General Information of the Protein
Protein ID
PT01920
Protein Name
Cyclin-G-associated kinase
Gene Name
GAK
Sequence
MSLLQSALDFLAGPGSLGGASGRDQSDFVGQTVELGELRLRVRRVLAEGGFAFVYEAQDVGSGREYALKRLLSNEEEKNRAIIQEVCFMKKLSGHPNIVQFCSAASIGKEESDTGQAEFLLLTELCKGQLVEFLKKMESRGPLSCDTVLKIFYQTCRAVQHMHRQKPPIIHRDLKVENLLLSNQGTIKLCDFGSATTISHYPDYSWSAQRRALVEEEITRNTTPMYRTPEIIDLYSNFPIGEKQDIWALGCILYLLCFRQHPFEDGAKLRIVNGKYSIPPHDTQYTVFHSLIRAMLQVNPEERLSIAEVVHQLQEIAAARNVNPKSPITELLEQNGGYGSATLSRGPPPPVGPAGSGYSGGLALAEYDQPYGGFLDILRGGTERLFTNLKDTSSKVIQSVANYAKGDLDISYITSRIAVMSFPAEGVESALKNNIEDVRLFLDSKHPGHYAVYNLSPRTYRPSRFHNRVSECGWAARRAPHLHTLYNICRNMHAWLRQDHKNVCVVHCMDGRAASAVAVCSFLCFCRLFSTAEAAVYMFSMKRCPPGIWPSHKRYIEYMCDMVAEEPITPHSKPILVRAVVMTPVPLFSKQRSGCRPFCEVYVGDERVASTSQEYDKMRDFKIEDGKAVIPLGVTVQGDVLIVIYHARSTLGGRLQAKMASMKMFQIQFHTGFVPRNATTVKFAKYDLDACDIQEKYPDLFQVNLEVEVEPRDRPSREAPPWENSSMRGLNPKILFSSREEQQDILSKFGKPELPRQPGSTAQYDAGAGSPEAEPTDSDSPPSSSADASRFLHTLDWQEEKEAETGAENASSKESESALMEDRDESEVSDEGGSPISSEGQEPRADPEPPGLAAGLVQQDLVFEVETPAVLPEPVPQEDGVDLLGLHSEVGAGPAVPPQACKAPSSNTDLLSCLLGPPEAASQGPPEDLLSEDPLLLASPAPPLSVQSTPRGGPPAAADPFGPLLPSSGNNSQPCSNPDLFGEFLNSDSVTVPPSFPSAHSAPPPSCSADFLHLGDLPGEPSKMTASSSNPDLLGGWAAWTETAASAVAPTPATEGPLFSPGGQPAPCGSQASWTKSQNPDPFADLGDLSSGLQGSPAGFPPGGFIPKTATTPKGSSSWQTSRPPAQGASWPPQAKPPPKACTQPRPNYASNFSVIGAREERGVRAPSFAQKPKVSENDFEDLLSNQGFSSRSDKKGPKTIAEMRKQDLAKDTDPLKLKLLDWIEGKERNIRALLSTLHTVLWDGESRWTPVGMADLVAPEQVKKHYRRAVLAVHPDKAAGQPYEQHAKMIFMELNDAWSEFENQGSRPLF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Other protein kinase group
>
Other protein kinase NAK family
Function
Associates with cyclin G and CDK5. Seems to act as an auxilin homolog that is involved in the uncoating of clathrin-coated vesicles by Hsc70 in non-neuronal cells. Expression oscillates slightly during the cell cycle, peaking at G1.
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Uniprot ID
Primary ID:
O14976

Secondarily ID:
Q5U4P5
Q9BVY6
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Ensembl ID
ENSG00000178950
HGNC ID
HGNC:4113
Subcellular Location
Cytoplasm
Perinuclear region
Golgi apparatus
Trans-Golgi network
Cell junction
Focal adhesion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0110399
 Compound Info 
4-Anilino-3-cyanoquinoline deriv. 4
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C21H21N3O5
  1
1
IC50 = 2.4 nM
 Bioactivity Info 
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CP0099872
 Compound Info 
4-Anilinoquinoline deriv. 8
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C20H22N2O5
  1
1
IC50 = 23 nM
 Bioactivity Info 
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CP0569632
 Compound Info 
4-(3-ethynylanilino)-6,7-dimethoxyquinoline-3-carbonitrile
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C20H15N3O2
  1
1
IC50 = 31 nM
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CP0180553
 Compound Info 
6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
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C18H17BrN2O3
  1
1
IC50 = 48 nM
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CP0183162
 Compound Info 
(6,7-Dimethoxy-quinazolin-4-yl)-(3-ethynyl-phenyl)-amine
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C18H15N3O2
  1
1
IC50 = 72 nM
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CP0289874
 Compound Info 
4-(3-Bromophenylamino)-6,7-dimethoxyquinoline-3-carbonitrile
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C18H14BrN3O2
  1
1
IC50 = 130 nM
 Bioactivity Info 
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CP0245015
 Compound Info 
6-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
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C19H17F3N2O3
  1
1
IC50 = 170 nM
 Bioactivity Info 
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CP0011998
 Compound Info 
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
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C16H14BrN3O2
  1
1
IC50 = 260 nM
 Bioactivity Info 
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CP0363886
 Compound Info 
6,7-dimethoxy-N-(3,4,5-trimethoxyphenyl)quinazolin-4-amine
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C19H21N3O5
  1
1
IC50 = 350 nM
 Bioactivity Info 
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CP0036082
 Compound Info 
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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C22H24ClFN4O3
  1
1
IC50 = 420 nM
 Bioactivity Info 
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CP0294002
 Compound Info 
N-(3-ethynylphenyl)-6,7-dimethoxyquinolin-4-amine
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C19H16N2O2
  1
1
IC50 = 500 nM
 Bioactivity Info 
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CP0438056
 Compound Info 
(3-Bromo-phenyl)-(6,7-dimethoxy-quinolin-4-yl)-amine
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C17H15BrN2O2
  1
1
IC50 = 510 nM
 Bioactivity Info 
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CP0037987
 Compound Info 
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
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C22H23N3O4
  1
1
IC50 = 910 nM
 Bioactivity Info 
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CP0402833
 Compound Info 
6,7-bis(2-methoxyethoxy)-N-(3,4,5-trimethoxyphenyl)quinazolin-4-amine
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C23H29N3O7
  1
1
IC50 = 2600 nM
 Bioactivity Info 
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CP0307724
 Compound Info 
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinolin-4-amine
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C23H24N2O4
  1
1
IC50 = 4200 nM
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CP0423044
 Compound Info 
N-[6-[3-[(4-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C24H21FN4O3S
  1
1
IC50 = 9240 nM
 Bioactivity Info 
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CP0489852
 Compound Info 
N-[6-[3-(propylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C20H22N4O3S
  1
1
IC50 = 9250 nM
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CP0423041
 Compound Info 
N-[6-[3-[(3-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C24H21FN4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0423042
 Compound Info 
N-[6-[3-[[[methyl(2,2,2-trifluoroethyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H22F3N5O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0423043
 Compound Info 
N-[6-[3-[(2-methylpropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C22H26N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0423045
 Compound Info 
N-[6-[3-[(cyclopropylmethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C22H24N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0423046
 Compound Info 
N-[6-[3-(cyclopropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C20H20N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0469511
 Compound Info 
N-[6-[3-(diethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H25N5O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0474150
 Compound Info 
N-[6-[3-[(2-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C24H21FN4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0474151
 Compound Info 
N-[6-[3-[[[ethyl(methyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H25N5O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0489853
 Compound Info 
N-[6-[3-[(3,3,3-trifluoropropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H21F3N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0519352
 Compound Info 
N-[6-[3-(cyclobutylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H22N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0519634
 Compound Info 
N-[6-[3-[(2,2,2-trifluoroethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C20H19F3N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0542395
 Compound Info 
N-[6-[3-[[ethyl(methyl)sulfamoyl]amino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C20H23N5O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0555200
 Compound Info 
N-[6-[3-(2-methylpropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C21H24N4O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0555201
 Compound Info 
N-[6-[3-[(diethylsulfamoylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide
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C22H27N5O3S
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037987
 Compound Info 
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
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C22H23N3O4
  4
1 IC50 = 38 nM
2 Kd = 3.1 nM
3 Kd = 21 nM
4 Kd = 40 nM
CP0099872
 Compound Info 
4-Anilinoquinoline deriv. 8
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C20H22N2O5
  1
1 IC50 = 45 nM
CP0180553
 Compound Info 
6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
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C18H17BrN2O3
  5
1 IC50 = 200 nM
2 Kd = 1.9 nM
3 Kd = 3.1 nM
4 Kd = 4.5 nM
5 Ki = 3.1 nM
CP0245015
 Compound Info 
6-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
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C19H17F3N2O3
  2
1 IC50 = 210 nM
2 Kd = 31 nM
CP0036082
 Compound Info 
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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C22H24ClFN4O3
  2
1 Kd = 7 nM
2 Kd = 13 nM
CP0011998
 Compound Info 
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
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C16H14BrN3O2
  1
1 Kd = 29 nM
Clinical Information about the Protein
Target 1 ( HUMAN cyclin G-associated kinase (GAK) )
Target Type Unknown Type Target
Disease 1 Target-related Disease  1
1 Rheumatoid arthritis [ICD-11: FA20]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Baricitinib
 Drug Info 
Approved
Rheumatoid arthritis