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Patent code US9469639

Compile Data Set for Download or QSAR
Found 14 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
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250510
PNG
(US9469639, Compound (IV))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3cncc4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C24H20N6O/c1-14-5-4-6-15(11-14)27-24(31)28-20-10-9-17(16-7-2-3-8-18(16)20)19-12-26-13-21-22(19)23(25)30-29-21/h2-13H,1H3,(H3,25,29,30)(H2,27,28,31)
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US Patent
n/an/a 4.30n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250511
PNG
(US9469639, Compound (III))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3cncc4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C24H19FN6O/c1-13-6-8-18(25)20(10-13)29-24(32)28-19-9-7-15(14-4-2-3-5-16(14)19)17-11-27-12-21-22(17)23(26)31-30-21/h2-12H,1H3,(H3,26,30,31)(H2,28,29,32)
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n/an/a 5.10n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250510
PNG
(US9469639, Compound (IV))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3cncc4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C24H20N6O/c1-14-5-4-6-15(11-14)27-24(31)28-20-10-9-17(16-7-2-3-8-18(16)20)19-12-26-13-21-22(19)23(25)30-29-21/h2-13H,1H3,(H3,25,29,30)(H2,27,28,31)
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n/an/a 6.70n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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n/an/a 11.1n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250509
PNG
(US9469639, Compound (V))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3ccc(OCCCN4CCCC4)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C32H33FN6O2/c1-20-9-12-25(33)27(19-20)36-32(40)35-26-13-10-22(21-7-2-3-8-23(21)26)24-11-14-28(30-29(24)31(34)38-37-30)41-18-6-17-39-15-4-5-16-39/h2-3,7-14,19H,4-6,15-18H2,1H3,(H3,34,37,38)(H2,35,36,40)
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n/an/a 16.3n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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n/an/a 18.4n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250514
PNG
(US9469639, Compound (VIII))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3ccc(OCCC(C)(C)N)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C30H32N6O2/c1-18-7-6-8-19(17-18)33-29(37)34-24-13-11-21(20-9-4-5-10-22(20)24)23-12-14-25(38-16-15-30(2,3)32)27-26(23)28(31)36-35-27/h4-14,17H,15-16,32H2,1-3H3,(H3,31,35,36)(H2,33,34,37)
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n/an/a 21n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250511
PNG
(US9469639, Compound (III))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3cncc4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C24H19FN6O/c1-13-6-8-18(25)20(10-13)29-24(32)28-19-9-7-15(14-4-2-3-5-16(14)19)17-11-27-12-21-22(17)23(26)31-30-21/h2-12H,1H3,(H3,26,30,31)(H2,28,29,32)
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n/an/a 25.4n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250509
PNG
(US9469639, Compound (V))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3ccc(OCCCN4CCCC4)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C32H33FN6O2/c1-20-9-12-25(33)27(19-20)36-32(40)35-26-13-10-22(21-7-2-3-8-23(21)26)24-11-14-28(30-29(24)31(34)38-37-30)41-18-6-17-39-15-4-5-16-39/h2-3,7-14,19H,4-6,15-18H2,1H3,(H3,34,37,38)(H2,35,36,40)
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n/an/a 30.4n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250512
PNG
(US9469639, Compound (VI))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3ccc(OCCCN4CCCC4)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C32H34N6O2/c1-21-8-6-9-22(20-21)34-32(39)35-27-14-12-24(23-10-2-3-11-25(23)27)26-13-15-28(30-29(26)31(33)37-36-30)40-19-7-18-38-16-4-5-17-38/h2-3,6,8-15,20H,4-5,7,16-19H2,1H3,(H3,33,36,37)(H2,34,35,39)
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n/an/a 45.4n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250512
PNG
(US9469639, Compound (VI))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3ccc(OCCCN4CCCC4)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C32H34N6O2/c1-21-8-6-9-22(20-21)34-32(39)35-27-14-12-24(23-10-2-3-11-25(23)27)26-13-15-28(30-29(26)31(33)37-36-30)40-19-7-18-38-16-4-5-17-38/h2-3,6,8-15,20H,4-5,7,16-19H2,1H3,(H3,33,36,37)(H2,34,35,39)
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Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Vascular endothelial growth factor receptor 2


(Homo sapiens (human))
BDBM250513
PNG
(US9469639, Compound (VII))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3ccc(OCCC(C)(C)N)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C30H31FN6O2/c1-17-8-11-22(31)24(16-17)35-29(38)34-23-12-9-19(18-6-4-5-7-20(18)23)21-10-13-25(39-15-14-30(2,3)33)27-26(21)28(32)37-36-27/h4-13,16H,14-15,33H2,1-3H3,(H3,32,36,37)(H2,34,35,38)
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n/an/a 48.3n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250513
PNG
(US9469639, Compound (VII))
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(-c3ccc(OCCC(C)(C)N)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C30H31FN6O2/c1-17-8-11-22(31)24(16-17)35-29(38)34-23-12-9-19(18-6-4-5-7-20(18)23)21-10-13-25(39-15-14-30(2,3)33)27-26(21)28(32)37-36-27/h4-13,16H,14-15,33H2,1-3H3,(H3,32,36,37)(H2,34,35,38)
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Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor beta


(Homo sapiens (human))
BDBM250514
PNG
(US9469639, Compound (VIII))
Show SMILES Cc1cccc(NC(=O)Nc2ccc(-c3ccc(OCCC(C)(C)N)c4[nH]nc(N)c34)c3ccccc23)c1
Show InChI InChI=1S/C30H32N6O2/c1-18-7-6-8-19(17-18)33-29(37)34-24-13-11-21(20-9-4-5-10-22(20)24)23-12-14-25(38-16-15-30(2,3)32)27-26(23)28(31)36-35-27/h4-14,17H,15-16,32H2,1-3H3,(H3,31,35,36)(H2,33,34,37)
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n/an/a 155n/an/an/an/an/an/a



Radiant Pharma & Tech. Co., Ltd.

US Patent


Assay Description
Experimental Procedures(1) Kinase reaction substrate Poly(Glu, Tyr, 4:1) was diluted to 20 μg/ml with potassium ion-free PBS, and enzyme labeled pla...


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