O14976 | GAK_HUMAN | Cyclin-G-associated kinase (GAK)

Pfam Domain Table

AccessionDomainRangeColor
PF00069Pkinase - Protein kinase domain43~312
PF10409PTEN_C2 - C2 domain of PTEN tumour-suppressor protein570~708

3D structures mapped by conservation among orthologs

[ Domain: "Protein kinase" // Pkinase_Tyr ]

 PyMOL session


[ Alpha Fold Model ] (go)



Known binders annotated in ChEMBL

 IC50 CSV    Ki CSV
Only the first 20 rows are shown.
molecule_chembl_idstructureassay_typerelation valueunitmol_wtsmilesorganism assay_chembl_idbao_label
CHEMBL4531690 IC50 = 0.06 nM 330.78 Clc1cc2cc(c1)-c1cnn3ccc(nc13)NCCOCCO2 Homo sapiens CHEMBL4481510 cell-based format
CHEMBL1287853 IC50 = 1.0 nM 524.69 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 Homo sapiens CHEMBL5131610 single protein format
CHEMBL4740761 IC50 = 2.2 nM 445.55 COc1cc(-c2cnc3c(-c4cccc(NC(=O)N5CCCC5)c4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL81073 IC50 = 2.4 nM 395.42 COc1cc2ncc(C#N)c(Nc3cc(OC)c(OC)c(OC)c3)c2cc1OC Homo sapiens CHEMBL4394509 cell-based format
CHEMBL4778276 IC50 = 3.2 nM 461.55 COc1cc(-c2cnc3c(-c4cccc(NC(=O)N5CCOCC5)c4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4762694 IC50 = 3.8 nM 418.52 COc1cc(-c2cnc3c(-c4cccc(NC(=O)C(C)C)c4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4764705 IC50 = 7.7 nM 404.5 CCC(=O)Nc1cccc(-c2snc3cc(-c4ccc(N)c(OC)c4)cnc23)c1 Homo sapiens CHEMBL4736826 single protein format
CHEMBL4794323 IC50 = 8.8 nM 416.51 COc1cc(-c2cnc3c(-c4cccc(NC(=O)C5CC5)c4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL1738797 IC50 < 10.0 nM 482.63 CCc1cc2c(cc1N1CCC(N3CCOCC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O Homo sapiens CHEMBL4705535 single protein format
CHEMBL388978 IC50 = 11.0 nM 466.54 CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4 Homo sapiens CHEMBL4736826 single protein format
CHEMBL4745919 IC50 = 12.0 nM 402.48 C=CC(=O)Nc1cccc(-c2snc3cc(-c4ccc(N)c(OC)c4)cnc23)c1 Homo sapiens CHEMBL4736826 single protein format
CHEMBL4745028 IC50 = 13.0 nM 437.57 COc1cc(-c2cnc3c(N4CCC[C@H](CNC(=O)C5CC5)C4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4800032 IC50 = 14.0 nM 437.57 COc1cc(-c2cnc3c(N4CCCC(CNC(=O)C5CC5)C4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4779229 IC50 = 17.0 nM 444.56 COc1cc(-c2cnc3c(-c4cccc(NC(=O)C5CCCC5)c4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4646895 IC50 = 22.0 nM 398.49 COc1cc(-c2cnc3c(N4C[C@@H](C)O[C@@H](C)C4)snc3c2)ccc1C(N)=O Homo sapiens CHEMBL4610426 cell-based format
CHEMBL311959 IC50 = 23.0 nM 370.41 COc1cc2nccc(Nc3cc(OC)c(OC)c(OC)c3)c2cc1OC Homo sapiens CHEMBL4394509 cell-based format
CHEMBL4642467 IC50 = 24.0 nM 385.49 COc1ccc(-c2ccc3nsc(N4C[C@@H](C)O[C@@H](C)C4)c3n2)cc1OC Homo sapiens CHEMBL4610426 cell-based format
CHEMBL4440586 IC50 = 31.0 nM 329.36 C#Cc1cccc(Nc2c(C#N)cnc3cc(OC)c(OC)cc23)c1 Homo sapiens CHEMBL4394509 cell-based format
CHEMBL4752286 IC50 = 35.0 nM 473.6 COc1cc(-c2cnc3c(N4CCCC(CNC(=O)c5ccccc5)C4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format
CHEMBL4784439 IC50 = 37.0 nM 466.61 COc1cc(-c2cnc3c(N4CCCC(CNC(=O)N5CCCC5)C4)snc3c2)ccc1N Homo sapiens CHEMBL4736826 single protein format