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Compile Data Set for Download or QSAR

Found 631 hits with Last Name = 'besson' and Initial = 't'   
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))
BDBM50434358
PNG
(CHEMBL2386770 | US9446044, 68)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4Br)c3c2s1
Show InChI InChI=1S/C17H11BrFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(19)6-9(10)18/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.160n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.220n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.220n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of DYRK1A (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.220n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434358
PNG
(CHEMBL2386770 | US9446044, 68)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4Br)c3c2s1
Show InChI InChI=1S/C17H11BrFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(19)6-9(10)18/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.240n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.280n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.280n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of DYRK1B (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.280n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.360n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.360n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.360n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of DYRK1A (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.590n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.590n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of DYRK1B (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 0.590n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434352
PNG
(CHEMBL2386748 | US9446044, 78)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4F)c3c2s1
Show InChI InChI=1S/C17H11F2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.940n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434352
PNG
(CHEMBL2386748 | US9446044, 78)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4F)c3c2s1
Show InChI InChI=1S/C17H11F2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.940n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434364
PNG
(CHEMBL2386764 | US9446044, 65)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(C)cc4)c3c2s1
Show InChI InChI=1S/C18H15N5OS/c1-10-3-5-11(6-4-10)22-17-14-12(20-9-21-17)7-8-13-15(14)25-18(23-13)16(19)24-2/h3-9,19H,1-2H3,(H,20,21,22)
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n/an/a 0.980n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434364
PNG
(CHEMBL2386764 | US9446044, 65)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(C)cc4)c3c2s1
Show InChI InChI=1S/C18H15N5OS/c1-10-3-5-11(6-4-10)22-17-14-12(20-9-21-17)7-8-13-15(14)25-18(23-13)16(19)24-2/h3-9,19H,1-2H3,(H,20,21,22)
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n/an/a 0.980n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246384
PNG
(US9446044, 71)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4F)c3c2s1
Show InChI InChI=1S/C17H11ClFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.990n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246384
PNG
(US9446044, 71)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4F)c3c2s1
Show InChI InChI=1S/C17H11ClFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 0.990n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434352
PNG
(CHEMBL2386748 | US9446044, 78)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4F)c3c2s1
Show InChI InChI=1S/C17H11F2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 1.07n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434352
PNG
(CHEMBL2386748 | US9446044, 78)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4F)c3c2s1
Show InChI InChI=1S/C17H11F2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 1.10n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434338
PNG
(CHEMBL2386762 | US9446044, 56)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4)c3c2s1
Show InChI InChI=1S/C17H12ClN5OS/c1-24-15(19)17-23-12-7-6-11-13(14(12)25-17)16(21-8-20-11)22-10-4-2-9(18)3-5-10/h2-8,19H,1H3,(H,20,21,22)
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n/an/a 1.13n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246384
PNG
(US9446044, 71)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4F)c3c2s1
Show InChI InChI=1S/C17H11ClFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 1.60n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246384
PNG
(US9446044, 71)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4F)c3c2s1
Show InChI InChI=1S/C17H11ClFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 1.63n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434347
PNG
(CHEMBL2386753 | US9446044, 48)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc5OCOc5c4)c3c2s1
Show InChI InChI=1S/C18H13N5O3S/c1-24-16(19)18-23-11-4-3-10-14(15(11)27-18)17(21-7-20-10)22-9-2-5-12-13(6-9)26-8-25-12/h2-7,19H,8H2,1H3,(H,20,21,22)
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n/an/a 1.65n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434365
PNG
(CHEMBL2386763 | US9446044, 64)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccccc4)c3c2s1
Show InChI InChI=1S/C17H13N5OS/c1-23-15(18)17-22-12-8-7-11-13(14(12)24-17)16(20-9-19-11)21-10-5-3-2-4-6-10/h2-9,18H,1H3,(H,19,20,21)
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n/an/a 1.81n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246372
PNG
(US9446044, 47)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4cc5OCOc5c(Br)c4)c3c2s1
Show InChI InChI=1S/C18H12BrN5O3S/c1-25-16(20)18-24-11-3-2-10-13(15(11)28-18)17(22-6-21-10)23-8-4-9(19)14-12(5-8)26-7-27-14/h2-6,20H,7H2,1H3,(H,21,22,23)
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n/an/a 2.76n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434364
PNG
(CHEMBL2386764 | US9446044, 65)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(C)cc4)c3c2s1
Show InChI InChI=1S/C18H15N5OS/c1-10-3-5-11(6-4-10)22-17-14-12(20-9-21-17)7-8-13-15(14)25-18(23-13)16(19)24-2/h3-9,19H,1-2H3,(H,20,21,22)
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n/an/a 2.80n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434364
PNG
(CHEMBL2386764 | US9446044, 65)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(C)cc4)c3c2s1
Show InChI InChI=1S/C18H15N5OS/c1-10-3-5-11(6-4-10)22-17-14-12(20-9-21-17)7-8-13-15(14)25-18(23-13)16(19)24-2/h3-9,19H,1-2H3,(H,20,21,22)
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n/an/a 2.83n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 2


(Homo sapiens (Human))
BDBM246383
PNG
(US9446044, 69)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Show InChI InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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n/an/a 3.20n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of DYRK2 (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434365
PNG
(CHEMBL2386763 | US9446044, 64)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccccc4)c3c2s1
Show InChI InChI=1S/C17H13N5OS/c1-23-15(18)17-22-12-8-7-11-13(14(12)24-17)16(20-9-19-11)21-10-5-3-2-4-6-10/h2-9,18H,1H3,(H,19,20,21)
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n/an/a 3.48n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434356
PNG
(CHEMBL2386744 | US9446044, 44)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Br)cc4F)c3c2s1
Show InChI InChI=1S/C17H11BrFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 3.60n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246372
PNG
(US9446044, 47)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4cc5OCOc5c(Br)c4)c3c2s1
Show InChI InChI=1S/C18H12BrN5O3S/c1-25-16(20)18-24-11-3-2-10-13(15(11)28-18)17(22-6-21-10)23-8-4-9(19)14-12(5-8)26-7-27-14/h2-6,20H,7H2,1H3,(H,21,22,23)
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n/an/a 3.66n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434362
PNG
(CHEMBL2386766 | US9446044, 70)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(cc4)C#N)c3c2s1
Show InChI InChI=1S/C18H12N6OS/c1-25-16(20)18-24-13-7-6-12-14(15(13)26-18)17(22-9-21-12)23-11-4-2-10(8-19)3-5-11/h2-7,9,20H,1H3,(H,21,22,23)
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n/an/a 3.89n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434347
PNG
(CHEMBL2386753 | US9446044, 48)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc5OCOc5c4)c3c2s1
Show InChI InChI=1S/C18H13N5O3S/c1-24-16(19)18-23-11-4-3-10-14(15(11)27-18)17(21-7-20-10)22-9-2-5-12-13(6-9)26-8-25-12/h2-7,19H,8H2,1H3,(H,20,21,22)
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n/an/a 4.20n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246377
PNG
(US9446044, 54)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)c(O)c4)c3c2s1
Show InChI InChI=1S/C18H15N5O3S/c1-25-13-6-3-9(7-12(13)24)22-17-14-10(20-8-21-17)4-5-11-15(14)27-18(23-11)16(19)26-2/h3-8,19,24H,1-2H3,(H,20,21,22)
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n/an/a 4.25n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM246381
PNG
(US9446044, 59)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc5nc[nH]c5c4)c3c2s1
Show InChI InChI=1S/C18H13N7OS/c1-26-16(19)18-25-12-5-4-11-14(15(12)27-18)17(23-8-21-11)24-9-2-3-10-13(6-9)22-7-20-10/h2-8,19H,1H3,(H,20,22)(H,21,23,24)
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n/an/a 4.44n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM246381
PNG
(US9446044, 59)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc5nc[nH]c5c4)c3c2s1
Show InChI InChI=1S/C18H13N7OS/c1-26-16(19)18-25-12-5-4-11-14(15(12)27-18)17(23-8-21-11)24-9-2-3-10-13(6-9)22-7-20-10/h2-8,19H,1H3,(H,20,22)(H,21,23,24)
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n/an/a 4.65n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434338
PNG
(CHEMBL2386762 | US9446044, 56)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4)c3c2s1
Show InChI InChI=1S/C17H12ClN5OS/c1-24-15(19)17-23-12-7-6-11-13(14(12)25-17)16(21-8-20-11)22-10-4-2-9(18)3-5-10/h2-8,19H,1H3,(H,20,21,22)
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n/an/a 4.74n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434351
PNG
(CHEMBL2386749 | US9446044, 60)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(O)c(c4)[N+]([O-])=O)c3c2s1
Show InChI InChI=1S/C17H12N6O4S/c1-27-15(18)17-22-10-4-3-9-13(14(10)28-17)16(20-7-19-9)21-8-2-5-12(24)11(6-8)23(25)26/h2-7,18,24H,1H3,(H,19,20,21)
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n/an/a 4.91n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434340
PNG
(CHEMBL2386760 | US9446044, 89)
Show SMILES COC(=O)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H10Cl2N4O2S/c1-25-17(24)16-23-12-5-4-11-13(14(12)26-16)15(21-7-20-11)22-10-3-2-8(18)6-9(10)19/h2-7H,1H3,(H,20,21,22)
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n/an/a 5.10n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434351
PNG
(CHEMBL2386749 | US9446044, 60)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(O)c(c4)[N+]([O-])=O)c3c2s1
Show InChI InChI=1S/C17H12N6O4S/c1-27-15(18)17-22-10-4-3-9-13(14(10)28-17)16(20-7-19-9)21-8-2-5-12(24)11(6-8)23(25)26/h2-7,18,24H,1H3,(H,19,20,21)
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n/an/a 5.68n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Cyclin-dependent kinase 5 activator 1


(Homo sapiens (Human))
BDBM50304109
PNG
((Z)-5'-Nitro-1H,1'H-[2,3']biindolylidene-3,2'-dion...)
Show SMILES [O-][N+](=O)c1ccc2NC(=O)C(c2c1)c1[nH]c2ccccc2c1N=O
Show InChI InChI=1S/C16H10N4O4/c21-16-13(10-7-8(20(23)24)5-6-12(10)18-16)15-14(19-22)9-3-1-2-4-11(9)17-15/h1-7,13,17H,(H,18,21)
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Article
PubMed
n/an/a 6n/an/an/an/an/an/a



Universit£ de La Rochelle

Curated by ChEMBL


Assay Description
Inhibition of GST-fused CDK5/p25 expressed in Escherichia coli assessed as [gamma-33P]ATP incorporation after 10 mins by scintillation counting


Bioorg Med Chem 17: 6257-63 (2009)


Article DOI: 10.1016/j.bmc.2009.07.051
BindingDB Entry DOI: 10.7270/Q2BR8S9W
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434346
PNG
(CHEMBL2386754 | US9446044, 82)
Show SMILES CCOC(=N)c1nc2ccc3ncnc(Nc4ccc5OCOc5c4)c3c2s1
Show InChI InChI=1S/C19H15N5O3S/c1-2-25-17(20)19-24-12-5-4-11-15(16(12)28-19)18(22-8-21-11)23-10-3-6-13-14(7-10)27-9-26-13/h3-8,20H,2,9H2,1H3,(H,21,22,23)
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n/an/a 6.02n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50434363
PNG
(CHEMBL2386765 | US9446044, 66)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(F)cc4)c3c2s1
Show InChI InChI=1S/C17H12FN5OS/c1-24-15(19)17-23-12-7-6-11-13(14(12)25-17)16(21-8-20-11)22-10-4-2-9(18)3-5-10/h2-8,19H,1H3,(H,20,21,22)
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n/an/a 6.06n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434356
PNG
(CHEMBL2386744 | US9446044, 44)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Br)cc4F)c3c2s1
Show InChI InChI=1S/C17H11BrFN5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 6.55n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
Glycogen synthase kinase-3 alpha


(Homo sapiens (Human))
BDBM50434353
PNG
(CHEMBL2386747 | US9446044, 72)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(Cl)cc4Cl)c3c2s1
Show InChI InChI=1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
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n/an/a 7.40n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of GSK3A (unknown origin)


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1A


(Homo sapiens (Human))
BDBM50347750
PNG
(CHEMBL1802358)
Show SMILES O=C1NC(Nc2ccccc2)=NC1=Cc1ccc2OCOc2c1 |w:13.15,c:11|
Show InChI InChI=1S/C17H13N3O3/c21-16-13(8-11-6-7-14-15(9-11)23-10-22-14)19-17(20-16)18-12-4-2-1-3-5-12/h1-9H,10H2,(H2,18,19,20,21)
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n/an/a 7.60n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins


Citation and Details

BindingDB Entry DOI: 10.7270/Q2GH9NMG
More data for this
Ligand-Target Pair
Dual specificity tyrosine-phosphorylation-regulated kinase 1B


(Homo sapiens (Human))
BDBM50434362
PNG
(CHEMBL2386766 | US9446044, 70)
Show SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(cc4)C#N)c3c2s1
Show InChI InChI=1S/C18H12N6OS/c1-25-16(20)18-24-13-7-6-12-14(15(13)26-18)17(22-9-21-12)23-11-4-2-10(8-19)3-5-11/h2-7,9,20H,1H3,(H,21,22,23)
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n/an/a 7.69n/an/an/an/a7.525



DIAXONHIT

US Patent


Assay Description
The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...


US Patent US9446044 (2016)


BindingDB Entry DOI: 10.7270/Q2610Z7J
More data for this
Ligand-Target Pair
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