Found 640 hits of ic50 for UniProtKB: Q9Y463 Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kcal/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434358
(CHEMBL2386770 | US9446044, 68)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) | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet 
| CHEMBL
PC cid
PC sid
UniChem
Similars
| US Patent
| n/a | n/a | 0.240 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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
(CHEMBL2386744 | US9446044, 44)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) | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 0.240 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434353
(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) | PDB
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CHEMBL
MCE
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UniChem
Similars
| PubMed
| n/a | n/a | 0.280 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM50434353
(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) | PDB
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| US Patent
| n/a | n/a | 0.280 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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
(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) | PDB
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| Article
PubMed
| n/a | n/a | 0.280 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434353
(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) | PDB
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| Article
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| n/a | n/a | 0.280 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113949
BindingDB Entry DOI: 10.7270/Q2M90DP7 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434353
(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) | PDB
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| PubMed
| n/a | n/a | 0.280 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM401571
(US10005769, No. 35)Show SMILES O=C(Nc1nc2cc(ccc2[nH]1)C(=O)NCC1CCCO1)c1csc(n1)-c1ccc2OCCc2c1 | PDB
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| PC cid
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| US Patent
| n/a | n/a | <0.5 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434355
(CHEMBL2386745)Show InChI InChI=1S/C18H14FN5O2S/c1-25-13-7-9(19)3-4-10(13)23-17-14-11(21-8-22-17)5-6-12-15(14)27-18(24-12)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23) | PDB
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| CHEMBL
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UniChem
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| Article
PubMed
| n/a | n/a | 0.590 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM246383
(US9446044, 69)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) | PDB
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| Article
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| n/a | n/a | 0.590 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113949
BindingDB Entry DOI: 10.7270/Q2M90DP7 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM246383
(US9446044, 69)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) | PDB
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| US Patent
| n/a | n/a | 0.590 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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
(US9446044, 69)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) | PDB
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| PubMed
| n/a | n/a | 0.590 | n/a | n/a | n/a | n/a | n/a | n/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
(US9446044, 69)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) | PDB
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PC sid
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| PubMed
| n/a | n/a | 0.590 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM401559
(US10005769, No. 23)Show SMILES COCCNC(=O)c1ccc2[nH]c(NC(=O)c3csc(n3)-c3ccc4OCCc4c3)nc2c1 Show InChI InChI=1S/C23H21N5O4S/c1-31-9-7-24-20(29)14-2-4-16-17(11-14)27-23(26-16)28-21(30)18-12-33-22(25-18)15-3-5-19-13(10-15)6-8-32-19/h2-5,10-12H,6-9H2,1H3,(H,24,29)(H2,26,27,28,30) | PDB
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| PC cid
PC sid
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| US Patent
| n/a | n/a | 0.699 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401558
(US10005769, No. 22)Show SMILES O=C(Nc1nc2cc(ccc2[nH]1)C(=O)N1CCCC1)c1csc(n1)-c1ccc2OCCc2c1 Show InChI InChI=1S/C24H21N5O3S/c30-21(19-13-33-22(25-19)15-4-6-20-14(11-15)7-10-32-20)28-24-26-17-5-3-16(12-18(17)27-24)23(31)29-8-1-2-9-29/h3-6,11-13H,1-2,7-10H2,(H2,26,27,28,30) | PDB
UniProtKB/SwissProt
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 0.852 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM2579
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 | PDB
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| Article
PubMed
| n/a | n/a | 0.967 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Florida
Curated by ChEMBL
| Assay Description
Inhibition of human DYRK1B using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay |
Eur J Med Chem 161: 456-467 (2019)
Article DOI: 10.1016/j.ejmech.2018.10.052
BindingDB Entry DOI: 10.7270/Q2W380MT |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50081185
(CHEMBL3421963)Show SMILES COc1cc(ccc1Nc1cc(ncn1)-c1c[nH]c2cnccc12)N1CCN(C)CC1 Show InChI InChI=1S/C23H25N7O/c1-29-7-9-30(10-8-29)16-3-4-19(22(11-16)31-2)28-23-12-20(26-15-27-23)18-13-25-21-14-24-6-5-17(18)21/h3-6,11-15,25H,7-10H2,1-2H3,(H,26,27,28) | PDB
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| CHEMBL
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| Article
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca
Curated by ChEMBL
| Assay Description
Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins |
J Med Chem 58: 2834-44 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00098
BindingDB Entry DOI: 10.7270/Q23B61VW |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581233
(CHEMBL5091510) | PDB
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| PC cid
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| Article
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581236
(CHEMBL5090676) | PDB
UniProtKB/SwissProt
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| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581238
(CHEMBL5092157)Show SMILES Cc1nc(NCc2ccccc2)c2c(c[nH]c2n1)-c1ccnc(N)c1 | PDB
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| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581239
(CHEMBL5082044) | PDB
UniProtKB/SwissProt
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GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581240
(CHEMBL5083159) | PDB
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434352
(CHEMBL2386748 | US9446044, 78)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) | PDB
UniProtKB/SwissProt
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| CHEMBL
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PC sid
UniChem
Similars
| US Patent
| n/a | n/a | 1.07 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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
(CHEMBL2386748 | US9446044, 78)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) | PDB
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| Article
PubMed
| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113949
BindingDB Entry DOI: 10.7270/Q2M90DP7 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434352
(CHEMBL2386748 | US9446044, 78)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) | PDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM2579
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 | PDB
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| Article
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human DYRK1B using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay |
Citation and Details
Article DOI: 10.1016/j.bmc.2018.02.022
BindingDB Entry DOI: 10.7270/Q2DJ5KB8 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434352
(CHEMBL2386748 | US9446044, 78)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) | PDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401537
(US10005769, No. 1)Show SMILES O=C(Nc1nc2cc(ccc2[nH]1)C#N)c1csc(n1)-c1ccc2OCCc2c1 Show InChI InChI=1S/C20H13N5O2S/c21-9-11-1-3-14-15(7-11)24-20(23-14)25-18(26)16-10-28-19(22-16)13-2-4-17-12(8-13)5-6-27-17/h1-4,7-8,10H,5-6H2,(H2,23,24,25,26) | PDB
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| US Patent
| n/a | n/a | 1.38 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401539
(US10005769, No. 3)Show SMILES CS(=O)(=O)c1ccc2[nH]c(NC(=O)c3csc(n3)-c3ccc4OCCc4c3)nc2c1 Show InChI InChI=1S/C20H16N4O4S2/c1-30(26,27)13-3-4-14-15(9-13)23-20(22-14)24-18(25)16-10-29-19(21-16)12-2-5-17-11(8-12)6-7-28-17/h2-5,8-10H,6-7H2,1H3,(H2,22,23,24,25) | PDB
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| PC cid
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| US Patent
| n/a | n/a | 1.49 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434354
(CHEMBL2386746)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(19)6-9(10)18/h2-7,20H,1H3,(H,21,22,23) | PDB
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| CHEMBL
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| Article
PubMed
| n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM246384
(US9446044, 71)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) | PDB
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| PC cid
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UniChem
| PubMed
| n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/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
(US9446044, 71)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) | PDB
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| PC cid
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| Article
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| n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113949
BindingDB Entry DOI: 10.7270/Q2M90DP7 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM246384
(US9446044, 71)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) | PDB
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| PC cid
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UniChem
| US Patent
| n/a | n/a | 1.63 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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)) | BDBM401543
(US10005769, No. 7)Show SMILES CN(C)C(=O)c1ccc2[nH]c(NC(=O)c3csc(n3)-c3ccc4OCCc4c3)nc2c1 Show InChI InChI=1S/C22H19N5O3S/c1-27(2)21(29)14-3-5-15-16(10-14)25-22(24-15)26-19(28)17-11-31-20(23-17)13-4-6-18-12(9-13)7-8-30-18/h3-6,9-11H,7-8H2,1-2H3,(H2,24,25,26,28) | PDB
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| PC cid
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| US Patent
| n/a | n/a | 1.74 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401542
(US10005769, No. 6)Show SMILES Clc1ccc2[nH]c(NC(=O)c3csc(n3)-c3ccc4OCCc4c3)nc2c1 Show InChI InChI=1S/C19H13ClN4O2S/c20-12-2-3-13-14(8-12)23-19(22-13)24-17(25)15-9-27-18(21-15)11-1-4-16-10(7-11)5-6-26-16/h1-4,7-9H,5-6H2,(H2,22,23,24,25) | PDB
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| PC cid
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UniChem
| US Patent
| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50081186
(CHEMBL3421962)Show SMILES CN1CCN(CC1)c1ccc(Nc2cc(ncn2)-c2c[nH]c3cnccc23)cc1 Show InChI InChI=1S/C22H23N7/c1-28-8-10-29(11-9-28)17-4-2-16(3-5-17)27-22-12-20(25-15-26-22)19-13-24-21-14-23-7-6-18(19)21/h2-7,12-15,24H,8-11H2,1H3,(H,25,26,27) | PDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca
Curated by ChEMBL
| Assay Description
Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins |
J Med Chem 58: 2834-44 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00098
BindingDB Entry DOI: 10.7270/Q23B61VW |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50571345
(CHEMBL4872233)Show SMILES COc1ccc(cc1)-c1n[nH]c2ncc(cc12)-c1ccc(NC(N)=O)cc1 | PDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) |
Citation and Details
Article DOI: 10.1016/j.bmcl.2021.128226
BindingDB Entry DOI: 10.7270/Q26Q2209 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM293424
(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) | PDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.bmc.2022.116914
BindingDB Entry DOI: 10.7270/Q2HH6Q1V |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401578
(US10005769, No. 42)Show SMILES O=C(Nc1nc(n[nH]1)-c1ccncc1)c1csc(n1)-c1ccc2OCCc2c1 Show InChI InChI=1S/C19H14N6O2S/c26-17(23-19-22-16(24-25-19)11-3-6-20-7-4-11)14-10-28-18(21-14)13-1-2-15-12(9-13)5-8-27-15/h1-4,6-7,9-10H,5,8H2,(H2,22,23,24,25,26) | PDB
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| PC cid
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| US Patent
| n/a | n/a | 2.06 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401583
(US10005769, No. 47)Show SMILES CCN1CCN(CC1)C(=O)c1ccc2[nH]c(NC(=O)c3csc(n3)-c3ccc4OCCc4c3)nc2c1 Show InChI InChI=1S/C26H26N6O3S/c1-2-31-8-10-32(11-9-31)25(34)18-3-5-19-20(14-18)29-26(28-19)30-23(33)21-15-36-24(27-21)17-4-6-22-16(13-17)7-12-35-22/h3-6,13-15H,2,7-12H2,1H3,(H2,28,29,30,33) | PDB
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| PC cid
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| US Patent
| n/a | n/a | 2.17 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434364
(CHEMBL2386764 | US9446044, 65)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) | PDB
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Similars
| PubMed
| n/a | n/a | 2.80 | n/a | n/a | n/a | n/a | n/a | n/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
(CHEMBL2386764 | US9446044, 65)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) | PDB
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| n/a | n/a | 2.80 | n/a | n/a | n/a | n/a | n/a | n/a |
Dart Neuroscience LLC
Curated by ChEMBL
| Assay Description
Inhibition of recombinant DYRK1B (unknown origin) after 120 mins in presence of [33P]-ATP |
ACS Med Chem Lett 4: 502-3 (2013)
Article DOI: 10.1021/ml400137s
BindingDB Entry DOI: 10.7270/Q2NK3GDP |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434364
(CHEMBL2386764 | US9446044, 65)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) | PDB
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| n/a | n/a | 2.80 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2021.113949
BindingDB Entry DOI: 10.7270/Q2M90DP7 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM401581
(US10005769, No. 45)Show SMILES O=C(Nc1nc(n[nH]1)-c1cccnc1)c1csc(n1)-c1ccc2OCCc2c1 Show InChI InChI=1S/C19H14N6O2S/c26-17(23-19-22-16(24-25-19)13-2-1-6-20-9-13)14-10-28-18(21-14)12-3-4-15-11(8-12)5-7-27-15/h1-4,6,8-10H,5,7H2,(H2,22,23,24,25,26) | PDB
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| PC cid
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| US Patent
| n/a | n/a | 2.81 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer
| Assay Description
The substrate DYRKtide (synthetic peptide RRRFRPASPLRGPPK) was dissolved in freshly prepared Base Reaction Buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2,... |
Bioorg Med Chem Lett 19: 908-11 (2009)
BindingDB Entry DOI: 10.7270/Q2F19224 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50434364
(CHEMBL2386764 | US9446044, 65)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) | PDB
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| n/a | n/a | 2.83 | n/a | n/a | n/a | n/a | 7.5 | 25 |
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)) | BDBM2579
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 | PDB
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TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) |
Citation and Details
Article DOI: 10.1016/j.bmcl.2021.128226
BindingDB Entry DOI: 10.7270/Q26Q2209 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50571338
(CHEMBL4873449)Show SMILES Oc1ccc(cc1)-c1n[nH]c2ncc(cc12)-c1ccc(O)c(O)c1 | PDB
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TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) |
Citation and Details
Article DOI: 10.1016/j.bmcl.2021.128226
BindingDB Entry DOI: 10.7270/Q26Q2209 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50581211
(CHEMBL5093650)Show SMILES Cc1nc(NCc2c(F)cccc2F)c2c(c[nH]c2n1)-c1ccnc(N)c1 | PDB
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TBA
| Assay Description
Inhibition of DYRK1B (unknown origin) by TR FRET assay |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00024
BindingDB Entry DOI: 10.7270/Q28W3J52 |
More data for this
Ligand-Target Pair | |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50081174
(CHEMBL3421968)Show SMILES COc1cc(ccc1Nc1nccc(n1)-c1cn(C)c2cnccc12)N1CCN(C)CC1 Show InChI InChI=1S/C24H27N7O/c1-29-10-12-31(13-11-29)17-4-5-21(23(14-17)32-3)28-24-26-9-7-20(27-24)19-16-30(2)22-15-25-8-6-18(19)22/h4-9,14-16H,10-13H2,1-3H3,(H,26,27,28) | PDB
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AstraZeneca
Curated by ChEMBL
| Assay Description
Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins |
J Med Chem 58: 2834-44 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00098
BindingDB Entry DOI: 10.7270/Q23B61VW |
More data for this
Ligand-Target Pair | 
3D Structure (crystal) |
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
(Homo sapiens (Human)) | BDBM50081188
(CHEMBL3421981)Show InChI InChI=1S/C14H10N4/c1-4-15-8-13-10(1)12(7-18-13)9-2-5-16-14-11(9)3-6-17-14/h1-8,18H,(H,16,17) | PDB
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AstraZeneca
Curated by ChEMBL
| Assay Description
Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins |
J Med Chem 58: 2834-44 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00098
BindingDB Entry DOI: 10.7270/Q23B61VW |
More data for this
Ligand-Target Pair | |
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