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TargetSerine/threonine-protein kinase GAK
LigandBDBM50314070
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742474
Kd>1000±n/a nM
Citation Goldstein, DMSoth, MGabriel, TDewdney, NKuglstatter, AArzeno, HChen, JBingenheimer, WDalrymple, SADunn, JFarrell, RFrauchiger, SLa Fargue, JGhate, MGraves, BHill, RJLi, FLitman, RLoe, BMcIntosh, JMcWeeney, DPapp, EPark, JReese, HFRoberts, RTRotstein, DSan Pablo, BSarma, KStahl, MSung, MLSuttman, RTSjogren, EBTan, YTrejo, AWelch, MWeller, PWong, BRZecic, H Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors J Med Chem54:2255-65 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase GAK
Name:Serine/threonine-protein kinase GAK
Synonyms:GAK
Type:PROTEIN
Mol. Mass.:143171.28
Organism:Homo sapiens
Description:ChEMBL_1478229
Residue:1311
Sequence:
MSLLQSALDFLAGPGSLGGASGRDQSDFVGQTVELGELRLRVRRVLAEGGFAFVYEAQDV
GSGREYALKRLLSNEEEKNRAIIQEVCFMKKLSGHPNIVQFCSAASIGKEESDTGQAEFL
LLTELCKGQLVEFLKKMESRGPLSCDTVLKIFYQTCRAVQHMHRQKPPIIHRDLKVENLL
LSNQGTIKLCDFGSATTISHYPDYSWSAQRRALVEEEITRNTTPMYRTPEIIDLYSNFPI
GEKQDIWALGCILYLLCFRQHPFEDGAKLRIVNGKYSIPPHDTQYTVFHSLIRAMLQVNP
EERLSIAEVVHQLQEIAAARNVNPKSPITELLEQNGGYGSATLSRGPPPPVGPAGSGYSG
GLALAEYDQPYGGFLDILRGGTERLFTNLKDTSSKVIQSVANYAKGDLDISYITSRIAVM
SFPAEGVESALKNNIEDVRLFLDSKHPGHYAVYNLSPRTYRPSRFHNRVSECGWAARRAP
HLHTLYNICRNMHAWLRQDHKNVCVVHCMDGRAASAVAVCSFLCFCRLFSTAEAAVYMFS
MKRCPPGIWPSHKRYIEYMCDMVAEEPITPHSKPILVRAVVMTPVPLFSKQRSGCRPFCE
VYVGDERVASTSQEYDKMRDFKIEDGKAVIPLGVTVQGDVLIVIYHARSTLGGRLQAKMA
SMKMFQIQFHTGFVPRNATTVKFAKYDLDACDIQEKYPDLFQVNLEVEVEPRDRPSREAP
PWENSSMRGLNPKILFSSREEQQDILSKFGKPELPRQPGSTAQYDAGAGSPEAEPTDSDS
PPSSSADASRFLHTLDWQEEKEAETGAENASSKESESALMEDRDESEVSDEGGSPISSEG
QEPRADPEPPGLAAGLVQQDLVFEVETPAVLPEPVPQEDGVDLLGLHSEVGAGPAVPPQA
CKAPSSNTDLLSCLLGPPEAASQGPPEDLLSEDPLLLASPAPPLSVQSTPRGGPPAAADP
FGPLLPSSGNNSQPCSNPDLFGEFLNSDSVTVPPSFPSAHSAPPPSCSADFLHLGDLPGE
PSKMTASSSNPDLLGGWAAWTETAASAVAPTPATEGPLFSPGGQPAPCGSQASWTKSQNP
DPFADLGDLSSGLQGSPAGFPPGGFIPKTATTPKGSSSWQTSRPPAQGASWPPQAKPPPK
ACTQPRPNYASNFSVIGAREERGVRAPSFAQKPKVSENDFEDLLSNQGFSSRSDKKGPKT
IAEMRKQDLAKDTDPLKLKLLDWIEGKERNIRALLSTLHTVLWDGESRWTPVGMADLVAP
EQVKKHYRRAVLAVHPDKAAGQPYEQHAKMIFMELNDAWSEFENQGSRPLF
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50314070
NameBDBM50314070
Synonyms:6-(2,4-difluorophenoxy)-2-{[3-hydroxy-1-(2-hydroxyethyl)propyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1090089 | pamapimod
TypeSmall organic molecule
Emp. Form.C19H20F2N4O4
Mol. Mass.406.3833
SMILESCn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a