| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-G-associated kinase |
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| Ligand | BDBM50562907 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2081035 (CHEMBL4736826) |
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| IC50 | 35±n/a nM |
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| Citation |  Martinez-Gualda, B; Saul, S; Froeyen, M; Schols, D; Herdewijn, P; Einav, S; De Jonghe, S Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase. Eur J Med Chem213:0 (2021) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Cyclin-G-associated kinase |
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| Name: | Cyclin-G-associated kinase |
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| Synonyms: | GAK | GAK_HUMAN | Serine/threonine-protein kinase GAK |
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| Type: | PROTEIN |
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| Mol. Mass.: | 143171.28 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_1478229 |
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| Residue: | 1311 |
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| Sequence: | MSLLQSALDFLAGPGSLGGASGRDQSDFVGQTVELGELRLRVRRVLAEGGFAFVYEAQDV
GSGREYALKRLLSNEEEKNRAIIQEVCFMKKLSGHPNIVQFCSAASIGKEESDTGQAEFL
LLTELCKGQLVEFLKKMESRGPLSCDTVLKIFYQTCRAVQHMHRQKPPIIHRDLKVENLL
LSNQGTIKLCDFGSATTISHYPDYSWSAQRRALVEEEITRNTTPMYRTPEIIDLYSNFPI
GEKQDIWALGCILYLLCFRQHPFEDGAKLRIVNGKYSIPPHDTQYTVFHSLIRAMLQVNP
EERLSIAEVVHQLQEIAAARNVNPKSPITELLEQNGGYGSATLSRGPPPPVGPAGSGYSG
GLALAEYDQPYGGFLDILRGGTERLFTNLKDTSSKVIQSVANYAKGDLDISYITSRIAVM
SFPAEGVESALKNNIEDVRLFLDSKHPGHYAVYNLSPRTYRPSRFHNRVSECGWAARRAP
HLHTLYNICRNMHAWLRQDHKNVCVVHCMDGRAASAVAVCSFLCFCRLFSTAEAAVYMFS
MKRCPPGIWPSHKRYIEYMCDMVAEEPITPHSKPILVRAVVMTPVPLFSKQRSGCRPFCE
VYVGDERVASTSQEYDKMRDFKIEDGKAVIPLGVTVQGDVLIVIYHARSTLGGRLQAKMA
SMKMFQIQFHTGFVPRNATTVKFAKYDLDACDIQEKYPDLFQVNLEVEVEPRDRPSREAP
PWENSSMRGLNPKILFSSREEQQDILSKFGKPELPRQPGSTAQYDAGAGSPEAEPTDSDS
PPSSSADASRFLHTLDWQEEKEAETGAENASSKESESALMEDRDESEVSDEGGSPISSEG
QEPRADPEPPGLAAGLVQQDLVFEVETPAVLPEPVPQEDGVDLLGLHSEVGAGPAVPPQA
CKAPSSNTDLLSCLLGPPEAASQGPPEDLLSEDPLLLASPAPPLSVQSTPRGGPPAAADP
FGPLLPSSGNNSQPCSNPDLFGEFLNSDSVTVPPSFPSAHSAPPPSCSADFLHLGDLPGE
PSKMTASSSNPDLLGGWAAWTETAASAVAPTPATEGPLFSPGGQPAPCGSQASWTKSQNP
DPFADLGDLSSGLQGSPAGFPPGGFIPKTATTPKGSSSWQTSRPPAQGASWPPQAKPPPK
ACTQPRPNYASNFSVIGAREERGVRAPSFAQKPKVSENDFEDLLSNQGFSSRSDKKGPKT
IAEMRKQDLAKDTDPLKLKLLDWIEGKERNIRALLSTLHTVLWDGESRWTPVGMADLVAP
EQVKKHYRRAVLAVHPDKAAGQPYEQHAKMIFMELNDAWSEFENQGSRPLF
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| BDBM50562907 |
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| n/a |
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| Name | BDBM50562907 |
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| Synonyms: | CHEMBL4752286 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H27N5O2S |
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| Mol. Mass. | 473.59 |
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| SMILES | COc1cc(ccc1N)-c1cnc2c(snc2c1)N1CCCC(CNC(=O)c2ccccc2)C1 |
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| Structure | 
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