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Compile Data Set for Download or QSAR

Found 1793 hits of ph data with Target = 'Tyrosine-protein kinase SYK'   
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
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212270
PNG
(6-(6-amino-5-methylpyrazin-2-yl)-N-(4-(4-(oxetan-3...)
Show SMILES Cc1ncc(nc1N)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Show InChI InChI=1S/C24H27N9O/c1-16-22(25)29-20(12-27-16)21-13-33-7-6-26-24(33)23(30-21)28-17-2-4-18(5-3-17)31-8-10-32(11-9-31)19-14-34-15-19/h2-7,12-13,19H,8-11,14-15H2,1H3,(H2,25,29)(H,28,30)
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n/an/a 6.20n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212280
PNG
(US11517570, Example Kn.-4: | US9290505, 6-(6-amino...)
Show SMILES COc1ccc(Nc2nc(cn3ccnc23)-c2ccc(N)nc2)cc1OC
Show InChI InChI=1S/C19H18N6O2/c1-26-15-5-4-13(9-16(15)27-2)23-18-19-21-7-8-25(19)11-14(24-18)12-3-6-17(20)22-10-12/h3-11H,1-2H3,(H2,20,22)(H,23,24)
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n/an/a 53n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212272
PNG
((R)-(4-(4-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]p...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCO[C@@H](CO)C2)n1
Show InChI InChI=1S/C21H22N8O2/c22-19-10-23-9-17(26-19)18-12-29-6-5-24-21(29)20(27-18)25-14-1-3-15(4-2-14)28-7-8-31-16(11-28)13-30/h1-6,9-10,12,16,30H,7-8,11,13H2,(H2,22,26)(H,25,27)/t16-/m1/s1
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n/an/a 13.3n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212273
PNG
(6-(6-aminopyrazin-2-yl)-5-methyl-N-(4-(4-(oxetan-3...)
Show SMILES Cc1c(nc(Nc2ccc(cc2)N2CCN(CC2)C2COC2)c2nccn12)-c1cncc(N)n1
Show InChI InChI=1S/C24H27N9O/c1-16-22(20-12-26-13-21(25)29-20)30-23(24-27-6-7-33(16)24)28-17-2-4-18(5-3-17)31-8-10-32(11-9-31)19-14-34-15-19/h2-7,12-13,19H,8-11,14-15H2,1H3,(H2,25,29)(H,28,30)
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n/an/a 44n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212274
PNG
(2-(5-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]pyrazi...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(N3CCN(CC3)C3COC3)c(OCCO)c2)n1
Show InChI InChI=1S/C25H29N9O3/c26-23-13-27-12-19(30-23)20-14-34-4-3-28-25(34)24(31-20)29-17-1-2-21(22(11-17)37-10-9-35)33-7-5-32(6-8-33)18-15-36-16-18/h1-4,11-14,18,35H,5-10,15-16H2,(H2,26,30)(H,29,31)
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n/an/a 12.2n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212275
PNG
(2-((4-(4-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]py...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC(CO)CO)CC2)n1
Show InChI InChI=1S/C24H29N9O2/c25-22-12-26-11-20(29-22)21-14-33-6-5-27-24(33)23(30-21)28-18-1-3-19(4-2-18)32-9-7-31(8-10-32)13-17(15-34)16-35/h1-6,11-12,14,17,34-35H,7-10,13,15-16H2,(H2,25,29)(H,28,30)
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n/an/a 14.5n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212276
PNG
(2-(5-((6-(6-amino-5-methylpyrazin-2-yl)imidazo[1,2...)
Show SMILES Cc1ncc(nc1N)-c1cn2ccnc2c(Nc2ccc(N3CCN(CC3)C3COC3)c(OCCO)c2)n1
Show InChI InChI=1S/C26H31N9O3/c1-17-24(27)31-20(13-29-17)21-14-35-5-4-28-26(35)25(32-21)30-18-2-3-22(23(12-18)38-11-10-36)34-8-6-33(7-9-34)19-15-37-16-19/h2-5,12-14,19,36H,6-11,15-16H2,1H3,(H2,27,31)(H,30,32)
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n/an/a 8.70n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212277
PNG
(US11517570, Example Kn.-1: | US9290505, 6-(5-amino...)
Show SMILES Nc1cncc(c1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCOCC2)n1
Show InChI InChI=1S/C21H21N7O/c22-16-11-15(12-23-13-16)19-14-28-6-5-24-21(28)20(26-19)25-17-1-3-18(4-2-17)27-7-9-29-10-8-27/h1-6,11-14H,7-10,22H2,(H,25,26)
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n/an/a 31n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212278
PNG
(US11517570, Example Kn.-2: | US9290505, 6-(3-amino...)
Show SMILES COc1ccc(Nc2nc(cn3ccnc23)-c2cccc(N)c2)cc1OC
Show InChI InChI=1S/C20H19N5O2/c1-26-17-7-6-15(11-18(17)27-2)23-19-20-22-8-9-25(20)12-16(24-19)13-4-3-5-14(21)10-13/h3-12H,21H2,1-2H3,(H,23,24)
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n/an/a 188n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212279
PNG
(US11517570, Example Kn.-3: | US9290505, 6-(5-amino...)
Show SMILES Cc1ncc(cc1N)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCOCC2)n1
Show InChI InChI=1S/C22H23N7O/c1-15-19(23)12-16(13-25-15)20-14-29-7-6-24-22(29)21(27-20)26-17-2-4-18(5-3-17)28-8-10-30-11-9-28/h2-7,12-14H,8-11,23H2,1H3,(H,26,27)
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n/an/a 16n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212280
PNG
(US11517570, Example Kn.-4: | US9290505, 6-(6-amino...)
Show SMILES COc1ccc(Nc2nc(cn3ccnc23)-c2ccc(N)nc2)cc1OC
Show InChI InChI=1S/C19H18N6O2/c1-26-15-5-4-13(9-16(15)27-2)23-18-19-21-7-8-25(19)11-14(24-18)12-3-6-17(20)22-10-12/h3-11H,1-2H3,(H2,20,22)(H,23,24)
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n/an/a 53n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212270
PNG
(6-(6-amino-5-methylpyrazin-2-yl)-N-(4-(4-(oxetan-3...)
Show SMILES Cc1ncc(nc1N)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Show InChI InChI=1S/C24H27N9O/c1-16-22(25)29-20(12-27-16)21-13-33-7-6-26-24(33)23(30-21)28-17-2-4-18(5-3-17)31-8-10-32(11-9-31)19-14-34-15-19/h2-7,12-13,19H,8-11,14-15H2,1H3,(H2,25,29)(H,28,30)
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n/an/a 6.20n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212271
PNG
(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Show InChI InChI=1S/C23H25N9O/c24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18/h1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29)
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n/an/a 13.5n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212272
PNG
((R)-(4-(4-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]p...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCO[C@@H](CO)C2)n1
Show InChI InChI=1S/C21H22N8O2/c22-19-10-23-9-17(26-19)18-12-29-6-5-24-21(29)20(27-18)25-14-1-3-15(4-2-14)28-7-8-31-16(11-28)13-30/h1-6,9-10,12,16,30H,7-8,11,13H2,(H2,22,26)(H,25,27)/t16-/m1/s1
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n/an/a 13.3n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212273
PNG
(6-(6-aminopyrazin-2-yl)-5-methyl-N-(4-(4-(oxetan-3...)
Show SMILES Cc1c(nc(Nc2ccc(cc2)N2CCN(CC2)C2COC2)c2nccn12)-c1cncc(N)n1
Show InChI InChI=1S/C24H27N9O/c1-16-22(20-12-26-13-21(25)29-20)30-23(24-27-6-7-33(16)24)28-17-2-4-18(5-3-17)31-8-10-32(11-9-31)19-14-34-15-19/h2-7,12-13,19H,8-11,14-15H2,1H3,(H2,25,29)(H,28,30)
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n/an/a 44n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212274
PNG
(2-(5-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]pyrazi...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(N3CCN(CC3)C3COC3)c(OCCO)c2)n1
Show InChI InChI=1S/C25H29N9O3/c26-23-13-27-12-19(30-23)20-14-34-4-3-28-25(34)24(31-20)29-17-1-2-21(22(11-17)37-10-9-35)33-7-5-32(6-8-33)18-15-36-16-18/h1-4,11-14,18,35H,5-10,15-16H2,(H2,26,30)(H,29,31)
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n/an/a 12.2n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212275
PNG
(2-((4-(4-((6-(6-aminopyrazin-2-yl)imidazo[1,2-a]py...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC(CO)CO)CC2)n1
Show InChI InChI=1S/C24H29N9O2/c25-22-12-26-11-20(29-22)21-14-33-6-5-27-24(33)23(30-21)28-18-1-3-19(4-2-18)32-9-7-31(8-10-32)13-17(15-34)16-35/h1-6,11-12,14,17,34-35H,7-10,13,15-16H2,(H2,25,29)(H,28,30)
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n/an/a 14.5n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212276
PNG
(2-(5-((6-(6-amino-5-methylpyrazin-2-yl)imidazo[1,2...)
Show SMILES Cc1ncc(nc1N)-c1cn2ccnc2c(Nc2ccc(N3CCN(CC3)C3COC3)c(OCCO)c2)n1
Show InChI InChI=1S/C26H31N9O3/c1-17-24(27)31-20(13-29-17)21-14-35-5-4-28-26(35)25(32-21)30-18-2-3-22(23(12-18)38-11-10-36)34-8-6-33(7-9-34)19-15-37-16-19/h2-5,12-14,19,36H,6-11,15-16H2,1H3,(H2,27,31)(H,30,32)
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n/an/a 8.70n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212277
PNG
(US11517570, Example Kn.-1: | US9290505, 6-(5-amino...)
Show SMILES Nc1cncc(c1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCOCC2)n1
Show InChI InChI=1S/C21H21N7O/c22-16-11-15(12-23-13-16)19-14-28-6-5-24-21(28)20(26-19)25-17-1-3-18(4-2-17)27-7-9-29-10-8-27/h1-6,11-14H,7-10,22H2,(H,25,26)
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n/an/a 31n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212278
PNG
(US11517570, Example Kn.-2: | US9290505, 6-(3-amino...)
Show SMILES COc1ccc(Nc2nc(cn3ccnc23)-c2cccc(N)c2)cc1OC
Show InChI InChI=1S/C20H19N5O2/c1-26-17-7-6-15(11-18(17)27-2)23-19-20-22-8-9-25(20)12-16(24-19)13-4-3-5-14(21)10-13/h3-12H,21H2,1-2H3,(H,23,24)
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n/an/a 188n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212279
PNG
(US11517570, Example Kn.-3: | US9290505, 6-(5-amino...)
Show SMILES Cc1ncc(cc1N)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCOCC2)n1
Show InChI InChI=1S/C22H23N7O/c1-15-19(23)12-16(13-25-15)20-14-29-7-6-24-22(29)21(27-20)26-17-2-4-18(5-3-17)28-8-10-30-11-9-28/h2-7,12-14H,8-11,23H2,1H3,(H,26,27)
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n/an/a 16n/an/an/an/a7.025



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9504684 (2016)


BindingDB Entry DOI: 10.7270/Q2XS5TB7
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM212271
PNG
(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Show SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Show InChI InChI=1S/C23H25N9O/c24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18/h1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29)
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n/an/a 13.5n/an/an/an/a7.0n/a



Gilead Sciences, Inc.

US Patent


Assay Description
Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...


US Patent US9290505 (2016)


BindingDB Entry DOI: 10.7270/Q2TB15RT
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM50040727
PNG
(CHEMBL3353220 | US9255110, 7)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cnc(nc12)N(C)CCN
Show InChI InChI=1S/C20H20N6O2S/c1-26(7-5-21)20-23-10-17-18(25-20)13(11-29-17)19(27)24-15-8-12-4-3-6-22-14(12)9-16(15)28-2/h3-4,6,8-11H,5,7,21H2,1-2H3,(H,24,27)
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US Patent
n/an/a 410n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206177
PNG
(US9255110, 90)
Show SMILES OC1CCC(CC1)Oc1ccc(Cl)cc1NC(=O)c1cnn2cccnc12 |(5.33,-5,;4,-4.23,;2.67,-5,;1.33,-4.23,;1.33,-2.69,;2.67,-1.93,;4,-2.69,;,-1.93,;-1.33,-2.69,;-1.33,-4.23,;-2.67,-5,;-4,-4.23,;-5.33,-5,;-4,-2.69,;-2.67,-1.93,;-2.67,-.38,;-4,.38,;-5.33,-.38,;-4,1.93,;-5.33,2.69,;-5.33,4.23,;-2.67,4.23,;-1.33,5,;,4.23,;,2.69,;-1.33,1.93,;-2.67,2.69,)|
Show InChI InChI=1S/C19H19ClN4O3/c20-12-2-7-17(27-14-5-3-13(25)4-6-14)16(10-12)23-19(26)15-11-22-24-9-1-8-21-18(15)24/h1-2,7-11,13-14,25H,3-6H2,(H,23,26)
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n/an/a 806n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206104
PNG
(US9255110, 17)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cncnc12
Show InChI InChI=1S/C17H12N4O2S/c1-23-14-6-12-10(3-2-4-19-12)5-13(14)21-17(22)11-8-24-15-7-18-9-20-16(11)15/h2-9H,1H3,(H,21,22)
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n/an/a 622n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206108
PNG
(US9255110, 21)
Show SMILES CC(O)CC(C)Oc1cc2ncccc2cc1NC(=O)c1csc2cncnc12
Show InChI InChI=1S/C21H20N4O3S/c1-12(26)6-13(2)28-18-8-16-14(4-3-5-23-16)7-17(18)25-21(27)15-10-29-19-9-22-11-24-20(15)19/h3-5,7-13,26H,6H2,1-2H3,(H,25,27)
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n/an/a 449n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206110
PNG
(US9255110, 23)
Show SMILES OC1CCC(CC1)Oc1cc2ncccc2cc1NC(=O)c1cnn2cccnc12 |(5.35,-5.95,;4.26,-4.86,;2.78,-5.26,;1.69,-4.17,;2.09,-2.68,;3.57,-2.28,;4.66,-3.37,;1,-1.59,;-.49,-1.99,;-.89,-3.48,;-2.38,-3.88,;-2.78,-5.36,;-4.26,-5.76,;-5.35,-4.67,;-4.95,-3.19,;-3.47,-2.79,;-3.07,-1.3,;-1.58,-.9,;-1.18,.59,;-2.27,1.67,;-3.76,1.28,;-1.87,3.16,;-2.78,4.41,;-1.87,5.65,;-.41,5.18,;.93,5.95,;2.26,5.18,;2.26,3.64,;.93,2.87,;-.41,3.64,)|
Show InChI InChI=1S/C22H21N5O3/c28-15-4-6-16(7-5-15)30-20-12-18-14(3-1-8-23-18)11-19(20)26-22(29)17-13-25-27-10-2-9-24-21(17)27/h1-3,8-13,15-16,28H,4-7H2,(H,26,29)
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n/an/a 103n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206112
PNG
(US9255110, 25 | US9255110, 26 | US9255110, 27 | US...)
Show SMILES NCC1CCN(CC1)c1ccc(Cl)cc1NC(=O)c1cnn2cccnc12
Show InChI InChI=1S/C19H21ClN6O/c20-14-2-3-17(25-8-4-13(11-21)5-9-25)16(10-14)24-19(27)15-12-23-26-7-1-6-22-18(15)26/h1-3,6-7,10,12-13H,4-5,8-9,11,21H2,(H,24,27)
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n/an/a 725n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206117
PNG
(US9255110, 30)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cc(CO)cnc12
Show InChI InChI=1S/C19H15N3O3S/c1-25-16-7-14-12(3-2-4-20-14)6-15(16)22-19(24)13-10-26-17-5-11(9-23)8-21-18(13)17/h2-8,10,23H,9H2,1H3,(H,22,24)
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n/an/a 746n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206121
PNG
(US9255110, 34)
Show SMILES OCC1CCN(CC1)c1cc2CC(=O)Nc2cc1NC(=O)c1cnn2cccnc12
Show InChI InChI=1S/C21H22N6O3/c28-12-13-2-6-26(7-3-13)18-8-14-9-19(29)24-16(14)10-17(18)25-21(30)15-11-23-27-5-1-4-22-20(15)27/h1,4-5,8,10-11,13,28H,2-3,6-7,9,12H2,(H,24,29)(H,25,30)
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n/an/a 478n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206126
PNG
(US9255110, 39)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cnc(N[C@H](C)CO)nc12 |r|
Show InChI InChI=1S/C20H19N5O3S/c1-11(9-26)23-20-22-8-17-18(25-20)13(10-29-17)19(27)24-15-6-12-4-3-5-21-14(12)7-16(15)28-2/h3-8,10-11,26H,9H2,1-2H3,(H,24,27)(H,22,23,25)/t11-/m1/s1
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n/an/a 492n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206127
PNG
(US9255110, 40)
Show SMILES NC(=O)C1CCN(CC1)c1ccc(Cl)cc1NC(=O)c1cnn2cccnc12
Show InChI InChI=1S/C19H19ClN6O2/c20-13-2-3-16(25-8-4-12(5-9-25)17(21)27)15(10-13)24-19(28)14-11-23-26-7-1-6-22-18(14)26/h1-3,6-7,10-12H,4-5,8-9H2,(H2,21,27)(H,24,28)
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n/an/a 500n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206130
PNG
(US9255110, 43)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cnc(NC3CC3)nc12
Show InChI InChI=1S/C20H17N5O2S/c1-27-16-8-14-11(3-2-6-21-14)7-15(16)24-19(26)13-10-28-17-9-22-20(25-18(13)17)23-12-4-5-12/h2-3,6-10,12H,4-5H2,1H3,(H,24,26)(H,22,23,25)
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n/an/a 810n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206132
PNG
(US9255110, 45)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cnc(NCCO)nc12
Show InChI InChI=1S/C19H17N5O3S/c1-27-15-8-13-11(3-2-4-20-13)7-14(15)23-18(26)12-10-28-16-9-22-19(21-5-6-25)24-17(12)16/h2-4,7-10,25H,5-6H2,1H3,(H,23,26)(H,21,22,24)
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n/an/a 216n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206138
PNG
(US9255110, 51)
Show SMILES NCCCOc1cc2ncccc2cc1NC(=O)c1csc2cncnc12
Show InChI InChI=1S/C19H17N5O2S/c20-4-2-6-26-16-8-14-12(3-1-5-22-14)7-15(16)24-19(25)13-10-27-17-9-21-11-23-18(13)17/h1,3,5,7-11H,2,4,6,20H2,(H,24,25)
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n/an/a 376n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206140
PNG
(US9255110, 53)
Show SMILES COc1ccc(Cl)cc1NC(=O)c1csc2cnc(NCCN)nc12
Show InChI InChI=1S/C16H16ClN5O2S/c1-24-12-3-2-9(17)6-11(12)21-15(23)10-8-25-13-7-20-16(19-5-4-18)22-14(10)13/h2-3,6-8H,4-5,18H2,1H3,(H,21,23)(H,19,20,22)
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n/an/a 350n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206141
PNG
(US9255110, 54)
Show SMILES O[C@H]1CC[C@H](C1)Oc1cc2ncccc2cc1NC(=O)c1csc2cncnc12 |r|
Show InChI InChI=1S/C21H18N4O3S/c26-13-3-4-14(7-13)28-18-8-16-12(2-1-5-23-16)6-17(18)25-21(27)15-10-29-19-9-22-11-24-20(15)19/h1-2,5-6,8-11,13-14,26H,3-4,7H2,(H,25,27)/t13-,14+/m0/s1
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US Patent
n/an/a 500n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206142
PNG
(US9255110, 55)
Show SMILES OC1CCC(CC1)Oc1cc2ccccc2cc1NC(=O)c1cnn2cccnc12 |(5.33,-3.85,;4,-3.08,;2.67,-3.85,;1.33,-3.08,;1.33,-1.54,;2.67,-.77,;4,-1.54,;,-.77,;-1.33,-1.54,;-1.33,-3.08,;-2.67,-3.85,;-2.67,-5.39,;-4,-6.16,;-5.33,-5.39,;-5.33,-3.85,;-4,-3.08,;-4,-1.54,;-2.67,-.77,;-2.67,.77,;-4,1.54,;-5.33,.77,;-4,3.08,;-5.33,3.85,;-5.33,5.39,;-2.67,5.39,;-1.33,6.16,;,5.39,;,3.85,;-1.33,3.08,;-2.67,3.85,)|
Show InChI InChI=1S/C23H22N4O3/c28-17-6-8-18(9-7-17)30-21-13-16-5-2-1-4-15(16)12-20(21)26-23(29)19-14-25-27-11-3-10-24-22(19)27/h1-5,10-14,17-18,28H,6-9H2,(H,26,29)
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US Patent
n/an/a 628n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206170
PNG
(US9255110, 83)
Show SMILES OC1CCC(C1)Oc1ccc(Cl)cc1NC(=O)c1cnn2cccnc12
Show InChI InChI=1S/C18H17ClN4O3/c19-11-2-5-16(26-13-4-3-12(24)9-13)15(8-11)22-18(25)14-10-21-23-7-1-6-20-17(14)23/h1-2,5-8,10,12-13,24H,3-4,9H2,(H,22,25)
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US Patent
n/an/a 656n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM206098
PNG
(US9255110, 11)
Show SMILES COc1cc2ncccc2cc1NC(=O)c1csc2cnc(NCCN)nc12
Show InChI InChI=1S/C19H18N6O2S/c1-27-15-8-13-11(3-2-5-21-13)7-14(15)24-18(26)12-10-28-16-9-23-19(22-6-4-20)25-17(12)16/h2-3,5,7-10H,4,6,20H2,1H3,(H,24,26)(H,22,23,25)
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US Patent
n/an/a 17n/an/an/an/a7.225



ROCHE PALO ALTO LLC; HOFFMANN-LA ROCHE INC.

US Patent


Assay Description
SYK activity is measured by phosphorylation of a peptide substrate (Biotin-EPEGDYEEVLE) with [gamma-33P] ATP. The enzyme reaction was conducted at 20...


US Patent US9255110 (2016)


BindingDB Entry DOI: 10.7270/Q2XG9PZ2
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM255515
PNG
(US10828301, Compound R950368 | US9499493, R950368)
Show SMILES CNC(=O)COc1cccc(Nc2ncc(F)c(Nc3ccc4OCCC(N)c4c3)n2)c1
Show InChI InChI=1S/C22H23FN6O3/c1-25-20(30)12-32-15-4-2-3-13(9-15)28-22-26-11-17(23)21(29-22)27-14-5-6-19-16(10-14)18(24)7-8-31-19/h2-6,9-11,18H,7-8,12,24H2,1H3,(H,25,30)(H2,26,27,28,29)
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US Patent
n/an/a 10.7n/an/an/an/a7.425



Rigel Pharmaceuticals, Inc.

US Patent


Assay Description
Several 2,4-pyrimidinediamine compounds were tested for the ability to inhibit Syk kinase catalyzed phosphorylation of a peptide substrate in a bioch...


US Patent US9499493 (2016)


BindingDB Entry DOI: 10.7270/Q2WW7GKQ
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM255526
PNG
(N4-(3-Methylcarbonyloximephenyl)-5-fluoro-N2-[3-(N...)
Show SMILES CNC(=O)COC1=C(C)CCC(Nc2ncc(F)c(Nc3cccc(c3)C(=O)NOC)n2)=C1 |c:6,33|
Show InChI InChI=1S/C22H25FN6O4/c1-13-7-8-16(10-18(13)33-12-19(30)24-2)27-22-25-11-17(23)20(28-22)26-15-6-4-5-14(9-15)21(31)29-32-3/h4-6,9-11H,7-8,12H2,1-3H3,(H,24,30)(H,29,31)(H2,25,26,27,28)
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US Patent
n/an/a 66.5n/an/an/an/a7.425



Rigel Pharmaceuticals, Inc.

US Patent


Assay Description
Several 2,4-pyrimidinediamine compounds were tested for the ability to inhibit Syk kinase catalyzed phosphorylation of a peptide substrate in a bioch...


US Patent US9499493 (2016)


BindingDB Entry DOI: 10.7270/Q2WW7GKQ
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM5057
PNG
(1,2,4-Oxadiazole Analogue 4b | 4-[(2S)-2-{[(1S)-3-...)
Show SMILES CC(=O)N[C@@H](Cc1ccc(OP(O)(O)=O)cc1)C(=O)N[C@@H](CCC(N)=O)c1nc(Cc2ccc(C)cc2)no1 |r|
Show InChI InChI=1S/C25H30N5O8P/c1-15-3-5-18(6-4-15)14-23-29-25(37-30-23)20(11-12-22(26)32)28-24(33)21(27-16(2)31)13-17-7-9-19(10-8-17)38-39(34,35)36/h3-10,20-21H,11-14H2,1-2H3,(H2,26,32)(H,27,31)(H,28,33)(H2,34,35,36)/t20-,21-/m0/s1
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n/an/a>5.00E+5n/an/an/an/a7.422



ARIAD Pharmaceuticals, Inc.



Assay Description
Fluorescence polarization competitive binding assays were used to measure the IC50s of compounds binding to the different SH2 domains. The difference...


J Med Chem 42: 4088-98 (1999)


Article DOI: 10.1021/jm990229t
BindingDB Entry DOI: 10.7270/Q27D2SBP
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM5059
PNG
(1,2,4-Oxadiazole Analogue 4d | 4-[(2S)-2-{[(1S)-3-...)
Show SMILES CC(=O)N[C@@H](Cc1ccc(OP(O)(O)=O)cc1)C(=O)N[C@@H](CCC(N)=O)c1nc(Cc2ccc(Cl)cc2)no1 |r|
Show InChI InChI=1S/C24H27ClN5O8P/c1-14(31)27-20(12-15-4-8-18(9-5-15)38-39(34,35)36)23(33)28-19(10-11-21(26)32)24-29-22(30-37-24)13-16-2-6-17(25)7-3-16/h2-9,19-20H,10-13H2,1H3,(H2,26,32)(H,27,31)(H,28,33)(H2,34,35,36)/t19-,20-/m0/s1
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n/an/a>5.00E+5n/an/an/an/a7.422



ARIAD Pharmaceuticals, Inc.



Assay Description
Fluorescence polarization competitive binding assays were used to measure the IC50s of compounds binding to the different SH2 domains. The difference...


J Med Chem 42: 4088-98 (1999)


Article DOI: 10.1021/jm990229t
BindingDB Entry DOI: 10.7270/Q27D2SBP
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM5061
PNG
(1,2,4-Oxadiazole Analogue 4g | 4-[(2S)-2-{[(1S)-3-...)
Show SMILES CC(=O)N[C@@H](Cc1ccc(OP(O)(O)=O)cc1)C(=O)N[C@@H](CCC(N)=O)c1nc(Cc2ccc(Cl)cc2Cl)no1 |r|
Show InChI InChI=1S/C24H26Cl2N5O8P/c1-13(32)28-20(10-14-2-6-17(7-3-14)39-40(35,36)37)23(34)29-19(8-9-21(27)33)24-30-22(31-38-24)11-15-4-5-16(25)12-18(15)26/h2-7,12,19-20H,8-11H2,1H3,(H2,27,33)(H,28,32)(H,29,34)(H2,35,36,37)/t19-,20-/m0/s1
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n/an/a>5.00E+5n/an/an/an/a7.422



ARIAD Pharmaceuticals, Inc.



Assay Description
Fluorescence polarization competitive binding assays were used to measure the IC50s of compounds binding to the different SH2 domains. The difference...


J Med Chem 42: 4088-98 (1999)


Article DOI: 10.1021/jm990229t
BindingDB Entry DOI: 10.7270/Q27D2SBP
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM5063
PNG
(1,2,4-Oxadiazole Analogue 4i | 4-[(2S)-2-{[(1S)-3-...)
Show SMILES CC(=O)N[C@@H](Cc1ccc(OP(O)(O)=O)cc1)C(=O)N[C@@H](CCC(N)=O)c1nc(Cc2cccc3ccccc23)no1 |r|
Show InChI InChI=1S/C28H30N5O8P/c1-17(34)30-24(15-18-9-11-21(12-10-18)41-42(37,38)39)27(36)31-23(13-14-25(29)35)28-32-26(33-40-28)16-20-7-4-6-19-5-2-3-8-22(19)20/h2-12,23-24H,13-16H2,1H3,(H2,29,35)(H,30,34)(H,31,36)(H2,37,38,39)/t23-,24-/m0/s1
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n/an/a>5.00E+5n/an/an/an/a7.422



ARIAD Pharmaceuticals, Inc.



Assay Description
Fluorescence polarization competitive binding assays were used to measure the IC50s of compounds binding to the different SH2 domains. The difference...


J Med Chem 42: 4088-98 (1999)


Article DOI: 10.1021/jm990229t
BindingDB Entry DOI: 10.7270/Q27D2SBP
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM92624
PNG
(Dimethoxyquinoline, 1)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)N[C@@H]4C[C@H]4c4ccccc4)nc3)c2cc1OC |r|
Show InChI InChI=1S/C26H24N4O4/c1-32-23-13-19-20(14-24(23)33-2)27-11-10-22(19)34-17-8-9-25(28-15-17)30-26(31)29-21-12-18(21)16-6-4-3-5-7-16/h3-11,13-15,18,21H,12H2,1-2H3,(H2,28,29,30,31)/t18-,21+/m0/s1
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n/an/a 320n/an/an/an/a7.425



Pfizer



Assay Description
A Lance TR-FRET assay (Perkin Elmer) was used to measure and compare the potency of compounds against Syk kinase domain.


Chem Biol Drug Des 80: 657-64 (2012)


Article DOI: 10.1111/j.1747-0285.2012.01443.x
BindingDB Entry DOI: 10.7270/Q2BG2MKC
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM92625
PNG
(Dimethoxyquinoline, 2)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)c4cccn(Cc5ccccc5)c4=O)nc3)c2cc1OC
Show InChI InChI=1S/C29H24N4O5/c1-36-25-15-22-23(16-26(25)37-2)30-13-12-24(22)38-20-10-11-27(31-17-20)32-28(34)21-9-6-14-33(29(21)35)18-19-7-4-3-5-8-19/h3-17H,18H2,1-2H3,(H,31,32,34)
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n/an/a 100n/an/an/an/a7.425



Pfizer



Assay Description
A Lance TR-FRET assay (Perkin Elmer) was used to measure and compare the potency of compounds against Syk kinase domain.


Chem Biol Drug Des 80: 657-64 (2012)


Article DOI: 10.1111/j.1747-0285.2012.01443.x
BindingDB Entry DOI: 10.7270/Q2BG2MKC
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM92626
PNG
(Pyrido analog, 3)
Show SMILES Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1-c1cc2cnc(Nc3ccccc3)nc2n(C)c1=O
Show InChI InChI=1S/C29H22F3N5O2/c1-17-11-12-22(34-26(38)18-7-6-8-20(13-18)29(30,31)32)15-23(17)24-14-19-16-33-28(35-21-9-4-3-5-10-21)36-25(19)37(2)27(24)39/h3-16H,1-2H3,(H,34,38)(H,33,35,36)
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n/an/a 2.10n/an/an/an/a7.425



Pfizer



Assay Description
A Lance TR-FRET assay (Perkin Elmer) was used to measure and compare the potency of compounds against Syk kinase domain.


Chem Biol Drug Des 80: 657-64 (2012)


Article DOI: 10.1111/j.1747-0285.2012.01443.x
BindingDB Entry DOI: 10.7270/Q2BG2MKC
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Tyrosine-protein kinase SYK


(Homo sapiens (Human))
BDBM50419247
PNG
(CHEMBL1835071 | US8470835, 1)
Show SMILES Cc1ccc(Nc2nc(N[C@@H]3CCOC[C@@H]3N)ncc2C(N)=O)cc1 |r|
Show InChI InChI=1S/C17H22N6O2/c1-10-2-4-11(5-3-10)21-16-12(15(19)24)8-20-17(23-16)22-14-6-7-25-9-13(14)18/h2-5,8,13-14H,6-7,9,18H2,1H3,(H2,19,24)(H2,20,21,22,23)/t13-,14+/m0/s1
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n/an/a 40n/an/an/an/a7.425



Glaxo Group Limited

US Patent


Assay Description
Recombinant human Syk was express as a His-tagged protein. The activity of Syk was asses using a time-resolved fluorescence resonance entery transfe...


US Patent US8470835 (2013)


BindingDB Entry DOI: 10.7270/Q28S4NJK
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
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