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TargetMAP kinase p38
LigandBDBM50126732
Substrate/Competitorn/a
Meas. Tech.ChEMBL_124474
IC50 150±n/a nM
Citation Goldberg DRButz TCardozo MGEckner RJHammach AHuang JJakes SKapadia SKashem MLukas SMorwick TMPanzenbeck MPatel UPav SPeet GWPeterson JDProkopowicz ASSnow RJSellati RTakahashi HTan JTschantz MAWang XJWang YWolak JXiong PMoss N Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. J Med Chem 46:1337-49 (2003) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
MAP kinase p38
Name:MAP kinase p38
Synonyms:n/a
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 124474
Components:This complex has 4 components.
Component 1
Name:p38 delta/gamma
Synonyms:MAP kinase p38 gamma | Mitogen-activated protein kinase 12 (MAPK12 p38 gamma) | Mitogen-activated protein kinase 12 (p38 gamma) | Mitogen-activated protein kinase p38 gamma (p38 MAPKγ)
Type:Protein
Mol. Mass.:41938.69
Organism:Homo sapiens (Human)
Description:P53778
Residue:367
Sequence:
MSSPPPARSGFYRQEVTKTAWEVRAVYRDLQPVGSGAYGAVCSAVDGRTGAKVAIKKLYR
PFQSELFAKRAYRELRLLKHMRHENVIGLLDVFTPDETLDDFTDFYLVMPFMGTDLGKLM
KHEKLGEDRIQFLVYQMLKGLRYIHAAGIIHRDLKPGNLAVNEDCELKILDFGLARQADS
EMTGYVVTRWYRAPEVILNWMRYTQTVDIWSVGCIMAEMITGKTLFKGSDHLDQLKEIMK
VTGTPPAEFVQRLQSDEAKNYMKGLPELEKKDFASILTNASPLAVNLLEKMLVLDAEQRV
TAGEALAHPYFESLHDTEDEPQVQKYDDSFDDVDRTLDEWKRVTYKEVLSFKPPRQLGAR
VSKETPL
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Component 2
Name:MAP kinase p38
Synonyms:MAP kinase p38 | Mitogen-activated protein kinase 11 | Mitogen-activated protein kinase p38 beta | Stress-activated protein kinase 2 | p38-2 | p38-beta | p38b
Type:Enzyme Catalytic Domain
Mol. Mass.:41351.73
Organism:Homo sapiens (Human)
Description:gi_20128774
Residue:364
Sequence:
MSGPRAGFYRQELNKTVWEVPQRLQGLRPVGSGAYGSVCSAYDARLRQKVAVKKLSRPFQ
SLIHARRTYRELRLLKHLKHENVIGLLDVFTPATSIEDFSEVYLVTTLMGADLNNIVKCQ
ALSDEHVQFLVYQLLRGLKYIHSAGIIHRDLKPSNVAVNEDCELRILDFGLARQADEEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLQGKALFPGSDYIDQLKRIMEVVG
TPSPEVLAKISSEHARTYIQSLPPMPQKDLSSIFRGANPLAIDLLGRMLVLDSDQRVSAA
EALAHAYFSQYHDPEDEPEAEPYDESVEAKERTLEEWKELTYQEVLSFKPPEPPKPPGSL
EIEQ
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Component 3
Name:Mitogen-activated protein kinase 14
Synonyms:CSAID-binding protein | CSBP | Cytokine suppressive anti-inflammatory drug-binding protein | MAP Kinase p38 alpha | MAP kinase MXI2 | MAP kinase p38 | MAX-interacting protein 2 | Mitogen-activated protein kinase (MAP) p38 alpha | Mitogen-activated protein kinase (Map p38 alpha) | Mitogen-activated protein kinase 14 (MAP kinase p38 alpha) | Mitogen-activated protein kinase 14 (MAPK14 p38 alpha) | Mitogen-activated protein kinase 14 (MAPK14) | Mitogen-activated protein kinase 14 (MAPK14) (p38 MAPKa) | Mitogen-activated protein kinase 14 (MAPK14) (p38 MAPKÿ±) | Mitogen-activated protein kinase 14 (p38 MAPKa) | Mitogen-activated protein kinase 14 (p38 alpha) | Mitogen-activated protein kinase 14, activated protein kinase p38 alpha | Mitogen-activated protein kinase p38 alpha | Mitogen-activated protein kinase p38 alpha (p38 MAPKa) | SAPK2A | p38-alpha
Type:Serine/threonine-protein kinase
Mol. Mass.:41286.76
Organism:Homo sapiens (Human)
Description:n/a
Residue:360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ
KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG
TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA
QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
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Component 4
Name:p38 delta/gamma
Synonyms:MAP kinase p38 delta | Mitogen-activated protein kinase 13 | Mitogen-activated protein kinase p38 | Mitogen-activated protein kinase p38 delta | Stress-activated protein kinase 4
Type:Enzyme
Mol. Mass.:42097.16
Organism:Homo sapiens (Human)
Description:O15264
Residue:365
Sequence:
MSLIRKKGFYKQDVNKTAWELPKTYVSPTHVGSGAYGSVCSAIDKRSGEKVAIKKLSRPF
QSEIFAKRAYRELLLLKHMQHENVIGLLDVFTPASSLRNFYDFYLVMPFMQTDLQKIMGM
EFSEEKIQYLVYQMLKGLKYIHSAGVVHRDLKPGNLAVNEDCELKILDFGLARHADAEMT
GYVVTRWYRAPEVILSWMHYNQTVDIWSVGCIMAEMLTGKTLFKGKDYLDQLTQILKVTG
VPGTEFVQKLNDKAAKSYIQSLPQTPRKDFTQLFPRASPQAADLLEKMLELDVDKRLTAA
QALTHPFFEPFRDPEEETEAQQPFDDSLEHEKLTVDEWKQHIYKEIVNFSPIARKDSRRR
SGMKL
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BDBM50126732
n/a
NameBDBM50126732
Synonyms:2-(2,6-Dichloro-phenylamino)-7-(3-diethylamino-propenyl)-1,6-dimethyl-1,8-dihydro-imidazo[4,5-h]isoquinolin-9-one | CHEMBL281957
TypeSmall organic molecule
Emp. Form.C25H27Cl2N5O
Mol. Mass.484.421
SMILESCCN(CC)CC=Cc1[nH]c(=O)c2c3n(C)c(Nc4c(Cl)cccc4Cl)nc3ccc2c1C |w:6.5|
Structure
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