmall GTPase binding
D0031435molecular_functionmitogen-activated protein kinase kinase kinase binding
D0032402biological_processmelanosome transport
D0032839cellular_componentdendrite cytoplasm
D0032872biological_processregulation of stress-activated MAPK cascade
D0032968biological_processpositive regulation of transcription elongation by RNA polymerase II
D0034111biological_processnegative regulation of homotypic cell-cell adhesion
D0036064cellular_componentciliary basal body
D0038127biological_processERBB signaling pathway
D0038133biological_processERBB2-ERBB3 signaling pathway
D0042552biological_processmyelination
D0043204cellular_componentperikaryon
D0043410biological_processpositive regulation of MAPK cascade
D0043539molecular_functionprotein serine/threonine kinase activator activity
D0044877molecular_functionprotein-containing complex binding
D0045893biological_processpositive regulation of DNA-templated transcription
D0045933biological_processpositive regulation of muscle contraction
D0047496biological_processvesicle transport along microtubule
D0048009biological_processinsulin-like growth factor receptor signaling pathway
D0048313biological_processGolgi inheritance
D0048471cellular_componentperinuclear region of cytoplasm
D0048678biological_processresponse to axon injury
D0048812biological_processneuron projection morphogenesis
D0051384biological_processresponse to glucocorticoid
D0070328biological_processtriglyceride homeostasis
D0070371biological_processERK1 and ERK2 cascade
D0070372biological_processregulation of ERK1 and ERK2 cascade
D0070374biological_processpositive regulation of ERK1 and ERK2 cascade
D0071902biological_processpositive regulation of protein serine/threonine kinase activity
D0090170biological_processregulation of Golgi inheritance
D0090398biological_processcellular senescence
D0097110molecular_functionscaffold protein binding
D0098696biological_processregulation of neurotransmitter receptor localization to postsynaptic specialization membrane
D0098978cellular_componentglutamatergic synapse
D0106310molecular_functionprotein serine kinase activity
D1903298biological_processnegative regulation of hypoxia-induced intrinsic apoptotic signaling pathway
D2000641biological_processregulation of early endosome to late endosome transport
D2001171biological_processpositive regulation of ATP biosynthetic process
F0000165biological_processMAPK cascade
F0000166molecular_functionnucleotide binding
F0000187biological_processobsolete activation of MAPK activity
F0003056biological_processregulation of vascular associated smooth muscle contraction
F0004672molecular_functionprotein kinase activity
F0004674molecular_functionprotein serine/threonine kinase activity
F0004708molecular_functionMAP kinase kinase activity
F0004712molecular_functionprotein serine/threonine/tyrosine kinase activity
F0004713molecular_functionprotein tyrosine kinase activity
F0005078molecular_functionMAP-kinase scaffold activity
F0005515molecular_functionprotein binding
F0005524molecular_functionATP binding
F0005634cellular_componentnucleus
F0005737cellular_componentcytoplasm
F0005739cellular_componentmitochondrion
F0005769cellular_componentearly endosome
F0005770cellular_componentlate endosome
F0005783cellular_componentendoplasmic reticulum
F0005794cellular_componentGolgi apparatus
F0005813cellular_componentcentrosome
F0005829cellular_componentcytosol
F0005874cellular_componentmicrotubule
F0005886cellular_componentplasma membrane
F0005925cellular_componentfocal adhesion
F0005938cellular_componentcell cortex
F0006935biological_processchemotaxis
F0006979biological_processresponse to oxidative stress
F0007165biological_processsignal transduction
F0007528biological_processneuromuscular junction development
F0008285biological_processnegative regulation of cell population proliferation
F0010508biological_processpositive regulation of autophagy
F0010628biological_processpositive regulation of gene expression
F0010629biological_processnegative regulation of gene expression
F0014044biological_processSchwann cell development
F0014069cellular_componentpostsynaptic density
F0016020cellular_componentmembrane
F0016301molecular_functionkinase activity
F0016740molecular_functiontransferase activity
F0019901molecular_functionprotein kinase binding
F0030182biological_processneuron differentiation
F0030295molecular_functionprotein kinase activator activity
F0030335biological_processpositive regulation of cell migration
F0030424cellular_componentaxon
F0030425cellular_componentdendrite
F0031267molecular_functionsmall GTPase binding
F0031435molecular_functionmitogen-activated protein kinase kinase kinase binding
F0032402biological_processmelanosome transport
F0032839cellular_componentdendrite cytoplasm
F0032872biological_processregulation of stress-activated MAPK cascade
F0032968biological_processpositive regulation of transcription elongation by RNA polymerase II
F0034111biological_processnegative regulation of homotypic cell-cell adhesion
F0036064cellular_componentciliary basal body
F0038127biological_processERBB signaling pathway
F0038133biological_processERBB2-ERBB3 signaling pathway
F0042552biological_processmyelination
F0043204cellular_componentperikaryon
F0043410biological_processpositive regulation of MAPK cascade
F0043539molecular_functionprotein serine/threonine kinase activator activity
F0044877molecular_functionprotein-containing complex binding
F0045893biological_processpositive regulation of DNA-templated transcription
F0045933biological_processpositive regulation of muscle contraction
F0047496biological_processvesicle transport along microtubule
F0048009biological_processinsulin-like growth factor receptor signaling pathway
F0048313biological_processGolgi inheritance
F0048471cellular_componentperinuclear region of cytoplasm
F0048678biological_processresponse to axon injury
F0048812biological_processneuron projection morphogenesis
F0051384biological_processresponse to glucocorticoid
F0070328biological_processtriglyceride homeostasis
F0070371biological_processERK1 and ERK2 cascade
F0070372biological_processregulation of ERK1 and ERK2 cascade
F0070374biological_processpositive regulation of ERK1 and ERK2 cascade
F0071902biological_processpositive regulation of protein serine/threonine kinase activity
F0090170biological_processregulation of Golgi inheritance
F0090398biological_processcellular senescence
F0097110molecular_functionscaffold protein binding
F0098696biological_processregulation of neurotransmitter receptor localization to postsynaptic specialization membrane
F0098978cellular_componentglutamatergic synapse
F0106310molecular_functionprotein serine kinase activity
F1903298biological_processnegative regulation of hypoxia-induced intrinsic apoptotic signaling pathway
F2000641biological_processregulation of early endosome to late endosome transport
F2001171biological_processpositive regulation of ATP biosynthetic process
H0000165biological_processMAPK cascade
H0000166molecular_functionnucleotide binding
H0000187biological_processobsolete activation of MAPK activity
H0003056biological_processregulation of vascular associated smooth muscle contraction
H0004672molecular_functionprotein kinase activity
H0004674molecular_functionprotein serine/threonine kinase activity
H0004708molecular_functionMAP kinase kinase activity
H0004712molecular_functionprotein serine/threonine/tyrosine kinase activity
H0004713molecular_functionprotein tyrosine kinase activity
H0005078molecular_functionMAP-kinase scaffold activity
H0005515molecular_functionprotein binding
H0005524molecular_functionATP binding
H0005634cellular_componentnucleus
H0005737cellular_componentcytoplasm
H0005739cellular_componentmitochondrion
H0005769cellular_componentearly endosome
H0005770cellular_componentlate endosome
H0005783cellular_componentendoplasmic reticulum
H0005794cellular_componentGolgi apparatus
H0005813cellular_componentcentrosome
H0005829cellular_componentcytosol
H0005874cellular_componentmicrotubule
H0005886cellular_componentplasma membrane
H0005925cellular_componentfocal adhesion
H0005938cellular_componentcell cortex
H0006935biological_processchemotaxis
H0006979biological_processresponse to oxidative stress
H0007165biological_processsignal transduction
H0007528biological_processneuromuscular junction development
H0008285biological_processnegative regulation of cell population proliferation
H0010508biological_processpositive regulation of autophagy
H0010628biological_processpositive regulation of gene expression
H0010629biological_processnegative regulation of gene expression
H0014044biological_processSchwann cell development
H0014069cellular_componentpostsynaptic density
H0016020cellular_componentmembrane
H0016301molecular_functionkinase activity
H0016740molecular_functiontransferase activity
H0019901molecular_functionprotein kinase binding
H0030182biological_processneuron differentiation
H0030295molecular_functionprotein kinase activator activity
H0030335biological_processpositive regulation of cell migration
H0030424cellular_componentaxon
H0030425cellular_componentdendrite
H0031267molecular_functionsmall GTPase binding
H0031435molecular_functionmitogen-activated protein kinase kinase kinase binding
H0032402biological_processmelanosome transport
H0032839cellular_componentdendrite cytoplasm
H0032872biological_processregulation of stress-activated MAPK cascade
H0032968biological_processpositive regulation of transcription elongation by RNA polymerase II
H0034111biological_processnegative regulation of homotypic cell-cell adhesion
H0036064cellular_componentciliary basal body
H0038127biological_processERBB signaling pathway
H0038133biological_processERBB2-ERBB3 signaling pathway
H0042552biological_processmyelination
H0043204cellular_componentperikaryon
H0043410biological_processpositive regulation of MAPK cascade
H0043539molecular_functionprotein serine/threonine kinase activator activity
H0044877molecular_functionprotein-containing complex binding
H0045893biological_processpositive regulation of DNA-templated transcription
H0045933biological_processpositive regulation of muscle contraction
H0047496biological_processvesicle transport along microtubule
H0048009biological_processinsulin-like growth factor receptor signaling pathway
H0048313biological_processGolgi inheritance
H0048471cellular_componentperinuclear region of cytoplasm
H0048678biological_processresponse to axon injury
H0048812biological_processneuron projection morphogenesis
H0051384biological_processresponse to glucocorticoid
H0070328biological_processtriglyceride homeostasis
H0070371biological_processERK1 and ERK2 cascade
H0070372biological_processregulation of ERK1 and ERK2 cascade
H0070374biological_processpositive regulation of ERK1 and ERK2 cascade
H0071902biological_processpositive regulation of protein serine/threonine kinase activity
H0090170biological_processregulation of Golgi inheritance
H0090398biological_processcellular senescence
H0097110molecular_functionscaffold protein binding
H0098696biological_processregulation of neurotransmitter receptor localization to postsynaptic specialization membrane
H0098978cellular_componentglutamatergic synapse
H0106310molecular_functionprotein serine kinase activity
H1903298biological_processnegative regulation of hypoxia-induced intrinsic apoptotic signaling pathway
H2000641biological_processregulation of early endosome to late endosome transport
H2001171biological_processpositive regulation of ATP biosynthetic process
Functional Information from PROSITE/UniProt
site_idPS00107
Number of Residues21
DetailsPROTEIN_KINASE_ATP Protein kinases ATP-binding region signature. IGSGSFGTVYkGkwhgd.............VAVK
ChainResidueDetails
AILE355-LYS375
BLEU74-LYS97
site_idPS00108
Number of Residues13
DetailsPROTEIN_KINASE_ST Serine/Threonine protein kinases active-site signature. IiHrDMKsnNIFL
ChainResidueDetails
AILE464-LEU476
BILE186-VAL198
Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues4
DetailsActive site: {"description":"Proton acceptor"}
ChainResidueDetails
site_idSWS_FT_FI2
Number of Residues36
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails
site_idSWS_FT_FI3
Number of Residues3
DetailsModified residue: {"description":"Phosphoserine; by PAK1, PAK2 and PAK3","evidences":[{"source":"PubMed","id":"15849194","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI4
Number of Residues7
DetailsModified residue: {"description":"Phosphotyrosine; by SRC","evidences":[{"source":"PubMed","id":"16892053","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI5
Number of Residues4
DetailsModified residue: {"description":"Phosphoserine","evidences":[{"source":"PubMed","id":"16093354","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI6
Number of Residues3
DetailsModified residue: {"description":"Phosphothreonine","evidences":[{"source":"PubMed","id":"11447113","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI7
Number of Residues1
DetailsModified residue: {"description":"Phosphoserine","evidences":[{"source":"PubMed","id":"11447113","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI8
Number of Residues4
DetailsModified residue: {"description":"Symmetric dimethylarginine; by PRMT5","evidences":[{"source":"PubMed","id":"21917714","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI9
Number of Residues4
DetailsActive site: {"description":"Proton acceptor","evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PROSITE-ProRule","id":"PRU10027","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails
site_idSWS_FT_FI10
Number of Residues64
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"15543157","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"17880056","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"18951019","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"19019675","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"19706763","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"21310613","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI11
Number of Residues16
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"19161339","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"3EQH","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails
site_idSWS_FT_FI12
Number of Residues12
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"19161339","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"3EQF","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails
site_idSWS_FT_FI13
Number of Residues4
DetailsModified residue: {"description":"Phosphoserine; by BRAF and RAF1","evidences":[{"source":"PubMed","id":"10409742","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"20956560","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"29433126","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"8131746","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails
site_idSWS_FT_FI14
Number of Residues4
DetailsModified residue: {"description":"Phosphoserine; by BRAF and RAF1","evidences":[{"source":"PubMed","id":"20956560","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"29433126","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"8131746","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

246704

PDB entries from 2025-12-24

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