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Compile Data Set for Download or QSAR

Found 9 hits Enz. Inhib. hit(s) with Target = 'Cyclin-G-associated kinase' and Ligand = 'BDBM50524284'   
Target/Host
(Institution)		LigandTarget/Host
Links		Ligand
Links		Trg + Lig
Links		Ki
nM		ΔG°
kJ/mole		IC50
nM		Kd
nM		EC50/IC50
nM		koff
s-1		kon
M-1s-1		pHTemp
°C
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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 3.10n/an/an/an/an/an/an/an/a



Johann Wolfgang Goethe University

Curated by ChEMBL


Assay Description
Binding affinity to C-terminal AVI-tagged GAK (unknown origin) (12 to 347 residues) expressed in Escherichia coli after 1.5 hrs by TR-FRET assay

J Med Chem 62: 2830-2836 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01213
BindingDB Entry DOI: 10.7270/Q28919C7
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/a 48n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of NanoBRET tracer 5 binding to NL-fused GAK (unknown origin) expressed in HEK293 cells measured after 2 hrs by NanoBRET assay

Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113158
BindingDB Entry DOI: 10.7270/Q2R78JZ2
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/a 48n/an/an/an/an/an/a



University of North Carolina at Chapel Hill

Curated by ChEMBL


Assay Description
Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assay

J Med Chem 62: 4772-4778 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00350
BindingDB Entry DOI: 10.7270/Q2RJ4NVJ
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/a 120n/an/an/an/an/an/a



Johann Wolfgang Goethe University

Curated by ChEMBL


Assay Description
Displacement of fluorescent tracer from N-terminus of human GAK expressed in HEK293T cells after 2 hrs by NanoBRET target engagement assay

J Med Chem 62: 2830-2836 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01213
BindingDB Entry DOI: 10.7270/Q28919C7
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/a 200n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of GAK (unknown origin) by in-cell pulse based assay

Citation and Details

Article DOI: 10.1016/j.bmcl.2019.05.025
BindingDB Entry DOI: 10.7270/Q21J9FC5
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/an/a 1.90n/an/an/an/an/a



Johann Wolfgang Goethe University

Curated by ChEMBL


Assay Description
Binding affinity to biotinylated human GAK (13 to 338 residues) expressed in Escherichia coli incubated for 1.5 hrs by fluorescent tracer dependent T...

J Med Chem 62: 2830-2836 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01213
BindingDB Entry DOI: 10.7270/Q28919C7
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/an/a 4.5n/an/an/an/an/a



Johann Wolfgang Goethe University

Curated by ChEMBL


Assay Description
Binding affinity to GAK (unknown origin) by ITC assay

J Med Chem 62: 2830-2836 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01213
BindingDB Entry DOI: 10.7270/Q28919C7
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/an/a 3.10n/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00302
BindingDB Entry DOI: 10.7270/Q20Z779V
More data for this
Ligand-Target Pair
Cyclin-G-associated kinase


(Homo sapiens (Human))		BDBM50524284
PNG
(CHEMBL4443342)
Show SMILES COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Show InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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n/an/an/a 4.10n/an/an/an/an/a


TBA

Assay Description
Binding affinity to human wild type partial length GAK (G13 to Y338 residues) expressed in bacterial expression system by KinomeScan method

Citation and Details

Article DOI: 10.1016/j.bmcl.2019.05.025
BindingDB Entry DOI: 10.7270/Q21J9FC5
More data for this
Ligand-Target Pair