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Patent code US8987273

Compile Data Set for Download or QSAR
Found 75 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
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151095
PNG
(US8987273, 4-2)
Show SMILES COC(=O)c1cccc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H26N4O2/c1-36-29(35)23-10-5-9-22(17-23)26-19-32-27-18-25(20-7-3-2-4-8-20)28(33-34(26)27)21-11-13-24(14-12-21)30(31)15-6-16-30/h2-5,7-14,17-19H,6,15-16,31H2,1H3
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n/an/a 4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151092
PNG
(US8987273, 3-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cccc(c1)C#N
Show InChI InChI=1S/C29H23N5/c30-18-20-6-4-9-23(16-20)26-19-32-27-17-25(21-7-2-1-3-8-21)28(33-34(26)27)22-10-12-24(13-11-22)29(31)14-5-15-29/h1-4,6-13,16-17,19H,5,14-15,31H2
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n/an/a 5n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151111
PNG
(US8987273, 4-18)
Show SMILES COc1cncc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C28H25N5O/c1-34-23-14-21(16-30-17-23)25-18-31-26-15-24(19-6-3-2-4-7-19)27(32-33(25)26)20-8-10-22(11-9-20)28(29)12-5-13-28/h2-4,6-11,14-18H,5,12-13,29H2,1H3
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n/an/a 5n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151098
PNG
(US8987273, 4-5)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cccc(CO)c1
Show InChI InChI=1S/C29H26N4O/c30-29(14-5-15-29)24-12-10-22(11-13-24)28-25(21-7-2-1-3-8-21)17-27-31-18-26(33(27)32-28)23-9-4-6-20(16-23)19-34/h1-4,6-13,16-18,34H,5,14-15,19,30H2
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n/an/a 6n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151110
PNG
(US8987273, 4-17)
Show SMILES CCOC(=O)c1cncc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O2/c1-2-37-29(36)23-15-22(17-32-18-23)26-19-33-27-16-25(20-7-4-3-5-8-20)28(34-35(26)27)21-9-11-24(12-10-21)30(31)13-6-14-30/h3-5,7-12,15-19H,2,6,13-14,31H2,1H3
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n/an/a 7n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151105
PNG
(US8987273, 4-12)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cn[nH]c1
Show InChI InChI=1S/C25H22N6/c26-25(11-4-12-25)20-9-7-18(8-10-20)24-21(17-5-2-1-3-6-17)13-23-27-16-22(31(23)30-24)19-14-28-29-15-19/h1-3,5-10,13-16H,4,11-12,26H2,(H,28,29)
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n/an/a 9n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151102
PNG
(US8987273, 4-9)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(F)c(CO)c1
Show InChI InChI=1S/C29H25FN4O/c30-25-12-9-21(15-22(25)18-35)26-17-32-27-16-24(19-5-2-1-3-6-19)28(33-34(26)27)20-7-10-23(11-8-20)29(31)13-4-14-29/h1-3,5-12,15-17,35H,4,13-14,18,31H2
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n/an/a 9n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151109
PNG
(US8987273, 4-16)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc2cn[nH]c2c1
Show InChI InChI=1S/C29H24N6/c30-29(13-4-14-29)23-11-9-20(10-12-23)28-24(19-5-2-1-3-6-19)16-27-31-18-26(35(27)34-28)21-7-8-22-17-32-33-25(22)15-21/h1-3,5-12,15-18H,4,13-14,30H2,(H,32,33)
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n/an/a 11n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151108
PNG
(US8987273, 4-15)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccn[nH]1
Show InChI InChI=1S/C25H22N6/c26-25(12-4-13-25)19-9-7-18(8-10-19)24-20(17-5-2-1-3-6-17)15-23-27-16-22(31(23)30-24)21-11-14-28-29-21/h1-3,5-11,14-16H,4,12-13,26H2,(H,28,29)
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n/an/a 11n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151104
PNG
(US8987273, 4-11)
Show SMILES NC(=O)c1cccc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O/c30-28(35)22-9-4-8-21(16-22)25-18-32-26-17-24(19-6-2-1-3-7-19)27(33-34(25)26)20-10-12-23(13-11-20)29(31)14-5-15-29/h1-4,6-13,16-18H,5,14-15,31H2,(H2,30,35)
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n/an/a 13n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151107
PNG
(US8987273, 4-14)
Show SMILES COC(=O)c1ccc(cn1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O2/c1-36-28(35)24-13-10-21(17-31-24)25-18-32-26-16-23(19-6-3-2-4-7-19)27(33-34(25)26)20-8-11-22(12-9-20)29(30)14-5-15-29/h2-4,6-13,16-18H,5,14-15,30H2,1H3
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n/an/a 19n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151099
PNG
(US8987273, 4-6)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(CO)cc1
Show InChI InChI=1S/C29H26N4O/c30-29(15-4-16-29)24-13-11-23(12-14-24)28-25(21-5-2-1-3-6-21)17-27-31-18-26(33(27)32-28)22-9-7-20(19-34)8-10-22/h1-3,5-14,17-18,34H,4,15-16,19,30H2
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n/an/a 19n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151109
PNG
(US8987273, 4-16)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc2cn[nH]c2c1
Show InChI InChI=1S/C29H24N6/c30-29(13-4-14-29)23-11-9-20(10-12-23)28-24(19-5-2-1-3-6-19)16-27-31-18-26(35(27)34-28)21-7-8-22-17-32-33-25(22)15-21/h1-3,5-12,15-18H,4,13-14,30H2,(H,32,33)
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n/an/a 22n/an/an/an/a7.522



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US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151103
PNG
(US8987273, 4-10)
Show SMILES NC(=O)c1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O/c30-28(35)22-9-7-20(8-10-22)25-18-32-26-17-24(19-5-2-1-3-6-19)27(33-34(25)26)21-11-13-23(14-12-21)29(31)15-4-16-29/h1-3,5-14,17-18H,4,15-16,31H2,(H2,30,35)
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n/an/a 27n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151096
PNG
(US8987273, 4-3)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H23FN4/c29-23-13-9-20(10-14-23)25-18-31-26-17-24(19-5-2-1-3-6-19)27(32-33(25)26)21-7-11-22(12-8-21)28(30)15-4-16-28/h1-3,5-14,17-18H,4,15-16,30H2
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n/an/a 36n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151098
PNG
(US8987273, 4-5)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cccc(CO)c1
Show InChI InChI=1S/C29H26N4O/c30-29(14-5-15-29)24-12-10-22(11-13-24)28-25(21-7-2-1-3-8-21)17-27-31-18-26(33(27)32-28)23-9-4-6-20(16-23)19-34/h1-4,6-13,16-18,34H,5,14-15,19,30H2
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n/an/a 37n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151121
PNG
(US8987273, 8-0)
Show SMILES NC(=O)\C=C\c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H23N5O/c26-22(31)12-11-20-16-28-23-15-21(17-5-2-1-3-6-17)24(29-30(20)23)18-7-9-19(10-8-18)25(27)13-4-14-25/h1-3,5-12,15-16H,4,13-14,27H2,(H2,26,31)/b12-11+
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n/an/a 38n/an/an/an/a7.522



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US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151119
PNG
(US8987273, 6-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(c(Br)nc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H22BrFN4/c29-27-26(20-9-13-22(30)14-10-20)34-24(32-27)17-23(18-5-2-1-3-6-18)25(33-34)19-7-11-21(12-8-19)28(31)15-4-16-28/h1-3,5-14,17H,4,15-16,31H2
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n/an/a 41n/an/an/an/a7.522



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US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151097
PNG
(US8987273, 4-4)
Show SMILES Cc1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H26N4/c1-20-8-10-22(11-9-20)26-19-31-27-18-25(21-6-3-2-4-7-21)28(32-33(26)27)23-12-14-24(15-13-23)29(30)16-5-17-29/h2-4,6-15,18-19H,5,16-17,30H2,1H3
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n/an/a 44n/an/an/an/a7.522



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US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151122
PNG
(US8987273, 9-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(C=C)cnc2cc1-c1ccccc1
Show InChI InChI=1S/C24H22N4/c1-2-20-16-26-22-15-21(17-7-4-3-5-8-17)23(27-28(20)22)18-9-11-19(12-10-18)24(25)13-6-14-24/h2-5,7-12,15-16H,1,6,13-14,25H2
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n/an/a 44n/an/an/an/a7.522



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US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151111
PNG
(US8987273, 4-18)
Show SMILES COc1cncc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C28H25N5O/c1-34-23-14-21(16-30-17-23)25-18-31-26-15-24(19-6-3-2-4-7-19)27(32-33(25)26)20-8-10-22(11-9-20)28(29)12-5-13-28/h2-4,6-11,14-18H,5,12-13,29H2,1H3
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n/an/a 46n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151100
PNG
(US8987273, 4-7)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(cc1)S(N)(=O)=O
Show InChI InChI=1S/C28H25N5O2S/c29-28(15-4-16-28)22-11-7-21(8-12-22)27-24(19-5-2-1-3-6-19)17-26-31-18-25(33(26)32-27)20-9-13-23(14-10-20)36(30,34)35/h1-3,5-14,17-18H,4,15-16,29H2,(H2,30,34,35)
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n/an/a 47n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151095
PNG
(US8987273, 4-2)
Show SMILES COC(=O)c1cccc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H26N4O2/c1-36-29(35)23-10-5-9-22(17-23)26-19-32-27-18-25(20-7-3-2-4-8-20)28(33-34(26)27)21-11-13-24(14-12-21)30(31)15-6-16-30/h2-5,7-14,17-19H,6,15-16,31H2,1H3
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n/an/a 58n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151105
PNG
(US8987273, 4-12)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cn[nH]c1
Show InChI InChI=1S/C25H22N6/c26-25(11-4-12-25)20-9-7-18(8-10-20)24-21(17-5-2-1-3-6-17)13-23-27-16-22(31(23)30-24)19-14-28-29-15-19/h1-3,5-10,13-16H,4,11-12,26H2,(H,28,29)
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n/an/a 67n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151104
PNG
(US8987273, 4-11)
Show SMILES NC(=O)c1cccc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O/c30-28(35)22-9-4-8-21(16-22)25-18-32-26-17-24(19-6-2-1-3-7-19)27(33-34(25)26)20-10-12-23(13-11-20)29(31)14-5-15-29/h1-4,6-13,16-18H,5,14-15,31H2,(H2,30,35)
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n/an/a 68n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151119
PNG
(US8987273, 6-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(c(Br)nc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H22BrFN4/c29-27-26(20-9-13-22(30)14-10-20)34-24(32-27)17-23(18-5-2-1-3-6-18)25(33-34)19-7-11-21(12-8-19)28(31)15-4-16-28/h1-3,5-14,17H,4,15-16,31H2
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n/an/a 68n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151108
PNG
(US8987273, 4-15)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccn[nH]1
Show InChI InChI=1S/C25H22N6/c26-25(12-4-13-25)19-9-7-18(8-10-19)24-20(17-5-2-1-3-6-17)15-23-27-16-22(31(23)30-24)21-11-14-28-29-21/h1-3,5-11,14-16H,4,12-13,26H2,(H,28,29)
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n/an/a 70n/an/an/an/a7.522



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US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151101
PNG
(US8987273, 4-8)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(Br)cnc2cc1-c1ccccc1
Show InChI InChI=1S/C22H19BrN4/c23-19-14-25-20-13-18(15-5-2-1-3-6-15)21(26-27(19)20)16-7-9-17(10-8-16)22(24)11-4-12-22/h1-3,5-10,13-14H,4,11-12,24H2
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n/an/a 74n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151096
PNG
(US8987273, 4-3)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H23FN4/c29-23-13-9-20(10-14-23)25-18-31-26-17-24(19-5-2-1-3-6-19)27(32-33(25)26)21-7-11-22(12-8-21)28(30)15-4-16-28/h1-3,5-14,17-18H,4,15-16,30H2
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n/an/a 81n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151092
PNG
(US8987273, 3-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1cccc(c1)C#N
Show InChI InChI=1S/C29H23N5/c30-18-20-6-4-9-23(16-20)26-19-32-27-17-25(21-7-2-1-3-8-21)28(33-34(26)27)22-10-12-24(13-11-22)29(31)14-5-15-29/h1-4,6-13,16-17,19H,5,14-15,31H2
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n/an/a 82n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151102
PNG
(US8987273, 4-9)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(F)c(CO)c1
Show InChI InChI=1S/C29H25FN4O/c30-25-12-9-21(15-22(25)18-35)26-17-32-27-16-24(19-5-2-1-3-6-19)28(33-34(26)27)20-7-10-23(11-8-20)29(31)13-4-14-29/h1-3,5-12,15-17,35H,4,13-14,18,31H2
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n/an/a 92n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151120
PNG
(US8987273, 7-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(c(Cl)nc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H22ClFN4/c29-27-26(20-9-13-22(30)14-10-20)34-24(32-27)17-23(18-5-2-1-3-6-18)25(33-34)19-7-11-21(12-8-19)28(31)15-4-16-28/h1-3,5-14,17H,4,15-16,31H2
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n/an/a 99n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151120
PNG
(US8987273, 7-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(c(Cl)nc2cc1-c1ccccc1)-c1ccc(F)cc1
Show InChI InChI=1S/C28H22ClFN4/c29-27-26(20-9-13-22(30)14-10-20)34-24(32-27)17-23(18-5-2-1-3-6-18)25(33-34)19-7-11-21(12-8-19)28(31)15-4-16-28/h1-3,5-14,17H,4,15-16,31H2
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n/an/a 106n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151093
PNG
(US8987273, 4-0)
Show SMILES CS(=O)(=O)c1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H26N4O2S/c1-36(34,35)24-14-10-21(11-15-24)26-19-31-27-18-25(20-6-3-2-4-7-20)28(32-33(26)27)22-8-12-23(13-9-22)29(30)16-5-17-29/h2-4,6-15,18-19H,5,16-17,30H2,1H3
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n/an/a 110n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151110
PNG
(US8987273, 4-17)
Show SMILES CCOC(=O)c1cncc(c1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O2/c1-2-37-29(36)23-15-22(17-32-18-23)26-19-33-27-16-25(20-7-4-3-5-8-20)28(34-35(26)27)21-9-11-24(12-10-21)30(31)13-6-14-30/h3-5,7-12,15-19H,2,6,13-14,31H2,1H3
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n/an/a 110n/an/an/an/a7.522



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US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151107
PNG
(US8987273, 4-14)
Show SMILES COC(=O)c1ccc(cn1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O2/c1-36-28(35)24-13-10-21(17-31-24)25-18-32-26-16-23(19-6-3-2-4-7-19)27(33-34(25)26)20-8-11-22(12-9-20)29(30)14-5-15-29/h2-4,6-13,16-18H,5,14-15,30H2,1H3
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n/an/a 115n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151103
PNG
(US8987273, 4-10)
Show SMILES NC(=O)c1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25N5O/c30-28(35)22-9-7-20(8-10-22)25-18-32-26-17-24(19-5-2-1-3-6-19)27(33-34(25)26)21-11-13-23(14-12-21)29(31)15-4-16-29/h1-3,5-14,17-18H,4,15-16,31H2,(H2,30,35)
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n/an/a 118n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151099
PNG
(US8987273, 4-6)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(CO)cc1
Show InChI InChI=1S/C29H26N4O/c30-29(15-4-16-29)24-13-11-23(12-14-24)28-25(21-5-2-1-3-6-21)17-27-31-18-26(33(27)32-28)22-9-7-20(19-34)8-10-22/h1-3,5-14,17-18,34H,4,15-16,19,30H2
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n/an/a 123n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151094
PNG
(US8987273, 4-1)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H23N5/c30-18-20-7-9-22(10-8-20)26-19-32-27-17-25(21-5-2-1-3-6-21)28(33-34(26)27)23-11-13-24(14-12-23)29(31)15-4-16-29/h1-3,5-14,17,19H,4,15-16,31H2
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n/an/a 129n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151094
PNG
(US8987273, 4-1)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H23N5/c30-18-20-7-9-22(10-8-20)26-19-32-27-17-25(21-5-2-1-3-6-21)28(33-34(26)27)23-11-13-24(14-12-23)29(31)15-4-16-29/h1-3,5-14,17,19H,4,15-16,31H2
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n/an/a 136n/an/an/an/a7.522



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US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151106
PNG
(US8987273, 4-13)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(O)nc1
Show InChI InChI=1S/C27H23N5O/c28-27(13-4-14-27)21-10-7-19(8-11-21)26-22(18-5-2-1-3-6-18)15-24-29-17-23(32(24)31-26)20-9-12-25(33)30-16-20/h1-3,5-12,15-17H,4,13-14,28H2,(H,30,33)
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n/an/a 146n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151100
PNG
(US8987273, 4-7)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(cc1)S(N)(=O)=O
Show InChI InChI=1S/C28H25N5O2S/c29-28(15-4-16-28)22-11-7-21(8-12-22)27-24(19-5-2-1-3-6-19)17-26-31-18-25(33(26)32-27)20-9-13-23(14-10-20)36(30,34)35/h1-3,5-14,17-18H,4,15-16,29H2,(H2,30,34,35)
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n/an/a 151n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151121
PNG
(US8987273, 8-0)
Show SMILES NC(=O)\C=C\c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H23N5O/c26-22(31)12-11-20-16-28-23-15-21(17-5-2-1-3-6-17)24(29-30(20)23)18-7-9-19(10-8-18)25(27)13-4-14-25/h1-3,5-12,15-16H,4,13-14,27H2,(H2,26,31)/b12-11+
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n/an/a 222n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM50384861
PNG
(CHEMBL2035019)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2ccnc2cc1-c1ccccc1
Show InChI InChI=1S/C22H20N4/c23-22(11-4-12-22)18-9-7-17(8-10-18)21-19(16-5-2-1-3-6-16)15-20-24-13-14-26(20)25-21/h1-3,5-10,13-15H,4,11-12,23H2
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n/an/a 246n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151101
PNG
(US8987273, 4-8)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(Br)cnc2cc1-c1ccccc1
Show InChI InChI=1S/C22H19BrN4/c23-19-14-25-20-13-18(15-5-2-1-3-6-15)21(26-27(19)20)16-7-9-17(10-8-16)22(24)11-4-12-22/h1-3,5-10,13-14H,4,11-12,24H2
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n/an/a 264n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151097
PNG
(US8987273, 4-4)
Show SMILES Cc1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H26N4/c1-20-8-10-22(11-9-20)26-19-31-27-18-25(21-6-3-2-4-7-21)28(32-33(26)27)23-12-14-24(15-13-23)29(30)16-5-17-29/h2-4,6-15,18-19H,5,16-17,30H2,1H3
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n/an/a 277n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151093
PNG
(US8987273, 4-0)
Show SMILES CS(=O)(=O)c1ccc(cc1)-c1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H26N4O2S/c1-36(34,35)24-14-10-21(11-15-24)26-19-31-27-18-25(20-6-3-2-4-7-20)28(32-33(26)27)22-8-12-23(13-9-22)29(30)16-5-17-29/h2-4,6-15,18-19H,5,16-17,30H2,1H3
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n/an/a 278n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151122
PNG
(US8987273, 9-0)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(C=C)cnc2cc1-c1ccccc1
Show InChI InChI=1S/C24H22N4/c1-2-20-16-26-22-15-21(17-7-4-3-5-8-17)23(27-28(20)22)18-9-11-19(12-10-18)24(25)13-6-14-24/h2-5,7-12,15-16H,1,6,13-14,25H2
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n/an/a 326n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151106
PNG
(US8987273, 4-13)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2c(cnc2cc1-c1ccccc1)-c1ccc(O)nc1
Show InChI InChI=1S/C27H23N5O/c28-27(13-4-14-27)21-10-7-19(8-11-21)26-22(18-5-2-1-3-6-18)15-24-29-17-23(32(24)31-26)20-9-12-25(33)30-16-20/h1-3,5-12,15-17H,4,13-14,28H2,(H,30,33)
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n/an/a 431n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151091
PNG
(US8987273, 2-0)
Show SMILES Cc1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C23H22N4/c1-16-15-25-21-14-20(17-6-3-2-4-7-17)22(26-27(16)21)18-8-10-19(11-9-18)23(24)12-5-13-23/h2-4,6-11,14-15H,5,12-13,24H2,1H3
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n/an/a 441n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM50384861
PNG
(CHEMBL2035019)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nn2ccnc2cc1-c1ccccc1
Show InChI InChI=1S/C22H20N4/c23-22(11-4-12-22)18-9-7-17(8-10-18)21-19(16-5-2-1-3-6-16)15-20-24-13-14-26(20)25-21/h1-3,5-10,13-15H,4,11-12,23H2
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n/an/a 1.44E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151091
PNG
(US8987273, 2-0)
Show SMILES Cc1cnc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C23H22N4/c1-16-15-25-21-14-20(17-6-3-2-4-7-17)22(26-27(16)21)18-8-10-19(11-9-18)23(24)12-5-13-23/h2-4,6-11,14-15H,5,12-13,24H2,1H3
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n/an/a 1.73E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151117
PNG
(US8987273, 5-5)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccn[nH]1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C26H24N6/c1-17-25(22-12-15-28-30-22)32-23(29-17)16-21(18-6-3-2-4-7-18)24(31-32)19-8-10-20(11-9-19)26(27)13-5-14-26/h2-4,6-12,15-16H,5,13-14,27H2,1H3,(H,28,30)
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n/an/a 2.73E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151115
PNG
(US8987273, 5-3)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(F)cc1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25FN4/c1-19-28(22-10-14-24(30)15-11-22)34-26(32-19)18-25(20-6-3-2-4-7-20)27(33-34)21-8-12-23(13-9-21)29(31)16-5-17-29/h2-4,6-15,18H,5,16-17,31H2,1H3
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n/an/a 4.43E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151114
PNG
(US8987273, 5-2)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1cn[nH]c1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C26H24N6/c1-17-25(20-15-28-29-16-20)32-23(30-17)14-22(18-6-3-2-4-7-18)24(31-32)19-8-10-21(11-9-19)26(27)12-5-13-26/h2-4,6-11,14-16H,5,12-13,27H2,1H3,(H,28,29)
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n/an/a 4.78E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151116
PNG
(US8987273, 5-4)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(cc1)C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O/c1-19-28(22-8-10-23(11-9-22)29(31)36)35-26(33-19)18-25(20-6-3-2-4-7-20)27(34-35)21-12-14-24(15-13-21)30(32)16-5-17-30/h2-4,6-15,18H,5,16-17,32H2,1H3,(H2,31,36)
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n/an/a 4.82E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151115
PNG
(US8987273, 5-3)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(F)cc1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C29H25FN4/c1-19-28(22-10-14-24(30)15-11-22)34-26(32-19)18-25(20-6-3-2-4-7-20)27(33-34)21-8-12-23(13-9-21)29(31)16-5-17-29/h2-4,6-15,18H,5,16-17,31H2,1H3
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n/an/a 5.11E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151117
PNG
(US8987273, 5-5)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccn[nH]1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C26H24N6/c1-17-25(22-12-15-28-30-22)32-23(29-17)16-21(18-6-3-2-4-7-18)24(31-32)19-8-10-20(11-9-19)26(27)13-5-14-26/h2-4,6-12,15-16H,5,13-14,27H2,1H3,(H,28,30)
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n/an/a 5.23E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151124
PNG
(US8987273, 11-0)
Show SMILES COC(=O)\C=C\c1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C27H26N4O2/c1-18-23(13-14-25(32)33-2)31-24(29-18)17-22(19-7-4-3-5-8-19)26(30-31)20-9-11-21(12-10-20)27(28)15-6-16-27/h3-5,7-14,17H,6,15-16,28H2,1-2H3/b14-13+
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n/an/a 5.97E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151125
PNG
(US8987273, 12-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1C=C)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H24N4/c1-3-22-17(2)27-23-16-21(18-8-5-4-6-9-18)24(28-29(22)23)19-10-12-20(13-11-19)25(26)14-7-15-25/h3-6,8-13,16H,1,7,14-15,26H2,2H3
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n/an/a 8.94E+3n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151113
PNG
(US8987273, 5-1)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(F)c(CO)c1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27FN4O/c1-19-29(22-10-13-26(31)23(16-22)18-36)35-27(33-19)17-25(20-6-3-2-4-7-20)28(34-35)21-8-11-24(12-9-21)30(32)14-5-15-30/h2-4,6-13,16-17,36H,5,14-15,18,32H2,1H3
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n/an/a 1.01E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151124
PNG
(US8987273, 11-0)
Show SMILES COC(=O)\C=C\c1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C27H26N4O2/c1-18-23(13-14-25(32)33-2)31-24(29-18)17-22(19-7-4-3-5-8-19)26(30-31)20-9-11-21(12-10-20)27(28)15-6-16-27/h3-5,7-14,17H,6,15-16,28H2,1-2H3/b14-13+
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n/an/a 1.01E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151116
PNG
(US8987273, 5-4)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(cc1)C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O/c1-19-28(22-8-10-23(11-9-22)29(31)36)35-26(33-19)18-25(20-6-3-2-4-7-20)27(34-35)21-12-14-24(15-13-21)30(32)16-5-17-30/h2-4,6-15,18H,5,16-17,32H2,1H3,(H2,31,36)
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n/an/a 1.21E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151118
PNG
(US8987273, 5-6)
Show SMILES Cc1cc([nH]n1)-c1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C27H26N6/c1-17-15-23(31-30-17)26-18(2)29-24-16-22(19-7-4-3-5-8-19)25(32-33(24)26)20-9-11-21(12-10-20)27(28)13-6-14-27/h3-5,7-12,15-16H,6,13-14,28H2,1-2H3,(H,30,31)
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n/an/a 1.49E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151112
PNG
(US8987273, 5-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1cccc(c1)C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O/c1-19-28(22-9-5-10-23(17-22)29(31)36)35-26(33-19)18-25(20-7-3-2-4-8-20)27(34-35)21-11-13-24(14-12-21)30(32)15-6-16-30/h2-5,7-14,17-18H,6,15-16,32H2,1H3,(H2,31,36)
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n/an/a 1.50E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151125
PNG
(US8987273, 12-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1C=C)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H24N4/c1-3-22-17(2)27-23-16-21(18-8-5-4-6-9-18)24(28-29(22)23)19-10-12-20(13-11-19)25(26)14-7-15-25/h3-6,8-13,16H,1,7,14-15,26H2,2H3
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n/an/a 1.67E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151113
PNG
(US8987273, 5-1)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1ccc(F)c(CO)c1)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27FN4O/c1-19-29(22-10-13-26(31)23(16-22)18-36)35-27(33-19)17-25(20-6-3-2-4-7-20)28(34-35)21-8-11-24(12-9-21)30(32)14-5-15-30/h2-4,6-13,16-17,36H,5,14-15,18,32H2,1H3
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n/an/a 1.67E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151112
PNG
(US8987273, 5-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1-c1cccc(c1)C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C30H27N5O/c1-19-28(22-9-5-10-23(17-22)29(31)36)35-26(33-19)18-25(20-7-3-2-4-8-20)27(34-35)21-11-13-24(14-12-21)30(32)15-6-16-30/h2-5,7-14,17-18H,6,15-16,32H2,1H3,(H2,31,36)
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n/an/a 1.68E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151118
PNG
(US8987273, 5-6)
Show SMILES Cc1cc([nH]n1)-c1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C27H26N6/c1-17-15-23(31-30-17)26-18(2)29-24-16-22(19-7-4-3-5-8-19)25(32-33(24)26)20-9-11-21(12-10-20)27(28)13-6-14-27/h3-5,7-12,15-16H,6,13-14,28H2,1-2H3,(H,30,31)
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n/an/a 1.72E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151090
PNG
(US8987273, 1-1)
Show SMILES Cc1cn2nc(-c3ccc(cc3)C3(N)CCC3)c(cc2n1)-c1ccccc1
Show InChI InChI=1S/C23H22N4/c1-16-15-27-21(25-16)14-20(17-6-3-2-4-7-17)22(26-27)18-8-10-19(11-9-18)23(24)12-5-13-23/h2-4,6-11,14-15H,5,12-13,24H2,1H3
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n/an/a 1.73E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151123
PNG
(US8987273, 10-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1\C=C\C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C26H25N5O/c1-17-22(12-13-23(27)32)31-24(29-17)16-21(18-6-3-2-4-7-18)25(30-31)19-8-10-20(11-9-19)26(28)14-5-15-26/h2-4,6-13,16H,5,14-15,28H2,1H3,(H2,27,32)/b13-12+
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n/an/a 1.80E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151126
PNG
(US8987273, 13-0)
Show SMILES CCc1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H26N4/c1-3-22-17(2)27-23-16-21(18-8-5-4-6-9-18)24(28-29(22)23)19-10-12-20(13-11-19)25(26)14-7-15-25/h4-6,8-13,16H,3,7,14-15,26H2,1-2H3
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n/an/a 2.00E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151090
PNG
(US8987273, 1-1)
Show SMILES Cc1cn2nc(-c3ccc(cc3)C3(N)CCC3)c(cc2n1)-c1ccccc1
Show InChI InChI=1S/C23H22N4/c1-16-15-27-21(25-16)14-20(17-6-3-2-4-7-17)22(26-27)18-8-10-19(11-9-18)23(24)12-5-13-23/h2-4,6-11,14-15H,5,12-13,24H2,1H3
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n/an/a 2.00E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-beta serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151123
PNG
(US8987273, 10-0)
Show SMILES Cc1nc2cc(-c3ccccc3)c(nn2c1\C=C\C(N)=O)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C26H25N5O/c1-17-22(12-13-23(27)32)31-24(29-17)16-21(18-6-3-2-4-7-18)25(30-31)19-8-10-20(11-9-19)26(28)14-5-15-26/h2-4,6-13,16H,5,14-15,28H2,1H3,(H2,27,32)/b13-12+
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n/an/a 2.00E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt2 inhibitory activity of compounds of the present invention was quantified employing the Akt2 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
RAC-alpha serine/threonine-protein kinase


(Homo sapiens (Human))		BDBM151126
PNG
(US8987273, 13-0)
Show SMILES CCc1c(C)nc2cc(-c3ccccc3)c(nn12)-c1ccc(cc1)C1(N)CCC1
Show InChI InChI=1S/C25H26N4/c1-3-22-17(2)27-23-16-21(18-8-5-4-6-9-18)24(28-29(22)23)19-10-12-20(13-11-19)25(26)14-7-15-25/h4-6,8-13,16H,3,7,14-15,26H2,1-2H3
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n/an/a 2.00E+4n/an/an/an/a7.522



Bayer Intellectual Property GmbH

US Patent


Assay Description
Akt1 inhibitory activity of compounds of the present invention was quantified employing the Akt1 TR-FRET assay as described in the following paragrap...

US Patent US8987273 (2015)


BindingDB Entry DOI: 10.7270/Q2CZ35WJ
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%