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Target
Cyclin-G-associated kinase
Ligand
BDBM50524288
Substrate
n/a
Meas. Tech.
ChEMBL_1935747 (CHEMBL4481506)
Ki
19000±n/a nM
Citation
 Asquith, CRM; Berger, BT; Wan, J; Bennett, JM; Capuzzi, SJ; Crona, DJ; Drewry, DH; East, MP; Elkins, JM; Fedorov, O; Godoi, PH; Hunter, DM; Knapp, S; Müller, S; Torrice, CD; Wells, CI; Earp, HS; Willson, TM; Zuercher, WJ SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). J Med Chem 62:2830-2836 (2019) [PubMed]  Article 
Target
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:
MSLLQSALDFLAGPGSLGGASGRDQSDFVGQTVELGELRLRVRRVLAEGGFAFVYEAQDVGSGREYALKRLLSNEEEKNRAIIQEVCFMKKLSGHPNIVQFCSAASIGKEESDTGQAEFLLLTELCKGQLVEFLKKMESRGPLSCDTVLKIFYQTCRAVQHMHRQKPPIIHRDLKVENLLLSNQGTIKLCDFGSATTISHYPDYSWSAQRRALVEEEITRNTTPMYRTPEIIDLYSNFPIGEKQDIWALGCILYLLCFRQHPFEDGAKLRIVNGKYSIPPHDTQYTVFHSLIRAMLQVNPEERLSIAEVVHQLQEIAAARNVNPKSPITELLEQNGGYGSATLSRGPPPPVGPAGSGYSGGLALAEYDQPYGGFLDILRGGTERLFTNLKDTSSKVIQSVANYAKGDLDISYITSRIAVMSFPAEGVESALKNNIEDVRLFLDSKHPGHYAVYNLSPRTYRPSRFHNRVSECGWAARRAPHLHTLYNICRNMHAWLRQDHKNVCVVHCMDGRAASAVAVCSFLCFCRLFSTAEAAVYMFSMKRCPPGIWPSHKRYIEYMCDMVAEEPITPHSKPILVRAVVMTPVPLFSKQRSGCRPFCEVYVGDERVASTSQEYDKMRDFKIEDGKAVIPLGVTVQGDVLIVIYHARSTLGGRLQAKMASMKMFQIQFHTGFVPRNATTVKFAKYDLDACDIQEKYPDLFQVNLEVEVEPRDRPSREAPPWENSSMRGLNPKILFSSREEQQDILSKFGKPELPRQPGSTAQYDAGAGSPEAEPTDSDSPPSSSADASRFLHTLDWQEEKEAETGAENASSKESESALMEDRDESEVSDEGGSPISSEGQEPRADPEPPGLAAGLVQQDLVFEVETPAVLPEPVPQEDGVDLLGLHSEVGAGPAVPPQACKAPSSNTDLLSCLLGPPEAASQGPPEDLLSEDPLLLASPAPPLSVQSTPRGGPPAAADPFGPLLPSSGNNSQPCSNPDLFGEFLNSDSVTVPPSFPSAHSAPPPSCSADFLHLGDLPGEPSKMTASSSNPDLLGGWAAWTETAASAVAPTPATEGPLFSPGGQPAPCGSQASWTKSQNPDPFADLGDLSSGLQGSPAGFPPGGFIPKTATTPKGSSSWQTSRPPAQGASWPPQAKPPPKACTQPRPNYASNFSVIGAREERGVRAPSFAQKPKVSENDFEDLLSNQGFSSRSDKKGPKTIAEMRKQDLAKDTDPLKLKLLDWIEGKERNIRALLSTLHTVLWDGESRWTPVGMADLVAPEQVKKHYRRAVLAVHPDKAAGQPYEQHAKMIFMELNDAWSEFENQGSRPLF
  
Inhibitor
Name:
BDBM50524288
Synonyms:
CHEMBL4518437
Type:
Small organic molecule
Emp. Form.:
C20H19F3N2O3
Mol. Mass.:
392.3717
SMILES:
COc1cc(Nc2cc(C)nc3ccc(cc23)C(F)(F)F)cc(OC)c1OC
Structure:
Search PDB for entries with ligand similarity: