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Patent code US9492453

Compile Data Set for Download or QSAR
Found 77 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
AKT/p21CIP1


(Homo sapiens (human))
BDBM256830
PNG
(US9492453, 6)
Show SMILES C[C@H](NC(=O)C1(CN)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-14(15-2-4-16(22)5-3-15)27-20(29)21(12-23)7-10-28(11-8-21)19-17-6-9-24-18(17)25-13-26-19/h2-6,9,13-14H,7-8,10-12,23H2,1H3,(H,27,29)(H,24,25,26)/t14-/m0/s1
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n/an/a 1.20n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256843
PNG
(US9492453, 23)
Show SMILES NCC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c23-16-3-1-15(2-4-16)18(6-12-30)28-21(31)22(13-24)7-10-29(11-8-22)20-17-5-9-25-19(17)26-14-27-20/h1-5,9,14,18,30H,6-8,10-13,24H2,(H,28,31)(H,25,26,27)/t18-/m0/s1
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n/an/a 1.30n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427336
PNG
(CHEMBL2325992 | US9492453, 11)
Show SMILES CN(C)CCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H30ClN7O/c1-30(2)12-8-19(16-3-5-17(24)6-4-16)29-22(32)23(25)9-13-31(14-10-23)21-18-7-11-26-20(18)27-15-28-21/h3-7,11,15,19H,8-10,12-14,25H2,1-2H3,(H,29,32)(H,26,27,28)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256844
PNG
(US9492453, 24)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCO)c1ccc(Br)cc1
Show InChI InChI=1S/C21H25BrN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256828
PNG
(US9492453, 3A)
Show SMILES CC[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-2-17(14-3-5-15(22)6-4-14)27-20(29)21(23)8-11-28(12-9-21)19-16-7-10-24-18(16)25-13-26-19/h3-7,10,13,17H,2,8-9,11-12,23H2,1H3,(H,27,29)(H,24,25,26)/t17-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256833
PNG
(US9492453, 12)
Show SMILES NCC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c23-16-3-1-15(2-4-16)18(6-12-30)28-21(31)22(13-24)7-10-29(11-8-22)20-17-5-9-25-19(17)26-14-27-20/h1-5,9,14,18,30H,6-8,10-13,24H2,(H,28,31)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427361
PNG
(CHEMBL2325727 | US9492453, 11A)
Show SMILES CN(C)CC[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H30ClN7O/c1-30(2)12-8-19(16-3-5-17(24)6-4-16)29-22(32)23(25)9-13-31(14-10-23)21-18-7-11-26-20(18)27-15-28-21/h3-7,11,15,19H,8-10,12-14,25H2,1-2H3,(H,29,32)(H,26,27,28)/t19-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427335
PNG
(CHEMBL2325993 | US9492453, 25)
Show SMILES CN(C)CCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C24H32ClN7O/c1-31(2)13-3-4-20(17-5-7-18(25)8-6-17)30-23(33)24(26)10-14-32(15-11-24)22-19-9-12-27-21(19)28-16-29-22/h5-9,12,16,20H,3-4,10-11,13-15,26H2,1-2H3,(H,30,33)(H,27,28,29)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256835
PNG
(US9492453, 14)
Show SMILES NCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H26ClN7O/c22-15-3-1-14(2-4-15)17(5-9-23)28-20(30)21(24)7-11-29(12-8-21)19-16-6-10-25-18(16)26-13-27-19/h1-4,6,10,13,17H,5,7-9,11-12,23-24H2,(H,28,30)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256836
PNG
(BDBM50427349 | US9492453, 15)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256861
PNG
(US9492453, 49A)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@H](CCCN1CCCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C27H36ClN7O/c28-21-8-6-20(7-9-21)23(5-4-16-34-14-2-1-3-15-34)33-26(36)27(29)11-17-35(18-12-27)25-22-10-13-30-24(22)31-19-32-25/h6-10,13,19,23H,1-5,11-12,14-18,29H2,(H,33,36)(H,30,31,32)/t23-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256865
PNG
(US9492453, 54)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCn1ccnc1)c1ccc(Cl)cc1
Show InChI InChI=1S/C24H27ClN8O/c25-18-3-1-17(2-4-18)20(6-11-32-14-10-27-16-32)31-23(34)24(26)7-12-33(13-8-24)22-19-5-9-28-21(19)29-15-30-22/h1-5,9-10,14-16,20H,6-8,11-13,26H2,(H,31,34)(H,28,29,30)/t20-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427334
PNG
(CHEMBL2325994 | US9492453, 47)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCCN1CCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C26H34ClN7O/c27-20-7-5-19(6-8-20)22(4-3-15-33-13-1-2-14-33)32-25(35)26(28)10-16-34(17-11-26)24-21-9-12-29-23(21)30-18-31-24/h5-9,12,18,22H,1-4,10-11,13-17,28H2,(H,32,35)(H,29,30,31)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427360
PNG
(CHEMBL2325729 | US9492453, 52)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCN1CCCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C26H34ClN7O/c27-20-6-4-19(5-7-20)22(9-15-33-13-2-1-3-14-33)32-25(35)26(28)10-16-34(17-11-26)24-21-8-12-29-23(21)30-18-31-24/h4-8,12,18,22H,1-3,9-11,13-17,28H2,(H,32,35)(H,29,30,31)/t22-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427347
PNG
(CHEMBL2325743 | US9492453, 2)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H23ClN6O/c1-13(14-2-4-15(21)5-3-14)26-19(28)20(22)7-10-27(11-8-20)18-16-6-9-23-17(16)24-12-25-18/h2-6,9,12-13H,7-8,10-11,22H2,1H3,(H,26,28)(H,23,24,25)/t13-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427331
PNG
(CHEMBL2325728 | US9492453, 55)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCN1CCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C25H32ClN7O/c26-19-5-3-18(4-6-19)21(8-14-32-12-1-2-13-32)31-24(34)25(27)9-15-33(16-10-25)23-20-7-11-28-22(20)29-17-30-23/h3-7,11,17,21H,1-2,8-10,12-16,27H2,(H,31,34)(H,28,29,30)/t21-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256852
PNG
(US9492453, 35)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]cc(Br)c12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H22BrClN6O/c1-12(13-2-4-14(22)5-3-13)27-19(29)20(23)6-8-28(9-7-20)18-16-15(21)10-24-17(16)25-11-26-18/h2-5,10-12H,6-9,23H2,1H3,(H,27,29)(H,24,25,26)/t12-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256832
PNG
(US9492453, 10)
Show SMILES CC(=O)NCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H28ClN7O2/c1-15(32)26-11-7-19(16-2-4-17(24)5-3-16)30-22(33)23(25)8-12-31(13-9-23)21-18-6-10-27-20(18)28-14-29-21/h2-6,10,14,19H,7-9,11-13,25H2,1H3,(H,26,32)(H,30,33)(H,27,28,29)
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n/an/a 4.20n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256834
PNG
(US9492453, 13)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256862
PNG
(US9492453, 50)
Show SMILES CN1CCN(CC[C@H](NC(=O)C2(N)CCN(CC2)c2ncnc3[nH]ccc23)c2ccc(Cl)cc2)CC1
Show InChI InChI=1S/C26H35ClN8O/c1-33-14-16-34(17-15-33)11-7-22(19-2-4-20(27)5-3-19)32-25(36)26(28)8-12-35(13-9-26)24-21-6-10-29-23(21)30-18-31-24/h2-6,10,18,22H,7-9,11-17,28H2,1H3,(H,32,36)(H,29,30,31)/t22-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256847
PNG
(US9492453, 28)
Show SMILES CNCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H28ClN7O/c1-25-10-7-18(15-2-4-16(23)5-3-15)29-21(31)22(24)8-12-30(13-9-22)20-17-6-11-26-19(17)27-14-28-20/h2-6,11,14,18,25H,7-10,12-13,24H2,1H3,(H,29,31)(H,26,27,28)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256831
PNG
(US9492453, 7A)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c23-16-5-3-15(4-6-16)18(2-1-13-30)28-21(31)22(24)8-11-29(12-9-22)20-17-7-10-25-19(17)26-14-27-20/h3-7,10,14,18,30H,1-2,8-9,11-13,24H2,(H,28,31)(H,25,26,27)/t18-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427332
PNG
(CHEMBL2325996 | US9492453, 49)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCCN1CCCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C27H36ClN7O/c28-21-8-6-20(7-9-21)23(5-4-16-34-14-2-1-3-15-34)33-26(36)27(29)11-17-35(18-12-27)25-22-10-13-30-24(22)31-19-32-25/h6-10,13,19,23H,1-5,11-12,14-18,29H2,(H,33,36)(H,30,31,32)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427345
PNG
(CHEMBL2325983 | US9492453, 4)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(C1CC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H25ClN6O/c23-16-5-3-15(4-6-16)18(14-1-2-14)28-21(30)22(24)8-11-29(12-9-22)20-17-7-10-25-19(17)26-13-27-20/h3-7,10,13-14,18H,1-2,8-9,11-12,24H2,(H,28,30)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256855
PNG
(US9492453, 38)
Show SMILES CC(C)(O)C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H29ClN6O2/c1-22(2,32)13-18(15-3-5-16(24)6-4-15)29-21(31)23(25)8-11-30(12-9-23)20-17-7-10-26-19(17)27-14-28-20/h3-7,10,14,18,32H,8-9,11-13,25H2,1-2H3,(H,29,31)(H,26,27,28)/t18-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256845
PNG
(US9492453, 26)
Show SMILES CCN(CC)CC[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C25H34ClN7O/c1-3-32(4-2)14-10-21(18-5-7-19(26)8-6-18)31-24(34)25(27)11-15-33(16-12-25)23-20-9-13-28-22(20)29-17-30-23/h5-9,13,17,21H,3-4,10-12,14-16,27H2,1-2H3,(H,31,34)(H,28,29,30)/t21-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427333
PNG
(CHEMBL2325995 | US9492453, 48)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCCN1CCOCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C26H34ClN7O2/c27-20-5-3-19(4-6-20)22(2-1-11-33-14-16-36-17-15-33)32-25(35)26(28)8-12-34(13-9-26)24-21-7-10-29-23(21)30-18-31-24/h3-7,10,18,22H,1-2,8-9,11-17,28H2,(H,32,35)(H,29,30,31)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427351
PNG
(CHEMBL2325739 | US9492453, 7)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c23-16-5-3-15(4-6-16)18(2-1-13-30)28-21(31)22(24)8-11-29(12-9-22)20-17-7-10-25-19(17)26-14-27-20/h3-7,10,14,18,30H,1-2,8-9,11-13,24H2,(H,28,31)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256866
PNG
(US9492453, 59)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(Cc1ncc[nH]1)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H25ClN8O/c24-16-3-1-15(2-4-16)18(13-19-26-9-10-27-19)31-22(33)23(25)6-11-32(12-7-23)21-17-5-8-28-20(17)29-14-30-21/h1-5,8-10,14,18H,6-7,11-13,25H2,(H,26,27)(H,31,33)(H,28,29,30)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256864
PNG
(US9492453, 53)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCN1CCNCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C25H33ClN8O/c26-19-3-1-18(2-4-19)21(6-12-33-15-10-28-11-16-33)32-24(35)25(27)7-13-34(14-8-25)23-20-5-9-29-22(20)30-17-31-23/h1-5,9,17,21,28H,6-8,10-16,27H2,(H,32,35)(H,29,30,31)/t21-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427355
PNG
(CHEMBL2325734 | US9492453, 65)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CCS(N)(=O)=O)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H26ClN7O3S/c22-15-3-1-14(2-4-15)17(6-12-33(24,31)32)28-20(30)21(23)7-10-29(11-8-21)19-16-5-9-25-18(16)26-13-27-19/h1-5,9,13,17H,6-8,10-12,23H2,(H,28,30)(H2,24,31,32)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256870
PNG
(US9492453, 66)
Show SMILES NC(=O)CC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H24ClN7O2/c22-14-3-1-13(2-4-14)16(11-17(23)30)28-20(31)21(24)6-9-29(10-7-21)19-15-5-8-25-18(15)26-12-27-19/h1-5,8,12,16H,6-7,9-11,24H2,(H2,23,30)(H,28,31)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427346
PNG
(CHEMBL2325982 | US9492453, 3)
Show SMILES CCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-2-17(14-3-5-15(22)6-4-14)27-20(29)21(23)8-11-28(12-9-21)19-16-7-10-24-18(16)25-13-26-19/h3-7,10,13,17H,2,8-9,11-12,23H2,1H3,(H,27,29)(H,24,25,26)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427353
PNG
(CHEMBL2325736 | US9492453, 69)
Show SMILES CS(=O)(=O)NCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H28ClN7O3S/c1-34(32,33)28-11-7-18(15-2-4-16(23)5-3-15)29-21(31)22(24)8-12-30(13-9-22)20-17-6-10-25-19(17)26-14-27-20/h2-6,10,14,18,28H,7-9,11-13,24H2,1H3,(H,29,31)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427352
PNG
(CHEMBL2325737 | US9492453, 8)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CO)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H23ClN6O2/c21-14-3-1-13(2-4-14)16(11-28)26-19(29)20(22)6-9-27(10-7-20)18-15-5-8-23-17(15)24-12-25-18/h1-5,8,12,16,28H,6-7,9-11,22H2,(H,26,29)(H,23,24,25)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256842
PNG
(US9492453, 22)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]cnc12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H24ClN7O2/c21-14-3-1-13(2-4-14)15(5-10-29)27-19(30)20(22)6-8-28(9-7-20)18-16-17(24-11-23-16)25-12-26-18/h1-4,11-12,15,29H,5-10,22H2,(H,27,30)(H,23,24,25,26)/t15-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256827
PNG
(US9492453, 1)
Show SMILES CC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H23ClN6O/c1-13(14-2-4-15(21)5-3-14)26-19(28)20(22)7-10-27(11-8-20)18-16-6-9-23-17(16)24-12-25-18/h2-6,9,12-13H,7-8,10-11,22H2,1H3,(H,26,28)(H,23,24,25)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256871
PNG
(US9492453, 67)
Show SMILES NC(=O)NCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN8O2/c23-15-3-1-14(2-4-15)17(6-10-27-21(24)33)30-20(32)22(25)7-11-31(12-8-22)19-16-5-9-26-18(16)28-13-29-19/h1-5,9,13,17H,6-8,10-12,25H2,(H,30,32)(H3,24,27,33)(H,26,28,29)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427341
PNG
(CHEMBL2325987 | US9492453, 44)
Show SMILES CC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(F)cc1
Show InChI InChI=1S/C20H23FN6O/c1-13(14-2-4-15(21)5-3-14)26-19(28)20(22)7-10-27(11-8-20)18-16-6-9-23-17(16)24-12-25-18/h2-6,9,12-13H,7-8,10-11,22H2,1H3,(H,26,28)(H,23,24,25)
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n/an/a 8.90n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256851
PNG
(US9492453, 34)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]cc(Cl)c12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H24Cl2N6O2/c22-14-3-1-13(2-4-14)16(5-10-30)28-20(31)21(24)6-8-29(9-7-21)19-17-15(23)11-25-18(17)26-12-27-19/h1-4,11-12,16,30H,5-10,24H2,(H,28,31)(H,25,26,27)/t16-/m0/s1
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n/an/a 9.20n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427350
PNG
(CHEMBL2325740 | US9492453, 64)
Show SMILES COCCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c1-31-13-7-18(15-2-4-16(23)5-3-15)28-21(30)22(24)8-11-29(12-9-22)20-17-6-10-25-19(17)26-14-27-20/h2-6,10,14,18H,7-9,11-13,24H2,1H3,(H,28,30)(H,25,26,27)
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n/an/a 9.5n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256829
PNG
(US9492453, 5)
Show SMILES NCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H24ClN7O/c21-14-3-1-13(2-4-14)16(11-22)27-19(29)20(23)6-9-28(10-7-20)18-15-5-8-24-17(15)25-12-26-18/h1-5,8,12,16H,6-7,9-11,22-23H2,(H,27,29)(H,24,25,26)
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n/an/a 9.70n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256863
PNG
(US9492453, 51)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCN1CCOCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C25H32ClN7O2/c26-19-3-1-18(2-4-19)21(6-10-32-13-15-35-16-14-32)31-24(34)25(27)7-11-33(12-8-25)23-20-5-9-28-22(20)29-17-30-23/h1-5,9,17,21H,6-8,10-16,27H2,(H,31,34)(H,28,29,30)/t21-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256839
PNG
(US9492453, 19)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]cc(Br)c12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H24BrClN6O2/c22-15-11-25-18-17(15)19(27-12-26-18)29-8-6-21(24,7-9-29)20(31)28-16(5-10-30)13-1-3-14(23)4-2-13/h1-4,11-12,16,30H,5-10,24H2,(H,28,31)(H,25,26,27)/t16-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256837
PNG
(US9492453, 17)
Show SMILES C[C@@H](NC(=O)C1(CN)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-14(15-2-4-16(22)5-3-15)27-20(29)21(12-23)7-10-28(11-8-21)19-17-6-9-24-18(17)25-13-26-19/h2-6,9,13-14H,7-8,10-12,23H2,1H3,(H,27,29)(H,24,25,26)/t14-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427356
PNG
(CHEMBL2325733 | US9492453, 57)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CS(N)(=O)=O)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H24ClN7O3S/c21-14-3-1-13(2-4-14)16(11-32(23,30)31)27-19(29)20(22)6-9-28(10-7-20)18-15-5-8-24-17(15)25-12-26-18/h1-5,8,12,16H,6-7,9-11,22H2,(H,27,29)(H2,23,30,31)(H,24,25,26)
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n/an/a 12n/an/an/an/an/an/a



AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256872
PNG
(US9492453, 68)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(CC#N)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H22ClN7O/c22-15-3-1-14(2-4-15)17(5-9-23)28-20(30)21(24)7-11-29(12-8-21)19-16-6-10-25-18(16)26-13-27-19/h1-4,6,10,13,17H,5,7-8,11-12,24H2,(H,28,30)(H,25,26,27)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256849
PNG
(US9492453, 32)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]cc(Cl)c12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H22Cl2N6O/c1-12(13-2-4-14(21)5-3-13)27-19(29)20(23)6-8-28(9-7-20)18-16-15(22)10-24-17(16)25-11-26-18/h2-5,10-12H,6-9,23H2,1H3,(H,27,29)(H,24,25,26)/t12-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256850
PNG
(US9492453, 33)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]nc(Br)c12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H23BrClN7O2/c21-16-15-17(28-27-16)24-11-25-18(15)29-8-6-20(23,7-9-29)19(31)26-14(5-10-30)12-1-3-13(22)4-2-12/h1-4,11,14,30H,5-10,23H2,(H,26,31)(H,24,25,27,28)/t14-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256853
PNG
(US9492453, 36)
Show SMILES Cc1c[nH]c2ncnc(N3CCC(N)(CC3)C(=O)N[C@@H](CCO)c3ccc(Cl)cc3)c12
Show InChI InChI=1S/C22H27ClN6O2/c1-14-12-25-19-18(14)20(27-13-26-19)29-9-7-22(24,8-10-29)21(31)28-17(6-11-30)15-2-4-16(23)5-3-15/h2-5,12-13,17,30H,6-11,24H2,1H3,(H,28,31)(H,25,26,27)/t17-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256838
PNG
(US9492453, 18)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCO)c1ccc(cc1)C#N
Show InChI InChI=1S/C22H25N7O2/c23-13-15-1-3-16(4-2-15)18(6-12-30)28-21(31)22(24)7-10-29(11-8-22)20-17-5-9-25-19(17)26-14-27-20/h1-5,9,14,18,30H,6-8,10-12,24H2,(H,28,31)(H,25,26,27)/t18-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256858
PNG
(US9492453, 41)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C21H23F3N6O/c1-13(14-2-4-15(5-3-14)21(22,23)24)29-19(31)20(25)7-10-30(11-8-20)18-16-6-9-26-17(16)27-12-28-18/h2-6,9,12-13H,7-8,10-11,25H2,1H3,(H,29,31)(H,26,27,28)/t13-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256846
PNG
(US9492453, 27)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]cc(C3CC3)c12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C24H29ClN6O2/c25-17-5-3-16(4-6-17)19(7-12-32)30-23(33)24(26)8-10-31(11-9-24)22-20-18(15-1-2-15)13-27-21(20)28-14-29-22/h3-6,13-15,19,32H,1-2,7-12,26H2,(H,30,33)(H,27,28,29)/t19-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427354
PNG
(CHEMBL2325735 | US9492453, 56)
Show SMILES CS(=O)(=O)NCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H26ClN7O3S/c1-33(31,32)27-12-17(14-2-4-15(22)5-3-14)28-20(30)21(23)7-10-29(11-8-21)19-16-6-9-24-18(16)25-13-26-19/h2-6,9,13,17,27H,7-8,10-12,23H2,1H3,(H,28,30)(H,24,25,26)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256854
PNG
(US9492453, 37)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]cc(C)c12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-13-11-24-18-17(13)19(26-12-25-18)28-9-7-21(23,8-10-28)20(29)27-14(2)15-3-5-16(22)6-4-15/h3-6,11-12,14H,7-10,23H2,1-2H3,(H,27,29)(H,24,25,26)/t14-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256840
PNG
(US9492453, 20)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ncc12)C(=O)N[C@@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H24ClN7O2/c21-14-3-1-13(2-4-14)16(5-10-29)26-19(30)20(22)6-8-28(9-7-20)18-15-11-25-27-17(15)23-12-24-18/h1-4,11-12,16,29H,5-10,22H2,(H,26,30)(H,23,24,25,27)/t16-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256875
PNG
(US9492453, 11B)
Show SMILES CN(C)CC[C@@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H30ClN7O/c1-30(2)12-8-19(16-3-5-17(24)6-4-16)29-22(32)23(25)9-13-31(14-10-23)21-18-7-11-26-20(18)27-15-28-21/h3-7,11,15,19H,8-10,12-14,25H2,1-2H3,(H,29,32)(H,26,27,28)/t19-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256867
PNG
(US9492453, 60)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(Cn1cccn1)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H25ClN8O/c24-17-4-2-16(3-5-17)19(14-32-11-1-9-29-32)30-22(33)23(25)7-12-31(13-8-23)21-18-6-10-26-20(18)27-15-28-21/h1-6,9-11,15,19H,7-8,12-14,25H2,(H,30,33)(H,26,27,28)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256868
PNG
(US9492453, 61)
Show SMILES Cc1cc(CC(NC(=O)C2(N)CCN(CC2)c2ncnc3[nH]ccc23)c2ccc(Cl)cc2)on1
Show InChI InChI=1S/C24H26ClN7O2/c1-15-12-18(34-31-15)13-20(16-2-4-17(25)5-3-16)30-23(33)24(26)7-10-32(11-8-24)22-19-6-9-27-21(19)28-14-29-22/h2-6,9,12,14,20H,7-8,10-11,13,26H2,1H3,(H,30,33)(H,27,28,29)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256848
PNG
(US9492453, 31)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]nc(Br)c12)c1ccc(Cl)cc1
Show InChI InChI=1S/C19H21BrClN7O/c1-11(12-2-4-13(21)5-3-12)25-18(29)19(22)6-8-28(9-7-19)17-14-15(20)26-27-16(14)23-10-24-17/h2-5,10-11H,6-9,22H2,1H3,(H,25,29)(H,23,24,26,27)/t11-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256869
PNG
(US9492453, 62)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(Cc1nccs1)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H24ClN7OS/c24-16-3-1-15(2-4-16)18(13-19-26-9-12-33-19)30-22(32)23(25)6-10-31(11-7-23)21-17-5-8-27-20(17)28-14-29-21/h1-5,8-9,12,14,18H,6-7,10-11,13,25H2,(H,30,32)(H,27,28,29)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427359
PNG
(CHEMBL2325730 | US9492453, 30)
Show SMILES NC(=O)C(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H22ClN7O2/c21-13-3-1-12(2-4-13)15(16(22)29)27-19(30)20(23)6-9-28(10-7-20)18-14-5-8-24-17(14)25-11-26-18/h1-5,8,11,15H,6-7,9-10,23H2,(H2,22,29)(H,27,30)(H,24,25,26)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427343
PNG
(CHEMBL2325985 | US9492453, 43)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(Cc1ccccc1)c1ccc(Cl)cc1
Show InChI InChI=1S/C26H27ClN6O/c27-20-8-6-19(7-9-20)22(16-18-4-2-1-3-5-18)32-25(34)26(28)11-14-33(15-12-26)24-21-10-13-29-23(21)30-17-31-24/h1-10,13,17,22H,11-12,14-16,28H2,(H,32,34)(H,29,30,31)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427357
PNG
(CHEMBL2325732 | US9492453, 58)
Show SMILES CC(=O)NCC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H26ClN7O2/c1-14(31)26-12-18(15-2-4-16(23)5-3-15)29-21(32)22(24)7-10-30(11-8-22)20-17-6-9-25-19(17)27-13-28-20/h2-6,9,13,18H,7-8,10-12,24H2,1H3,(H,26,31)(H,29,32)(H,25,27,28)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256859
PNG
(US9492453, 42)
Show SMILES C[C@@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Br)cc1
Show InChI InChI=1S/C20H23BrN6O/c1-13(14-2-4-15(21)5-3-14)26-19(28)20(22)7-10-27(11-8-20)18-16-6-9-23-17(16)24-12-25-18/h2-6,9,12-13H,7-8,10-11,22H2,1H3,(H,26,28)(H,23,24,25)/t13-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256857
PNG
(US9492453, 40)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCO)c1cccc(Cl)c1
Show InChI InChI=1S/C21H25ClN6O2/c22-15-3-1-2-14(12-15)17(5-11-29)27-20(30)21(23)6-9-28(10-7-21)19-16-4-8-24-18(16)25-13-26-19/h1-4,8,12-13,17,29H,5-7,9-11,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427344
PNG
(CHEMBL2325984 | US9492453, 29)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(c1ccccc1)c1ccc(Cl)cc1
Show InChI InChI=1S/C25H25ClN6O/c26-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)31-24(33)25(27)11-14-32(15-12-25)23-20-10-13-28-22(20)29-16-30-23/h1-10,13,16,21H,11-12,14-15,27H2,(H,31,33)(H,28,29,30)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427358
PNG
(CHEMBL2325731 | US9492453, 63)
Show SMILES CN(C)C(=O)CC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C23H28ClN7O2/c1-30(2)19(32)13-18(15-3-5-16(24)6-4-15)29-22(33)23(25)8-11-31(12-9-23)21-17-7-10-26-20(17)27-14-28-21/h3-7,10,14,18H,8-9,11-13,25H2,1-2H3,(H,29,33)(H,26,27,28)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256876
PNG
(US9492453, 49B)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCCN1CCCCC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C27H36ClN7O/c28-21-8-6-20(7-9-21)23(5-4-16-34-14-2-1-3-15-34)33-26(36)27(29)11-17-35(18-12-27)25-22-10-13-30-24(22)31-19-32-25/h6-10,13,19,23H,1-5,11-12,14-18,29H2,(H,33,36)(H,30,31,32)/t23-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256856
PNG
(US9492453, 39)
Show SMILES C[C@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(cc1)C#N
Show InChI InChI=1S/C21H23N7O/c1-14(16-4-2-15(12-22)3-5-16)27-20(29)21(23)7-10-28(11-8-21)19-17-6-9-24-18(17)25-13-26-19/h2-6,9,13-14H,7-8,10-11,23H2,1H3,(H,27,29)(H,24,25,26)/t14-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256841
PNG
(US9492453, 21)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@@H](CCO)c1ccccc1
Show InChI InChI=1S/C21H26N6O2/c22-21(20(29)26-17(7-13-28)15-4-2-1-3-5-15)8-11-27(12-9-21)19-16-6-10-23-18(16)24-14-25-19/h1-6,10,14,17,28H,7-9,11-13,22H2,(H,26,29)(H,23,24,25)/t17-/m0/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256836
PNG
(BDBM50427349 | US9492453, 15)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@H](CCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427342
PNG
(CHEMBL2325986 | US9492453, 46)
Show SMILES CC(NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccccc1
Show InChI InChI=1S/C20H24N6O/c1-14(15-5-3-2-4-6-15)25-19(27)20(21)8-11-26(12-9-20)18-16-7-10-22-17(16)23-13-24-18/h2-7,10,13-14H,8-9,11-12,21H2,1H3,(H,25,27)(H,22,23,24)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256860
PNG
(US9492453, 45)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)NC(C#N)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H20ClN7O/c21-14-3-1-13(2-4-14)16(11-22)27-19(29)20(23)6-9-28(10-7-20)18-15-5-8-24-17(15)25-12-26-18/h1-5,8,12,16H,6-7,9-10,23H2,(H,27,29)(H,24,25,26)
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256874
PNG
(US9492453, 7B)
Show SMILES NC1(CCN(CC1)c1ncnc2[nH]ccc12)C(=O)N[C@H](CCCO)c1ccc(Cl)cc1
Show InChI InChI=1S/C22H27ClN6O2/c23-16-5-3-15(4-6-16)18(2-1-13-30)28-21(31)22(24)8-11-29(12-9-22)20-17-7-10-25-19(17)26-14-27-20/h3-7,10,14,18,30H,1-2,8-9,11-13,24H2,(H,28,31)(H,25,26,27)/t18-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM256873
PNG
(US9492453, 3B)
Show SMILES CC[C@@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C21H25ClN6O/c1-2-17(14-3-5-15(22)6-4-14)27-20(29)21(23)8-11-28(12-9-21)19-16-7-10-24-18(16)25-13-26-19/h3-7,10,13,17H,2,8-9,11-12,23H2,1H3,(H,27,29)(H,24,25,26)/t17-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
AKT/p21CIP1


(Homo sapiens (human))
BDBM50427348
PNG
(CHEMBL2325742 | US9492453, 16)
Show SMILES C[C@@H](NC(=O)C1(N)CCN(CC1)c1ncnc2[nH]ccc12)c1ccc(Cl)cc1
Show InChI InChI=1S/C20H23ClN6O/c1-13(14-2-4-15(21)5-3-14)26-19(28)20(22)7-10-27(11-8-20)18-16-6-9-23-17(16)24-12-25-18/h2-6,9,12-13H,7-8,10-11,22H2,1H3,(H,26,28)(H,23,24,25)/t13-/m1/s1
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AstraZeneca AB

US Patent


Assay Description
This assay detects inhibitors of AKT1 (PKBα) kinase activity using Caliper LabChip LC3000. The Caliper off-chip incubation mobility shift assay...


Citation and Details
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%