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PubMed code 17531483

Compile data set for download or QSAR
Found 39 hits of Enzyme Inhibition Constant Data   
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
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17048
PNG
(Indolinone based inhibitor, 4j | [(3Z)-2-oxo-3-[1-...)
Show SMILES CC\C(=C1\C(=O)Nc2ccc(NC(N)=O)cc12)c1ccc[nH]1
Show InChI InChI=1S/C16H16N4O2/c1-2-10(12-4-3-7-18-12)14-11-8-9(19-16(17)22)5-6-13(11)20-15(14)21/h3-8,18H,2H2,1H3,(H,20,21)(H3,17,19,22)/b14-10-
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n/an/a 3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17004
PNG
(BX-517 | Indolinone based inhibitor, 4i | [(3Z)-2-...)
Show SMILES C\C(=C1\C(=O)Nc2ccc(NC(N)=O)cc12)c1ccc[nH]1
Show InChI InChI=1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8-
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n/an/a 5n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17004
PNG
(BX-517 | Indolinone based inhibitor, 4i | [(3Z)-2-...)
Show SMILES C\C(=C1\C(=O)Nc2ccc(NC(N)=O)cc12)c1ccc[nH]1
Show InChI InChI=1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8-
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n/an/a 6n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
PDK1 inhibitory activity is measured directly using PDK1, a peptide substrate, 33PATP, and compound followed by capture on P81 phospho-cellulose pape...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17049
PNG
(Indolinone based inhibitor, 4k | [(3Z)-3-[(3-amino...)
Show SMILES NC(=O)Nc1ccc2NC(=O)\C(=C(/c3ccc[nH]3)c3cccc(N)c3)c2c1
Show InChI InChI=1S/C20H17N5O2/c21-12-4-1-3-11(9-12)17(16-5-2-8-23-16)18-14-10-13(24-20(22)27)6-7-15(14)25-19(18)26/h1-10,23H,21H2,(H,25,26)(H3,22,24,27)/b18-17-
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n/an/a 9n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17050
PNG
(Indolinone based inhibitor, 4l | [(3Z)-2-oxo-3-[py...)
Show SMILES NC(=O)Nc1ccc2NC(=O)\C(=C(/c3ccc[nH]3)c3ccncc3)c2c1
Show InChI InChI=1S/C19H15N5O2/c20-19(26)23-12-3-4-14-13(10-12)17(18(25)24-14)16(15-2-1-7-22-15)11-5-8-21-9-6-11/h1-10,22H,(H,24,25)(H3,20,23,26)/b17-16-
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n/an/a 10n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17041
PNG
((3Z)-2-oxo-3-[1-(1H-pyrrol-2-yl)propylidene]-2,3-d...)
Show SMILES CC\C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)c1ccc[nH]1
Show InChI InChI=1S/C15H15N3O3S/c1-2-10(12-4-3-7-17-12)14-11-8-9(22(16,20)21)5-6-13(11)18-15(14)19/h3-8,17H,2H2,1H3,(H,18,19)(H2,16,20,21)/b14-10-
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n/an/a 14n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM16981
PNG
(BX-201 | [(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)...)
Show SMILES NC(=O)Nc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H12N4O2/c15-14(20)17-9-3-4-12-10(7-9)11(13(19)18-12)6-8-2-1-5-16-8/h1-7,16H,(H,18,19)(H3,15,17,20)/b11-6-
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n/an/a 18n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17042
PNG
((3Z)-2-oxo-3-[phenyl(1H-pyrrol-2-yl)methylidene]-2...)
Show SMILES NS(=O)(=O)c1ccc2NC(=O)\C(=C(/c3ccc[nH]3)c3ccccc3)c2c1
Show InChI InChI=1S/C19H15N3O3S/c20-26(24,25)13-8-9-15-14(11-13)18(19(23)22-15)17(16-7-4-10-21-16)12-5-2-1-3-6-12/h1-11,21H,(H,22,23)(H2,20,24,25)/b18-17-
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n/an/a 29n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17043
PNG
(Indolinone based inhibitor, 4d | ethyl 2-[(3E)-2-o...)
Show SMILES CCOC(=O)C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)\c1ccc[nH]1
Show InChI InChI=1S/C16H15N3O5S/c1-2-24-16(21)14(12-4-3-7-18-12)13-10-8-9(25(17,22)23)5-6-11(10)19-15(13)20/h3-8,18H,2H2,1H3,(H,19,20)(H2,17,22,23)/b14-13+
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n/an/a 34n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17039
PNG
(Indolinone based inhibitor, 3k | N-[(3Z)-2-oxo-3-(...)
Show SMILES CC(=O)Nc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C15H13N3O2/c1-9(19)17-11-4-5-14-12(8-11)13(15(20)18-14)7-10-3-2-6-16-10/h2-8,16H,1H3,(H,17,19)(H,18,20)/b13-7-
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n/an/a 55n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17040
PNG
((3Z)-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-2,3-di...)
Show SMILES C\C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)c1ccc[nH]1
Show InChI InChI=1S/C14H13N3O3S/c1-8(11-3-2-6-16-11)13-10-7-9(21(15,19)20)4-5-12(10)17-14(13)18/h2-7,16H,1H3,(H,17,18)(H2,15,19,20)/b13-8-
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n/an/a 67n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17023
PNG
((3Z)-5-hydroxy-3-[1-(1H-pyrrol-2-yl)ethylidene]-2,...)
Show SMILES C\C(=C1\C(=O)Nc2ccc(O)cc12)c1ccc[nH]1
Show InChI InChI=1S/C14H12N2O2/c1-8(11-3-2-6-15-11)13-10-7-9(17)4-5-12(10)16-14(13)18/h2-7,15,17H,1H3,(H,16,18)/b13-8-
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n/an/a 80n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17033
PNG
((3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihyd...)
Show SMILES NC(=O)c1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H11N3O2/c15-13(18)8-3-4-12-10(6-8)11(14(19)17-12)7-9-2-1-5-16-9/h1-7,16H,(H2,15,18)(H,17,19)/b11-7-
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n/an/a 120n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17034
PNG
((3Z)-3-(1H-pyrrol-2-ylmethylidene)-5-(1H-1,2,3,4-t...)
Show SMILES O=C1Nc2ccc(cc2C1=Cc1ccc[nH]1)-c1nnn[nH]1 |w:10.12|
Show InChI InChI=1S/C14H10N6O/c21-14-11(7-9-2-1-5-15-9)10-6-8(3-4-12(10)16-14)13-17-19-20-18-13/h1-7,15H,(H,16,21)(H,17,18,19,20)
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n/an/a 200n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17032
PNG
((3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihyd...)
Show SMILES OC(=O)c1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H10N2O3/c17-13-11(7-9-2-1-5-15-9)10-6-8(14(18)19)3-4-12(10)16-13/h1-7,15H,(H,16,17)(H,18,19)/b11-7-
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n/an/a 260n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17024
PNG
((3Z)-5-hydroxy-3-[(3-methyl-1H-pyrrol-2-yl)methyli...)
Show SMILES Cc1cc[nH]c1\C=C1/C(=O)Nc2ccc(O)cc12
Show InChI InChI=1S/C14H12N2O2/c1-8-4-5-15-13(8)7-11-10-6-9(17)2-3-12(10)16-14(11)18/h2-7,15,17H,1H3,(H,16,18)/b11-7-
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n/an/a 280n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17025
PNG
((3Z)-5-hydroxy-3-[(4-methyl-1H-pyrrol-2-yl)methyli...)
Show SMILES Cc1c[nH]c(\C=C2/C(=O)Nc3ccc(O)cc23)c1
Show InChI InChI=1S/C14H12N2O2/c1-8-4-9(15-7-8)5-12-11-6-10(17)2-3-13(11)16-14(12)18/h2-7,15,17H,1H3,(H,16,18)/b12-5-
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n/an/a 280n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17030
PNG
((3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihyd...)
Show SMILES NS(=O)(=O)c1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C13H11N3O3S/c14-20(18,19)9-3-4-12-10(7-9)11(13(17)16-12)6-8-2-1-5-15-8/h1-7,15H,(H,16,17)(H2,14,18,19)/b11-6-
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n/an/a 290n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17020
PNG
((3Z)-5-hydroxy-3-(1H-pyrrol-2-ylmethylidene)-2,3-d...)
Show SMILES Oc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C13H10N2O2/c16-9-3-4-12-10(7-9)11(13(17)15-12)6-8-2-1-5-14-8/h1-7,14,16H,(H,15,17)/b11-6-
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n/an/a 340n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17016
PNG
((3Z)-4-methyl-3-(1H-pyrrol-2-ylmethylidene)-2,3-di...)
Show SMILES Cc1cccc2NC(=O)\C(=C/c3ccc[nH]3)c12
Show InChI InChI=1S/C14H12N2O/c1-9-4-2-6-12-13(9)11(14(17)16-12)8-10-5-3-7-15-10/h2-8,15H,1H3,(H,16,17)/b11-8-
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n/an/a 510n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17038
PNG
(Indolinone based inhibitor, 3j | N-[(3Z)-2-oxo-3-(...)
Show SMILES CS(=O)(=O)Nc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H13N3O3S/c1-21(19,20)17-10-4-5-13-11(8-10)12(14(18)16-13)7-9-3-2-6-15-9/h2-8,15,17H,1H3,(H,16,18)/b12-7-
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n/an/a 530n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17029
PNG
((3Z)-5-methoxy-3-(1H-pyrrol-2-ylmethylidene)-2,3-d...)
Show SMILES COc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H12N2O2/c1-18-10-4-5-13-11(8-10)12(14(17)16-13)7-9-3-2-6-15-9/h2-8,15H,1H3,(H,16,17)/b12-7-
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n/an/a 580n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17035
PNG
((3Z)-5-amino-3-(1H-pyrrol-2-ylmethylidene)-2,3-dih...)
Show SMILES Nc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C13H11N3O/c14-8-3-4-12-10(6-8)11(13(17)16-12)7-9-2-1-5-15-9/h1-7,15H,14H2,(H,16,17)/b11-7-
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n/an/a 580n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17031
PNG
(Indolinone based inhibitor, 3c | methyl (3Z)-2-oxo...)
Show SMILES COC(=O)c1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C15H12N2O3/c1-20-15(19)9-4-5-13-11(7-9)12(14(18)17-13)8-10-3-2-6-16-10/h2-8,16H,1H3,(H,17,18)/b12-8-
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n/an/a 670n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17026
PNG
((3Z)-5-hydroxy-3-[(5-methyl-1H-pyrrol-2-yl)methyli...)
Show SMILES Cc1ccc(\C=C2/C(=O)Nc3ccc(O)cc23)[nH]1
Show InChI InChI=1S/C14H12N2O2/c1-8-2-3-9(15-8)6-12-11-7-10(17)4-5-13(11)16-14(12)18/h2-7,15,17H,1H3,(H,16,18)/b12-6-
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n/an/a 680n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17021
PNG
((3Z)-6-hydroxy-3-(1H-pyrrol-2-ylmethylidene)-2,3-d...)
Show SMILES Oc1ccc2\C(=C\c3ccc[nH]3)C(=O)Nc2c1
Show InChI InChI=1S/C13H10N2O2/c16-9-3-4-10-11(6-8-2-1-5-14-8)13(17)15-12(10)7-9/h1-7,14,16H,(H,15,17)/b11-6-
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n/an/a 900n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17036
PNG
((3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihyd...)
Show SMILES O=C1Nc2ccc(cc2\C1=C\c1ccc[nH]1)C#N
Show InChI InChI=1S/C14H9N3O/c15-8-9-3-4-13-11(6-9)12(14(18)17-13)7-10-2-1-5-16-10/h1-7,16H,(H,17,18)/b12-7-
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n/an/a 990n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17037
PNG
((3Z)-5-(aminomethyl)-3-(1H-pyrrol-2-ylmethylidene)...)
Show SMILES NCc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H13N3O/c15-8-9-3-4-13-11(6-9)12(14(18)17-13)7-10-2-1-5-16-10/h1-7,16H,8,15H2,(H,17,18)/b12-7-
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n/an/a 1.00E+3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17019
PNG
((3Z)-4-hydroxy-3-(1H-pyrrol-2-ylmethylidene)-2,3-d...)
Show SMILES Oc1cccc2NC(=O)\C(=C/c3ccc[nH]3)c12
Show InChI InChI=1S/C13H10N2O2/c16-11-5-1-4-10-12(11)9(13(17)15-10)7-8-3-2-6-14-8/h1-7,14,16H,(H,15,17)/b9-7-
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n/an/a 1.00E+3n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17028
PNG
((3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-...)
Show SMILES Cc1cc(C)c(\C=C2/C(=O)Nc3ccc(O)cc23)[nH]1
Show InChI InChI=1S/C15H14N2O2/c1-8-5-9(2)16-14(8)7-12-11-6-10(18)3-4-13(11)17-15(12)19/h3-7,16,18H,1-2H3,(H,17,19)/b12-7-
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n/an/a 1.10E+3n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17015
PNG
((3Z)-3-(1H-pyrrol-2-ylmethylidene)-2,3-dihydro-1H-...)
Show SMILES O=C1Nc2ccccc2\C1=C\c1ccc[nH]1
Show InChI InChI=1S/C13H10N2O/c16-13-11(8-9-4-3-7-14-9)10-5-1-2-6-12(10)15-13/h1-8,14H,(H,15,16)/b11-8-
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n/an/a 1.80E+3n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17027
PNG
((3Z)-3-[(5-ethyl-1H-pyrrol-2-yl)methylidene]-5-hyd...)
Show SMILES CCc1ccc(\C=C2/C(=O)Nc3ccc(O)cc23)[nH]1
Show InChI InChI=1S/C15H14N2O2/c1-2-9-3-4-10(16-9)7-13-12-8-11(18)5-6-14(12)17-15(13)19/h3-8,16,18H,2H2,1H3,(H,17,19)/b13-7-
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n/an/a 2.30E+3n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17017
PNG
((3Z)-5-methyl-3-(1H-pyrrol-2-ylmethylidene)-2,3-di...)
Show SMILES Cc1ccc2NC(=O)\C(=C/c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H12N2O/c1-9-4-5-13-11(7-9)12(14(17)16-13)8-10-3-2-6-15-10/h2-8,15H,1H3,(H,16,17)/b12-8-
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n/an/a 2.70E+3n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17045
PNG
(2-[(3E)-2-oxo-5-sulfamoyl-2,3-dihydro-1H-indol-3-y...)
Show SMILES NC(=O)C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)\c1ccc[nH]1
Show InChI InChI=1S/C14H12N4O4S/c15-13(19)12(10-2-1-5-17-10)11-8-6-7(23(16,21)22)3-4-9(8)18-14(11)20/h1-6,17H,(H2,15,19)(H,18,20)(H2,16,21,22)/b12-11+
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n/an/a 3.90E+3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17044
PNG
(2-[(3E)-2-oxo-5-sulfamoyl-2,3-dihydro-1H-indol-3-y...)
Show SMILES NS(=O)(=O)c1ccc2NC(=O)\C(=C(\C(O)=O)c3ccc[nH]3)c2c1
Show InChI InChI=1S/C14H11N3O5S/c15-23(21,22)7-3-4-9-8(6-7)11(13(18)17-9)12(14(19)20)10-2-1-5-16-10/h1-6,16H,(H,17,18)(H,19,20)(H2,15,21,22)/b12-11+
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n/an/a 4.20E+3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17047
PNG
(Indolinone based inhibitor, 4h | N,N-diethyl-2-[(3...)
Show SMILES CCN(CC)C(=O)C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)\c1ccc[nH]1
Show InChI InChI=1S/C18H20N4O4S/c1-3-22(4-2)18(24)16(14-6-5-9-20-14)15-12-10-11(27(19,25)26)7-8-13(12)21-17(15)23/h5-10,20H,3-4H2,1-2H3,(H,21,23)(H2,19,25,26)/b16-15+
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n/an/a 5.40E+3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17046
PNG
(Indolinone based inhibitor, 4g | N-ethyl-2-[(3E)-2...)
Show SMILES CCNC(=O)C(=C1\C(=O)Nc2ccc(cc12)S(N)(=O)=O)\c1ccc[nH]1
Show InChI InChI=1S/C16H16N4O4S/c1-2-18-15(21)14(12-4-3-7-19-12)13-10-8-9(25(17,23)24)5-6-11(10)20-16(13)22/h3-8,19H,2H2,1H3,(H,18,21)(H,20,22)(H2,17,23,24)/b14-13+
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n/an/a 6.10E+3n/an/an/an/an/an/a



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17018
PNG
((3Z)-7-methyl-3-(1H-pyrrol-2-ylmethylidene)-2,3-di...)
Show SMILES Cc1cccc2\C(=C\c3ccc[nH]3)C(=O)Nc12
Show InChI InChI=1S/C14H12N2O/c1-9-4-2-6-11-12(14(17)16-13(9)11)8-10-5-3-7-15-10/h2-8,15H,1H3,(H,16,17)/b12-8-
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n/an/a>2.60E+4n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
3-phosphoinositide-dependent protein kinase 1


(Homo sapiens (Human))		BDBM17022
PNG
((3Z)-7-hydroxy-3-(1H-pyrrol-2-ylmethylidene)-2,3-d...)
Show SMILES Oc1cccc2\C(=C\c3ccc[nH]3)C(=O)Nc12
Show InChI InChI=1S/C13H10N2O2/c16-11-5-1-4-9-10(13(17)15-12(9)11)7-8-3-2-6-14-8/h1-7,14,16H,(H,15,17)/b10-7-
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n/an/a>2.60E+4n/an/an/an/a7.222



Berlex Biosciences



Assay Description
The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...

Bioorg Med Chem Lett 17: 3814-8 (2007)


Article DOI: 10.1016/j.bmcl.2007.04.071
BindingDB Entry DOI: 10.7270/Q25Q4TBB
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%