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Patent code US10653688

Compile Data Set for Download or QSAR

Found 302 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
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442820
PNG
(US10653688, Compound 9)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cccnc1)C12CCN(CC1)CC2
Show InChI InChI=1S/C22H22N4O/c27-21(22-5-9-26(10-6-22)11-7-22)25-20-13-19-12-16(3-4-18(19)15-24-20)17-2-1-8-23-14-17/h1-4,8,12-15H,5-7,9-11H2,(H,24,25,27)
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n/an/an/an/a 26n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442827
PNG
(US10653688, Compound 15)
Show SMILES O=C(Cn1ccnc1)Nc1cc2cc(ccc2cn1)-c1cccnc1
Show InChI InChI=1S/C19H15N5O/c25-19(12-24-7-6-21-13-24)23-18-9-17-8-14(3-4-16(17)11-22-18)15-2-1-5-20-10-15/h1-11,13H,12H2,(H,22,23,25)
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n/an/an/an/a 5n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442818
PNG
(US10653688, Compound 19 | US10653688, Compound 8)
Show SMILES CN1CCC(CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cccnc1
Show InChI InChI=1S/C21H22N4O/c1-25-9-6-15(7-10-25)21(26)24-20-12-19-11-16(4-5-18(19)14-23-20)17-3-2-8-22-13-17/h2-5,8,11-15H,6-7,9-10H2,1H3,(H,23,24,26)
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n/an/an/an/a 10n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442887
PNG
(US10653688, Compound 69)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cnccn1)C1C[C@@H](C1)N1CCOCC1
Show InChI InChI=1S/C22H23N5O2/c28-22(18-10-19(11-18)27-5-7-29-8-6-27)26-21-12-17-9-15(1-2-16(17)13-25-21)20-14-23-3-4-24-20/h1-4,9,12-14,18-19H,5-8,10-11H2,(H,25,26,28)/t18?,19-
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n/an/an/an/a 20n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442894
PNG
(US10653688, Compound 75)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cnccn1)C1CCNCC1
Show InChI InChI=1S/C19H19N5O/c25-19(13-3-5-20-6-4-13)24-18-10-16-9-14(1-2-15(16)11-23-18)17-12-21-7-8-22-17/h1-2,7-13,20H,3-6H2,(H,23,24,25)
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n/an/an/an/a 10n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442929
PNG
(US10653688, Compound 107)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cncc(NC2CCNCC2)n1)C1CCCC1
Show InChI InChI=1S/C24H28N6O/c31-24(16-3-1-2-4-16)30-22-12-19-11-17(5-6-18(19)13-27-22)21-14-26-15-23(29-21)28-20-7-9-25-10-8-20/h5-6,11-16,20,25H,1-4,7-10H2,(H,28,29)(H,27,30,31)
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n/an/an/an/a 1n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442936
PNG
(US10653688, Compound 114)
Show SMILES CN1CCC(CC1)Nc1cncc(n1)-c1ccc2cnc(NC(=O)C3CCCC3)cc2c1
Show InChI InChI=1S/C25H30N6O/c1-31-10-8-21(9-11-31)28-24-16-26-15-22(29-24)18-6-7-19-14-27-23(13-20(19)12-18)30-25(32)17-4-2-3-5-17/h6-7,12-17,21H,2-5,8-11H2,1H3,(H,28,29)(H,27,30,32)
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n/an/an/an/a 1n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442942
PNG
(US10653688, Compound 120)
Show SMILES CN(C)c1cncc(n1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(C)CC3)cc2c1
Show InChI InChI=1S/C26H28N8O/c1-32(2)25-17-27-16-22(30-25)18-4-5-20-15-29-23(13-21(20)12-18)31-26(35)19-6-7-28-24(14-19)34-10-8-33(3)9-11-34/h4-7,12-17H,8-11H2,1-3H3,(H,29,31,35)
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n/an/an/an/a 7n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442957
PNG
(US10653688, Compound 133)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2[nH]c(C)cc2c1
Show InChI InChI=1S/C28H27N7O/c1-18-11-23-13-24(17-31-27(23)32-18)19-3-4-21-16-30-25(14-22(21)12-19)33-28(36)20-5-6-29-26(15-20)35-9-7-34(2)8-10-35/h3-6,11-17H,7-10H2,1-2H3,(H,31,32)(H,30,33,36)
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n/an/an/an/a 57n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442959
PNG
(US10653688, Compound 135)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2cc(C)[nH]c2c1
Show InChI InChI=1S/C28H27N7O/c1-18-11-24-25(32-18)13-23(17-30-24)19-3-4-21-16-31-26(14-22(21)12-19)33-28(36)20-5-6-29-27(15-20)35-9-7-34(2)8-10-35/h3-6,11-17,32H,7-10H2,1-2H3,(H,31,33,36)
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n/an/an/an/a 15n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442963
PNG
(US10653688, Compound 138)
Show SMILES CC(C)n1cc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(NC2CCNCC2)n1
Show InChI InChI=1S/C25H28N8O/c1-16(2)33-15-20(12-29-33)25(34)32-23-10-19-9-17(3-4-18(19)11-28-23)22-13-27-14-24(31-22)30-21-5-7-26-8-6-21/h3-4,9-16,21,26H,5-8H2,1-2H3,(H,30,31)(H,28,32,34)
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n/an/an/an/a 2n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442965
PNG
(US10653688, Compound 140)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cccnc1)c1coc(n1)C1CCNCC1
Show InChI InChI=1S/C23H21N5O2/c29-22(20-14-30-23(27-20)15-5-8-24-9-6-15)28-21-11-19-10-16(3-4-18(19)13-26-21)17-2-1-7-25-12-17/h1-4,7,10-15,24H,5-6,8-9H2,(H,26,28,29)
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n/an/an/an/a 1.05E+3n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442795
PNG
(US10653688, Compound 2)
Show SMILES CC(C)Nc1cc(F)cc(c1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(C)CC3)cc2c1
Show InChI InChI=1S/C29H31FN6O/c1-19(2)33-26-14-24(13-25(30)17-26)20-4-5-22-18-32-27(15-23(22)12-20)34-29(37)21-6-7-31-28(16-21)36-10-8-35(3)9-11-36/h4-7,12-19,33H,8-11H2,1-3H3,(H,32,34,37)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442942
PNG
(US10653688, Compound 120)
Show SMILES CN(C)c1cncc(n1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(C)CC3)cc2c1
Show InChI InChI=1S/C26H28N8O/c1-32(2)25-17-27-16-22(30-25)18-4-5-20-15-29-23(13-21(20)12-18)31-26(35)19-6-7-28-24(14-19)34-10-8-33(3)9-11-34/h4-7,12-17H,8-11H2,1-3H3,(H,29,31,35)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442949
PNG
(US10653688, Compound 125)
Show SMILES Fc1ccc(cc1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(OC2CNC2)n1
Show InChI InChI=1S/C23H18FN5O2/c24-18-5-3-14(4-6-18)23(30)29-21-8-17-7-15(1-2-16(17)9-27-21)20-12-26-13-22(28-20)31-19-10-25-11-19/h1-9,12-13,19,25H,10-11H2,(H,27,29,30)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442952
PNG
(US10653688, Compound 128)
Show SMILES CN1CCC(CC1)n1cc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc2[nH]ccc12
Show InChI InChI=1S/C26H25N7O/c1-32-8-5-21(6-9-32)33-16-20(13-30-33)26(34)31-25-11-19-10-17(2-3-18(19)12-29-25)23-14-27-15-24-22(23)4-7-28-24/h2-4,7,10-16,21,28H,5-6,8-9H2,1H3,(H,29,31,34)
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n/an/an/an/a 9.07E+3n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442958
PNG
(US10653688, Compound 134)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2[nH]cc(C)c2c1
Show InChI InChI=1S/C28H27N7O/c1-18-15-31-27-24(18)12-23(17-32-27)19-3-4-21-16-30-25(13-22(21)11-19)33-28(36)20-5-6-29-26(14-20)35-9-7-34(2)8-10-35/h3-6,11-17H,7-10H2,1-2H3,(H,31,32)(H,30,33,36)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442961
PNG
(US10653688, Compound 136)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2[nH]ccc2n1
Show InChI InChI=1S/C26H24N8O/c1-33-8-10-34(11-9-33)24-14-18(4-6-27-24)26(35)32-23-13-20-12-17(2-3-19(20)15-29-23)22-16-30-25-21(31-22)5-7-28-25/h2-7,12-16H,8-11H2,1H3,(H,28,30)(H,29,32,35)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442894
PNG
(US10653688, Compound 75)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cnccn1)C1CCNCC1
Show InChI InChI=1S/C19H19N5O/c25-19(13-3-5-20-6-4-13)24-18-10-16-9-14(1-2-15(16)11-23-18)17-12-21-7-8-22-17/h1-2,7-13,20H,3-6H2,(H,23,24,25)
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n/an/an/an/a 1.39E+3n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442906
PNG
(US10653688, Compound 86)
Show SMILES CC(C)Nc1cncc(n1)-c1ccc2cnc(NC(=O)C3CCC3)cc2c1
Show InChI InChI=1S/C21H23N5O/c1-13(2)24-20-12-22-11-18(25-20)15-6-7-16-10-23-19(9-17(16)8-15)26-21(27)14-4-3-5-14/h6-14H,3-5H2,1-2H3,(H,24,25)(H,23,26,27)
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n/an/an/an/a 17n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442862
PNG
(US10653688, Compound 44)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cncc(NC2CCNCC2)n1)C1CCCCC1
Show InChI InChI=1S/C25H30N6O/c32-25(17-4-2-1-3-5-17)31-23-13-20-12-18(6-7-19(20)14-28-23)22-15-27-16-24(30-22)29-21-8-10-26-11-9-21/h6-7,12-17,21,26H,1-5,8-11H2,(H,29,30)(H,28,31,32)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442864
PNG
(US10653688, Compound 46)
Show SMILES CN1CCC(CC1)Nc1cncc(c1)-c1ccc2cnc(NC(=O)c3ccc(F)cc3)cc2c1
Show InChI InChI=1S/C27H26FN5O/c1-33-10-8-24(9-11-33)31-25-13-22(15-29-17-25)19-2-3-20-16-30-26(14-21(20)12-19)32-27(34)18-4-6-23(28)7-5-18/h2-7,12-17,24,31H,8-11H2,1H3,(H,30,32,34)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442865
PNG
(US10653688, Compound 47)
Show SMILES CN1CCC(CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(NC(C)=O)c1
Show InChI InChI=1S/C23H25N5O2/c1-15(29)26-21-10-20(12-24-14-21)17-3-4-18-13-25-22(11-19(18)9-17)27-23(30)16-5-7-28(2)8-6-16/h3-4,9-14,16H,5-8H2,1-2H3,(H,26,29)(H,25,27,30)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442867
PNG
(US10653688, Compound 49)
Show SMILES CN(C)c1ccc(cn1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(C)CC3)cc2c1
Show InChI InChI=1S/C27H29N7O/c1-32(2)25-7-6-21(18-30-25)19-4-5-22-17-29-24(15-23(22)14-19)31-27(35)20-8-9-28-26(16-20)34-12-10-33(3)11-13-34/h4-9,14-18H,10-13H2,1-3H3,(H,29,31,35)
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n/an/an/an/a 904n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442795
PNG
(US10653688, Compound 2)
Show SMILES CC(C)Nc1cc(F)cc(c1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(C)CC3)cc2c1
Show InChI InChI=1S/C29H31FN6O/c1-19(2)33-26-14-24(13-25(30)17-26)20-4-5-22-18-32-27(15-23(22)12-20)34-29(37)21-6-7-31-28(16-21)36-10-8-35(3)9-11-36/h4-7,12-19,33H,8-11H2,1-3H3,(H,32,34,37)
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n/an/an/an/a 354n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442829
PNG
(US10653688, Compound 16)
Show SMILES Fc1cncc(c1)-c1ccc2cnc(NC(=O)[C@H]3C[C@@H](C3)N3CCOCC3)cc2c1
Show InChI InChI=1S/C23H23FN4O2/c24-20-8-19(12-25-14-20)15-1-2-16-13-26-22(11-17(16)7-15)27-23(29)18-9-21(10-18)28-3-5-30-6-4-28/h1-2,7-8,11-14,18,21H,3-6,9-10H2,(H,26,27,29)/t18-,21-
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442831
PNG
(US10653688, Compound 18)
Show SMILES Fc1cncc(c1)-c1ccc2cnc(NC(=O)CN3CCCC3)cc2c1
Show InChI InChI=1S/C20H19FN4O/c21-18-8-17(10-22-12-18)14-3-4-15-11-23-19(9-16(15)7-14)24-20(26)13-25-5-1-2-6-25/h3-4,7-12H,1-2,5-6,13H2,(H,23,24,26)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442836
PNG
(US10653688, Compound 22)
Show SMILES Fc1cncc(c1)-c1ccc2cnc(NC(=O)CN3CCNCC3)cc2c1
Show InChI InChI=1S/C20H20FN5O/c21-18-8-17(10-23-12-18)14-1-2-15-11-24-19(9-16(15)7-14)25-20(27)13-26-5-3-22-4-6-26/h1-2,7-12,22H,3-6,13H2,(H,24,25,27)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442821
PNG
(US10653688, Compound 10 | US10653688, Compound 151...)
Show SMILES O=C(CN1CCOCC1)Nc1cc2cc(ccc2cn1)-c1cccnc1
Show InChI InChI=1S/C20H20N4O2/c25-20(14-24-6-8-26-9-7-24)23-19-11-18-10-15(3-4-17(18)13-22-19)16-2-1-5-21-12-16/h1-5,10-13H,6-9,14H2,(H,22,23,25)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442882
PNG
(US10653688, Compound 64)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc(C)nc1
Show InChI InChI=1S/C25H25N7O/c1-17-27-15-22(16-28-17)18-3-4-20-14-29-23(12-21(20)11-18)30-25(33)19-5-6-26-24(13-19)32-9-7-31(2)8-10-32/h3-6,11-16H,7-10H2,1-2H3,(H,29,30,33)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442898
PNG
(US10653688, Compound 79)
Show SMILES O=C(CN1CCOCC1)Nc1cc2cc(ccc2cn1)-c1cnccn1
Show InChI InChI=1S/C19H19N5O2/c25-19(13-24-5-7-26-8-6-24)23-18-10-16-9-14(1-2-15(16)11-22-18)17-12-20-3-4-21-17/h1-4,9-12H,5-8,13H2,(H,22,23,25)
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n/an/an/an/a 79n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442900
PNG
(US10653688, Compound 81)
Show SMILES CC(C)CN1CCCC(CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnccn1
Show InChI InChI=1S/C24H29N5O/c1-17(2)16-29-10-3-4-18(7-11-29)24(30)28-23-13-21-12-19(5-6-20(21)14-27-23)22-15-25-8-9-26-22/h5-6,8-9,12-15,17-18H,3-4,7,10-11,16H2,1-2H3,(H,27,28,30)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442921
PNG
(US10653688, Compound 100)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(NC(C)(C)C)n1
Show InChI InChI=1S/C28H32N8O/c1-28(2,3)34-25-18-29-17-23(32-25)19-5-6-21-16-31-24(14-22(21)13-19)33-27(37)20-7-8-30-26(15-20)36-11-9-35(4)10-12-36/h5-8,13-18H,9-12H2,1-4H3,(H,32,34)(H,31,33,37)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442923
PNG
(US10653688, Compound 102)
Show SMILES CC(C)(C)Nc1cncc(n1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCOCC3)cc2c1
Show InChI InChI=1S/C27H29N7O2/c1-27(2,3)33-24-17-28-16-22(31-24)18-4-5-20-15-30-23(13-21(20)12-18)32-26(35)19-6-7-29-25(14-19)34-8-10-36-11-9-34/h4-7,12-17H,8-11H2,1-3H3,(H,31,33)(H,30,32,35)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442930
PNG
(US10653688, Compound 108)
Show SMILES FC1(F)CCC(CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(NC2CCNCC2)n1
Show InChI InChI=1S/C25H28F2N6O/c26-25(27)7-3-16(4-8-25)24(34)33-22-12-19-11-17(1-2-18(19)13-30-22)21-14-29-15-23(32-21)31-20-5-9-28-10-6-20/h1-2,11-16,20,28H,3-10H2,(H,31,32)(H,30,33,34)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442940
PNG
(US10653688, Compound 118)
Show SMILES CC(C)N1CCC(CC1)Nc1cncc(n1)-c1ccc2cnc(NC(=O)C3CCCC3)cc2c1
Show InChI InChI=1S/C27H34N6O/c1-18(2)33-11-9-23(10-12-33)30-26-17-28-16-24(31-26)20-7-8-21-15-29-25(14-22(21)13-20)32-27(34)19-5-3-4-6-19/h7-8,13-19,23H,3-6,9-12H2,1-2H3,(H,30,31)(H,29,32,34)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Dual-specificity tyrosine-phosphorylation regulated kinase 1A


(Homo sapiens (Human))
BDBM442953
PNG
(US10653688, Compound 129)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2[nH]ccc2c1
Show InChI InChI=1S/C27H25N7O/c1-33-8-10-34(11-9-33)25-15-20(5-6-28-25)27(35)32-24-14-22-12-18(2-3-21(22)16-30-24)23-13-19-4-7-29-26(19)31-17-23/h2-7,12-17H,8-11H2,1H3,(H,29,31)(H,30,32,35)
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Samumed, LLC

US Patent


Assay Description
The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Divis...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442808
PNG
(US10653688, Compound 4)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=C)Nc1cc2cc(ccc2cn1)-c1ccccn1
Show InChI InChI=1S/C26H26N6/c1-19(20-8-10-28-26(17-20)32-13-11-31(2)12-14-32)30-25-16-23-15-21(6-7-22(23)18-29-25)24-5-3-4-9-27-24/h3-10,15-18H,1,11-14H2,2H3,(H,29,30)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442823
PNG
(US10653688, Compound 11 | US10653688, Compound 61)
Show SMILES CN1CCN(CC(=O)Nc2cc3cc(ccc3cn2)-c2cccnc2)CC1
Show InChI InChI=1S/C21H23N5O/c1-25-7-9-26(10-8-25)15-21(27)24-20-12-19-11-16(4-5-18(19)14-23-20)17-3-2-6-22-13-17/h2-6,11-14H,7-10,15H2,1H3,(H,23,24,27)
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n/an/an/an/a 1.12E+3n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442825
PNG
(US10653688, Compound 13)
Show SMILES CN1CCN(CC1)c1ccc(CC(=O)Nc2cc3cc(ccc3cn2)-c2cccnc2)cc1
Show InChI InChI=1S/C27H27N5O/c1-31-11-13-32(14-12-31)25-8-4-20(5-9-25)15-27(33)30-26-17-24-16-21(6-7-23(24)19-29-26)22-3-2-10-28-18-22/h2-10,16-19H,11-15H2,1H3,(H,29,30,33)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442840
PNG
(US10653688, Compound 26)
Show SMILES FC(F)c1cncc(c1)-c1ccc2cnc(NC(=O)c3cccc(c3)C3CCNCC3)cc2c1
Show InChI InChI=1S/C27H24F2N4O/c28-26(29)24-12-23(14-31-15-24)19-4-5-21-16-32-25(13-22(21)11-19)33-27(34)20-3-1-2-18(10-20)17-6-8-30-9-7-17/h1-5,10-17,26,30H,6-9H2,(H,32,33,34)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442842
PNG
(US10653688, Compound 28)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(c1)C(F)F
Show InChI InChI=1S/C26H24F2N6O/c1-33-6-8-34(9-7-33)24-13-18(4-5-30-24)26(35)32-23-12-20-10-17(2-3-19(20)16-31-23)21-11-22(25(27)28)15-29-14-21/h2-5,10-16,25H,6-9H2,1H3,(H,31,32,35)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442843
PNG
(US10653688, Compound 29)
Show SMILES CN1CCN(CC(=O)Nc2cc3cc(ccc3cn2)-c2cncc(c2)C(F)(F)F)CC1
Show InChI InChI=1S/C22H22F3N5O/c1-29-4-6-30(7-5-29)14-21(31)28-20-10-17-8-15(2-3-16(17)12-27-20)18-9-19(13-26-11-18)22(23,24)25/h2-3,8-13H,4-7,14H2,1H3,(H,27,28,31)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442845
PNG
(US10653688, Compound 30)
Show SMILES CN1CCN(CC(=O)Nc2cc3cc(ccc3cn2)-c2ccc(nc2)C(F)(F)F)CC1
Show InChI InChI=1S/C22H22F3N5O/c1-29-6-8-30(9-7-29)14-21(31)28-20-11-18-10-15(2-3-17(18)13-27-20)16-4-5-19(26-12-16)22(23,24)25/h2-5,10-13H,6-9,14H2,1H3,(H,27,28,31)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442933
PNG
(US10653688, Compound 111)
Show SMILES F[C@H]1CNCCC1Nc1cncc(n1)-c1ccc2cnc(NC(=O)C3CC3)cc2c1
Show InChI InChI=1S/C22H23FN6O/c23-17-10-24-6-5-18(17)27-21-12-25-11-19(28-21)14-3-4-15-9-26-20(8-16(15)7-14)29-22(30)13-1-2-13/h3-4,7-9,11-13,17-18,24H,1-2,5-6,10H2,(H,27,28)(H,26,29,30)/t17-,18?/m0/s1
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n/an/an/an/a 4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442940
PNG
(US10653688, Compound 118)
Show SMILES CC(C)N1CCC(CC1)Nc1cncc(n1)-c1ccc2cnc(NC(=O)C3CCCC3)cc2c1
Show InChI InChI=1S/C27H34N6O/c1-18(2)33-11-9-23(10-12-33)30-26-17-28-16-24(31-26)20-7-8-21-15-29-25(14-22(21)13-20)32-27(34)19-5-3-4-6-19/h7-8,13-19,23H,3-6,9-12H2,1-2H3,(H,30,31)(H,29,32,34)
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n/an/an/an/a 78n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442954
PNG
(US10653688, Compound 130)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2cc[nH]c2c1
Show InChI InChI=1S/C27H25N7O/c1-33-8-10-34(11-9-33)26-15-19(4-6-29-26)27(35)32-25-14-21-12-18(2-3-20(21)16-31-25)22-13-24-23(30-17-22)5-7-28-24/h2-7,12-17,28H,8-11H2,1H3,(H,31,32,35)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442956
PNG
(US10653688, Compound 132)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2ocnc2c1
Show InChI InChI=1S/C26H23N7O2/c1-32-6-8-33(9-7-32)24-13-18(4-5-27-24)25(34)31-23-12-20-10-17(2-3-19(20)14-28-23)21-11-22-26(29-15-21)35-16-30-22/h2-5,10-16H,6-9H2,1H3,(H,28,31,34)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442957
PNG
(US10653688, Compound 133)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnc2[nH]c(C)cc2c1
Show InChI InChI=1S/C28H27N7O/c1-18-11-23-13-24(17-31-27(23)32-18)19-3-4-21-16-30-25(14-22(21)12-19)33-28(36)20-5-6-29-26(15-20)35-9-7-34(2)8-10-35/h3-6,11-17H,7-10H2,1-2H3,(H,31,32)(H,30,33,36)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

More data for this
Ligand-Target Pair
Axin-1/Glycogen synthase kinase-3 beta


(Homo sapiens (Human))
BDBM442964
PNG
(US10653688, Compound 139)
Show SMILES CC(C)n1cc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncc(NC2CCN(C)CC2)n1
Show InChI InChI=1S/C26H30N8O/c1-17(2)34-16-21(13-29-34)26(35)32-24-11-20-10-18(4-5-19(20)12-28-24)23-14-27-15-25(31-23)30-22-6-8-33(3)9-7-22/h4-5,10-17,22H,6-9H2,1-3H3,(H,30,31)(H,28,32,35)
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Samumed, LLC

US Patent


Assay Description
The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies—a Di...


US Patent US10653688 (2020)

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