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Found 1113 hits Enz. Inhib. hit(s) with Target = 'Dual-specificity tyrosine-phosphorylation regulated kinase 1A'   
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))
BDBM293423
PNG
(US10106527, Compound 461 | US10106527, Compound 9)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCNCC3)cc2c1
Show InChI InChI=1S/C23H23N7O/c1-29-15-20(14-27-29)16-2-3-18-13-26-21(11-19(18)10-16)28-23(31)17-4-5-25-22(12-17)30-8-6-24-7-9-30/h2-5,10-15,24H,6-9H2,1H3,(H,26,28,31)
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n/an/an/an/a 0.400n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293564
PNG
(US10106527, Compound 275)
Show SMILES CC(C)N1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncn1C
Show InChI InChI=1S/C26H29N7O/c1-18(2)32-8-10-33(11-9-32)25-14-20(6-7-28-25)26(34)30-24-13-22-12-19(4-5-21(22)15-29-24)23-16-27-17-31(23)3/h4-7,12-18H,8-11H2,1-3H3,(H,29,30,34)
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n/an/an/an/a 0.600n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293619
PNG
(US10106527, Compound 391)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1nncs1
Show InChI InChI=1S/C22H21N7OS/c1-28-6-8-29(9-7-28)20-12-15(4-5-23-20)21(30)26-19-11-18-10-16(22-27-25-14-31-22)2-3-17(18)13-24-19/h2-5,10-14H,6-9H2,1H3,(H,24,26,30)
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n/an/an/an/a 0.700n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293479
PNG
(US10106527, Compound 93)
Show SMILES CN1CCC2(CN(C2)c2cc(ccn2)C(=O)Nc2cc3cc(ccc3cn2)-c2cnn(C)c2)CC1
Show InChI InChI=1S/C27H29N7O/c1-32-9-6-27(7-10-32)17-34(18-27)25-13-20(5-8-28-25)26(35)31-24-12-22-11-19(3-4-21(22)14-29-24)23-15-30-33(2)16-23/h3-5,8,11-16H,6-7,9-10,17-18H2,1-2H3,(H,29,31,35)
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n/an/an/an/a 0.700n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293566
PNG
(US10106527, Compound 277)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CC4(C3)CCNCC4)cc2c1
Show InChI InChI=1S/C26H27N7O/c1-32-17-28-14-22(32)18-2-3-20-13-30-23(11-21(20)10-18)31-25(34)19-4-7-29-24(12-19)33-15-26(16-33)5-8-27-9-6-26/h2-4,7,10-14,17,27H,5-6,8-9,15-16H2,1H3,(H,30,31,34)
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n/an/an/an/a 0.800n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293415
PNG
(US10106527, Compound 1 | US10106527, Compound 145)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cn[nH]c1
Show InChI InChI=1S/C23H23N7O/c1-29-6-8-30(9-7-29)22-12-17(4-5-24-22)23(31)28-21-11-19-10-16(20-14-26-27-15-20)2-3-18(19)13-25-21/h2-5,10-15H,6-9H2,1H3,(H,26,27)(H,25,28,31)
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n/an/an/an/a 0.800n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293569
PNG
(US10106527, Compound 286)
Show SMILES CN1Cc2ccc(cc2C1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncn1C
Show InChI InChI=1S/C23H21N5O/c1-27-12-18-6-4-16(8-20(18)13-27)23(29)26-22-9-19-7-15(3-5-17(19)10-25-22)21-11-24-14-28(21)2/h3-11,14H,12-13H2,1-2H3,(H,25,26,29)
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n/an/an/an/a 0.800n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293616
PNG
(US10106527, Compound 388)
Show SMILES CN1CCN(CC1)c1ccc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1nncs1
Show InChI InChI=1S/C22H21N7OS/c1-28-6-8-29(9-7-28)20-5-4-17(13-24-20)21(30)26-19-11-18-10-15(22-27-25-14-31-22)2-3-16(18)12-23-19/h2-5,10-14H,6-9H2,1H3,(H,23,26,30)
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n/an/an/an/a 0.800n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293428
PNG
(US10106527, Compound 14)
Show SMILES CN1CCN(CC1)c1ccc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C24H25N7O/c1-29-7-9-31(10-8-29)23-6-5-19(14-26-23)24(32)28-22-12-20-11-17(3-4-18(20)13-25-22)21-15-27-30(2)16-21/h3-6,11-16H,7-10H2,1-2H3,(H,25,28,32)
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n/an/an/an/a 0.900n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293422
PNG
(US10106527, Compound 8)
Show SMILES CN1CCC(CC1)Oc1ccc(cc1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C26H27N5O2/c1-30-11-9-24(10-12-30)33-23-7-5-18(6-8-23)26(32)29-25-14-21-13-19(3-4-20(21)15-27-25)22-16-28-31(2)17-22/h3-8,13-17,24H,9-12H2,1-2H3,(H,27,29,32)
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n/an/an/an/a 0.900n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293417
PNG
(US10106527, Compound 3)
Show SMILES CN1CCN(CC1)c1cccc(c1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C25H26N6O/c1-29-8-10-31(11-9-29)23-5-3-4-19(13-23)25(32)28-24-14-21-12-18(6-7-20(21)15-26-24)22-16-27-30(2)17-22/h3-7,12-17H,8-11H2,1-2H3,(H,26,28,32)
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n/an/an/an/a 0.900n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293444
PNG
(US10106527, Compound 37)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncn1C
Show InChI InChI=1S/C24H25N7O/c1-29-7-9-31(10-8-29)23-13-18(5-6-26-23)24(32)28-22-12-20-11-17(3-4-19(20)14-27-22)21-15-25-16-30(21)2/h3-6,11-16H,7-10H2,1-2H3,(H,27,28,32)
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n/an/an/an/a 0.900n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293613
PNG
(US10106527, Compound 385)
Show SMILES CN1CCC(CC1)Oc1ccc(cc1)C(=O)Nc1cc2cc(ccc2cn1)-c1nncs1
Show InChI InChI=1S/C24H23N5O2S/c1-29-10-8-21(9-11-29)31-20-6-4-16(5-7-20)23(30)27-22-13-19-12-17(24-28-26-15-32-24)2-3-18(19)14-25-22/h2-7,12-15,21H,8-11H2,1H3,(H,25,27,30)
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n/an/an/an/a 0.900n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293577
PNG
(US10106527, Compound 301)
Show SMILES CN1CCC(CC1)Oc1cccc(c1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnco1
Show InChI InChI=1S/C25H24N4O3/c1-29-9-7-21(8-10-29)32-22-4-2-3-18(12-22)25(30)28-24-13-20-11-17(23-15-26-16-31-23)5-6-19(20)14-27-24/h2-6,11-16,21H,7-10H2,1H3,(H,27,28,30)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293593
PNG
(US10106527, Compound 334)
Show SMILES CN1CCN(CC1)c1ccc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncs1
Show InChI InChI=1S/C23H22N6OS/c1-28-6-8-29(9-7-28)22-5-4-18(13-26-22)23(30)27-21-11-19-10-16(20-14-24-15-31-20)2-3-17(19)12-25-21/h2-5,10-15H,6-9H2,1H3,(H,25,27,30)
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n/an/an/an/a 1n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293597
PNG
(US10106527, Compound 338)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncs1
Show InChI InChI=1S/C23H22N6OS/c1-28-6-8-29(9-7-28)22-12-17(4-5-25-22)23(30)27-21-11-19-10-16(20-14-24-15-31-20)2-3-18(19)13-26-21/h2-5,10-15H,6-9H2,1H3,(H,26,27,30)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293637
PNG
(US10106527, Compound 435)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)C#N)cc2c1
Show InChI InChI=1S/C20H14N6O/c1-26-12-22-11-18(26)13-2-3-15-10-24-19(8-16(15)6-13)25-20(27)14-4-5-23-17(7-14)9-21/h2-8,10-12H,1H3,(H,24,25,27)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293478
PNG
(US10106527, Compound 92)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CC4(C3)CCNCC4)cc2c1
Show InChI InChI=1S/C26H27N7O/c1-32-15-22(14-30-32)18-2-3-20-13-29-23(11-21(20)10-18)31-25(34)19-4-7-28-24(12-19)33-16-26(17-33)5-8-27-9-6-26/h2-4,7,10-15,27H,5-6,8-9,16-17H2,1H3,(H,29,31,34)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293424
PNG
(US10106527, Compound 10 | US10106527, Compound 142...)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C24H25N7O/c1-29-7-9-31(10-8-29)23-13-18(5-6-25-23)24(32)28-22-12-20-11-17(3-4-19(20)14-26-22)21-15-27-30(2)16-21/h3-6,11-16H,7-10H2,1-2H3,(H,26,28,32)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293563
PNG
(US10106527, Compound 273)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCOCC3)cc2c1
Show InChI InChI=1S/C23H22N6O2/c1-28-15-24-14-20(28)16-2-3-18-13-26-21(11-19(18)10-16)27-23(30)17-4-5-25-22(12-17)29-6-8-31-9-7-29/h2-5,10-15H,6-9H2,1H3,(H,26,27,30)
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n/an/an/an/a 1.10n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293565
PNG
(US10106527, Compound 276)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCN(CC3)C3CC3)cc2c1
Show InChI InChI=1S/C26H27N7O/c1-31-17-27-16-23(31)18-2-3-20-15-29-24(13-21(20)12-18)30-26(34)19-6-7-28-25(14-19)33-10-8-32(9-11-33)22-4-5-22/h2-3,6-7,12-17,22H,4-5,8-11H2,1H3,(H,29,30,34)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293582
PNG
(US10106527, Compound 317)
Show SMILES CN1CCC2(CN(C2)c2cc(ccn2)C(=O)Nc2cc3cc(ccc3cn2)-c2cnco2)CC1
Show InChI InChI=1S/C26H26N6O2/c1-31-8-5-26(6-9-31)15-32(16-26)24-12-19(4-7-28-24)25(33)30-23-11-21-10-18(22-14-27-17-34-22)2-3-20(21)13-29-23/h2-4,7,10-14,17H,5-6,8-9,15-16H2,1H3,(H,29,30,33)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293595
PNG
(US10106527, Compound 336)
Show SMILES CN(C)C1CN(C1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncs1
Show InChI InChI=1S/C23H22N6OS/c1-28(2)19-12-29(13-19)22-9-16(5-6-25-22)23(30)27-21-8-18-7-15(20-11-24-14-31-20)3-4-17(18)10-26-21/h3-11,14,19H,12-13H2,1-2H3,(H,26,27,30)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293420
PNG
(US10106527, Compound 6)
Show SMILES CN1CCC(CC1)Oc1cccc(c1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C26H27N5O2/c1-30-10-8-23(9-11-30)33-24-5-3-4-19(13-24)26(32)29-25-14-21-12-18(6-7-20(21)15-27-25)22-16-28-31(2)17-22/h3-7,12-17,23H,8-11H2,1-2H3,(H,27,29,32)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293430
PNG
(US10106527, Compound 16)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3ccnc(OC4CCNCC4)c3)cc2c1
Show InChI InChI=1S/C24H24N6O2/c1-30-15-20(14-28-30)16-2-3-18-13-27-22(11-19(18)10-16)29-24(31)17-4-9-26-23(12-17)32-21-5-7-25-8-6-21/h2-4,9-15,21,25H,5-8H2,1H3,(H,27,29,31)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293442
PNG
(US10106527, Compound 28)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccc(F)cc3)cc2c1
Show InChI InChI=1S/C20H15FN4O/c1-25-12-22-11-18(25)14-2-3-15-10-23-19(9-16(15)8-14)24-20(26)13-4-6-17(21)7-5-13/h2-12H,1H3,(H,23,24,26)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293452
PNG
(US10106527, Compound 55)
Show SMILES CN(C)C1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C26H29N7O/c1-31(2)23-7-10-33(11-8-23)25-14-19(6-9-27-25)26(34)30-24-13-21-12-18(4-5-20(21)15-28-24)22-16-29-32(3)17-22/h4-6,9,12-17,23H,7-8,10-11H2,1-3H3,(H,28,30,34)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293620
PNG
(US10106527, Compound 392)
Show SMILES CC(C)N1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1nncs1
Show InChI InChI=1S/C24H25N7OS/c1-16(2)30-7-9-31(10-8-30)22-13-17(5-6-25-22)23(32)28-21-12-20-11-18(24-29-27-15-33-24)3-4-19(20)14-26-21/h3-6,11-16H,7-10H2,1-2H3,(H,26,28,32)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293643
PNG
(US10106527, Compound 441)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCC(F)(F)CC3)cc2c1
Show InChI InChI=1S/C24H22F2N6O/c1-31-15-27-14-20(31)16-2-3-18-13-29-21(11-19(18)10-16)30-23(33)17-4-7-28-22(12-17)32-8-5-24(25,26)6-9-32/h2-4,7,10-15H,5-6,8-9H2,1H3,(H,29,30,33)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293568
PNG
(US10106527, Compound 285)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccc4CNCc4c3)cc2c1
Show InChI InChI=1S/C22H19N5O/c1-27-13-24-12-20(27)14-2-4-17-11-25-21(8-18(17)6-14)26-22(28)15-3-5-16-9-23-10-19(16)7-15/h2-8,11-13,23H,9-10H2,1H3,(H,25,26,28)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293599
PNG
(US10106527, Compound 340)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cncs1)c1ccc2CCNCc2c1
Show InChI InChI=1S/C22H18N4OS/c27-22(16-3-1-14-5-6-23-10-19(14)8-16)26-21-9-18-7-15(20-12-24-13-28-20)2-4-17(18)11-25-21/h1-4,7-9,11-13,23H,5-6,10H2,(H,25,26,27)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293424
PNG
(US10106527, Compound 10 | US10106527, Compound 142...)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C24H25N7O/c1-29-7-9-31(10-8-29)23-13-18(5-6-25-23)24(32)28-22-12-20-11-17(3-4-19(20)14-26-22)21-15-27-30(2)16-21/h3-6,11-16H,7-10H2,1-2H3,(H,26,28,32)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293415
PNG
(US10106527, Compound 1 | US10106527, Compound 145)
Show SMILES CN1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cn[nH]c1
Show InChI InChI=1S/C23H23N7O/c1-29-6-8-30(9-7-29)22-12-17(4-5-24-22)23(31)28-21-11-19-10-16(20-14-26-27-15-20)2-3-18(19)13-25-21/h2-5,10-15H,6-9H2,1H3,(H,26,27)(H,25,28,31)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293545
PNG
(US10106527, Compound 236)
Show SMILES CN(C)C1CN(C1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cn(C)nn1
Show InChI InChI=1S/C23H24N8O/c1-29(2)19-12-31(13-19)22-10-16(6-7-24-22)23(32)26-21-9-18-8-15(4-5-17(18)11-25-21)20-14-30(3)28-27-20/h4-11,14,19H,12-13H2,1-3H3,(H,25,26,32)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293421
PNG
(US10106527, Compound 7)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3ccc(OC4CCNCC4)cc3)cc2c1
Show InChI InChI=1S/C25H25N5O2/c1-30-16-21(15-28-30)18-2-3-19-14-27-24(13-20(19)12-18)29-25(31)17-4-6-22(7-5-17)32-23-8-10-26-11-9-23/h2-7,12-16,23,26H,8-11H2,1H3,(H,27,29,31)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293443
PNG
(US10106527, Compound 29)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccc(OC(F)F)cc3)cc2c1
Show InChI InChI=1S/C21H16F2N4O2/c1-27-12-24-11-18(27)14-2-3-15-10-25-19(9-16(15)8-14)26-20(28)13-4-6-17(7-5-13)29-21(22)23/h2-12,21H,1H3,(H,25,26,28)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293612
PNG
(US10106527, Compound 384)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1nncs1)c1ccc(OC2CCNCC2)cc1
Show InChI InChI=1S/C23H21N5O2S/c29-22(15-3-5-19(6-4-15)30-20-7-9-24-10-8-20)27-21-12-18-11-16(23-28-26-14-31-23)1-2-17(18)13-25-21/h1-6,11-14,20,24H,7-10H2,(H,25,27,29)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293621
PNG
(US10106527, Compound 393)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1nncs1)c1ccnc(c1)N1CCOCC1
Show InChI InChI=1S/C21H18N6O2S/c28-20(14-3-4-22-19(11-14)27-5-7-29-8-6-27)25-18-10-17-9-15(21-26-24-13-30-21)1-2-16(17)12-23-18/h1-4,9-13H,5-8H2,(H,23,25,28)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293419
PNG
(US10106527, Compound 5)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3cccc(OC4CCNCC4)c3)cc2c1
Show InChI InChI=1S/C25H25N5O2/c1-30-16-21(15-28-30)17-5-6-19-14-27-24(13-20(19)11-17)29-25(31)18-3-2-4-23(12-18)32-22-7-9-26-10-8-22/h2-6,11-16,22,26H,7-10H2,1H3,(H,27,29,31)
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Samumed, LLC

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Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293480
PNG
(US10106527, Compound 94)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CCC4(CNC4)CC3)cc2c1
Show InChI InChI=1S/C26H27N7O/c1-32-15-22(14-30-32)18-2-3-20-13-29-23(11-21(20)10-18)31-25(34)19-4-7-28-24(12-19)33-8-5-26(6-9-33)16-27-17-26/h2-4,7,10-15,27H,5-6,8-9,16-17H2,1H3,(H,29,31,34)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293482
PNG
(US10106527, Compound 97)
Show SMILES CN(C1CCN(C)CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C26H29N7O/c1-31-10-7-23(8-11-31)33(3)25-14-19(6-9-27-25)26(34)30-24-13-21-12-18(4-5-20(21)15-28-24)22-16-29-32(2)17-22/h4-6,9,12-17,23H,7-8,10-11H2,1-3H3,(H,28,30,34)
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n/an/an/an/a 1.30n/an/an/a25



Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293416
PNG
(US10106527, Compound 2)
Show SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)c3cccc(c3)N3CCNCC3)cc2c1
Show InChI InChI=1S/C24H24N6O/c1-29-16-21(15-27-29)17-5-6-19-14-26-23(13-20(19)11-17)28-24(31)18-3-2-4-22(12-18)30-9-7-25-8-10-30/h2-6,11-16,25H,7-10H2,1H3,(H,26,28,31)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293560
PNG
(US10106527, Compound 266)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CC(N)C3)cc2c1
Show InChI InChI=1S/C22H21N7O/c1-28-13-24-10-19(28)14-2-3-16-9-26-20(7-17(16)6-14)27-22(30)15-4-5-25-21(8-15)29-11-18(23)12-29/h2-10,13,18H,11-12,23H2,1H3,(H,26,27,30)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293455
PNG
(US10106527, Compound 59)
Show SMILES CN(C)C1CN(C1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C24H25N7O/c1-29(2)21-14-31(15-21)23-10-17(6-7-25-23)24(32)28-22-9-19-8-16(4-5-18(19)11-26-22)20-12-27-30(3)13-20/h4-13,21H,14-15H2,1-3H3,(H,26,28,32)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293636
PNG
(US10106527, Compound 434)
Show SMILES Cc1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncn1C
Show InChI InChI=1S/C20H17N5O/c1-13-7-15(5-6-22-13)20(26)24-19-9-17-8-14(3-4-16(17)10-23-19)18-11-21-12-25(18)2/h3-12H,1-2H3,(H,23,24,26)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293639
PNG
(US10106527, Compound 437)
Show SMILES Cn1cncc1-c1ccc2cnc(NC(=O)c3ccnc(c3)N3CC(F)(F)C3)cc2c1
Show InChI InChI=1S/C22H18F2N6O/c1-29-13-25-10-18(29)14-2-3-16-9-27-19(7-17(16)6-14)28-21(31)15-4-5-26-20(8-15)30-11-22(23,24)12-30/h2-10,13H,11-12H2,1H3,(H,27,28,31)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293425
PNG
(US10106527, Compound 11)
Show SMILES CC(C)N1CCN(CC1)c1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C26H29N7O/c1-18(2)32-8-10-33(11-9-32)25-14-20(6-7-27-25)26(34)30-24-13-22-12-19(4-5-21(22)15-28-24)23-16-29-31(3)17-23/h4-7,12-18H,8-11H2,1-3H3,(H,28,30,34)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293584
PNG
(US10106527, Compound 319)
Show SMILES O=C(Nc1cc2cc(ccc2cn1)-c1cnco1)c1ccnc(NC2CCNCC2)c1
Show InChI InChI=1S/C23H22N6O2/c30-23(16-3-8-26-21(10-16)28-19-4-6-24-7-5-19)29-22-11-18-9-15(20-13-25-14-31-20)1-2-17(18)12-27-22/h1-3,8-14,19,24H,4-7H2,(H,26,28)(H,27,29,30)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293540
PNG
(US10106527, Compound 222)
Show SMILES CN1CCN(CC1)c1ccc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn2CCN(CCF)Cc12
Show InChI InChI=1S/C28H31FN8O/c1-34-8-11-36(12-9-34)27-5-4-22(17-31-27)28(38)33-26-15-23-14-20(2-3-21(23)16-30-26)24-18-32-37-13-10-35(7-6-29)19-25(24)37/h2-5,14-18H,6-13,19H2,1H3,(H,30,33,38)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

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


(Homo sapiens (Human))
BDBM293453
PNG
(US10106527, Compound 56)
Show SMILES CC(C)N1CCC(CC1)Oc1cc(ccn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1
Show InChI InChI=1S/C27H30N6O2/c1-18(2)33-10-7-24(8-11-33)35-26-14-20(6-9-28-26)27(34)31-25-13-22-12-19(4-5-21(22)15-29-25)23-16-30-32(3)17-23/h4-6,9,12-18,24H,7-8,10-11H2,1-3H3,(H,29,31,34)
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Samumed, LLC

US Patent


Assay Description
Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...


US Patent US10106527 (2018)

More data for this
Ligand-Target Pair
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