Reaction Details |
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Target | Cyclin-G-associated kinase |
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Ligand | BDBM3032 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1892588 (CHEMBL4394509) |
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IC50 | 260±n/a nM |
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Citation | Asquith, CRM; Naegeli, KM; East, MP; Laitinen, T; Havener, TM; Wells, CI; Johnson, GL; Drewry, DH; Zuercher, WJ; Morris, DC Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. J Med Chem62:4772-4778 (2019) [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 |
Synonyms: | GAK | GAK_HUMAN | Serine/threonine-protein kinase GAK |
Type: | PROTEIN |
Mol. Mass.: | 143171.28 |
Organism: | Homo sapiens (Human) |
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
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BDBM3032 |
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n/a |
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Name | BDBM3032 |
Synonyms: | CHEMBL1204168 | CHEMBL29197 | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine | PD153035 | US11001595, Compound PD153035 | US11111252, Compound PD153035 | US9422297, PD153035 |
Type | Small organic molecule |
Emp. Form. | C16H14BrN3O2 |
Mol. Mass. | 360.205 |
SMILES | COc1cc2ncnc(Nc3cccc(Br)c3)c2cc1OC |
Structure |
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