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Compile Data Set for Download or QSAR

Marvin 2D Structure

Wt: 457.5
BDBM212270		Wt: 443.5
BDBM212271Purchase		Wt: 418.4
BDBM212272		Wt: 457.5
BDBM212273		Wt: 503.5
BDBM212274
Wt: 475.5
BDBM212275		Wt: 517.5
BDBM212276		Wt: 387.4
BDBM212277		Wt: 361.3
BDBM212278		Wt: 401.4
BDBM212279
Wt: 362.3
BDBM212280		Wt: 542.6
BDBM324284Purchase

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 106 hits in this display   
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 BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a<0.5n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human BTK using fluorescein-labeled polyGAT peptide as substrate incubated for 30 mins by FRET assay

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00926
BindingDB Entry DOI: 10.7270/Q23B641C
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Tyrosine-protein kinase BTK [14-552]


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a<1n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a<1n/an/an/an/an/an/a



BIOGEN MA INC.

US Patent


Assay Description
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...

US Patent US10189829 (2019)


BindingDB Entry DOI: 10.7270/Q2V69MP8
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Tyrosine-protein kinase BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a<1n/an/an/an/an/an/a



BIOGEN MA INC.

US Patent


Assay Description
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...

US Patent US10961237 (2021)


BindingDB Entry DOI: 10.7270/Q2GH9N29
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Tyrosine-protein kinase BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a 5.40n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of BTK in anti-IgM stimulated human PBMC cells assessed as reduction in PLCgamma2 phosphorylation

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00926
BindingDB Entry DOI: 10.7270/Q23B641C
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
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 6.20n/an/an/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) using XL665-labeled peptide as substrate in presence of ATP measured after 30 mins by TR-FRET assay

ACS Med Chem Lett 11: 506-513 (2020)


Article DOI: 10.1021/acsmedchemlett.9b00621
BindingDB Entry DOI: 10.7270/Q2ZG6WR1
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
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/a7.0n/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))		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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TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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))		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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
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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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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
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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TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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))		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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
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))		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))		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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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/an/an/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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
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/an/an/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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
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/a7.025



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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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))		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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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))		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))		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/an/an/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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/a



KRONOS BIO, 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 US10828299 (2020)


BindingDB Entry DOI: 10.7270/Q2PK0K6D
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/an/an/a



University of Wisconsin-Milwaukee



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

Bioorg Med Chem 16: 8853-62 (2008)


BindingDB Entry DOI: 10.7270/Q2K076M3
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))		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/an/an/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 US10342794 (2019)


BindingDB Entry DOI: 10.7270/Q2R49T3H
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))		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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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))		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))		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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
More data for this
Ligand-Target Pair
Tyrosine-protein kinase BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a 22n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human BTK assessed as reduction in OVA323-329 specific T cells proliferation

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00926
BindingDB Entry DOI: 10.7270/Q23B641C
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Tyrosine-protein kinase BTK


(Homo sapiens (Human))		BDBM324284
PNG
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
Show SMILES Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(Cc3c2)C2COC2)NC(=O)c2cn(nn2)C(C)(C)C)cn1 |r|
Show InChI InChI=1S/C28H34N10O2/c1-28(2,3)38-15-25(34-35-38)26(39)32-24-8-10-37(21-16-40-17-21)13-19-11-18(5-6-22(19)24)23-7-9-29-27(33-23)31-20-12-30-36(4)14-20/h5-7,9,11-12,14-15,21,24H,8,10,13,16-17H2,1-4H3,(H,32,39)(H,29,31,33)/t24-/m1/s1
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n/an/a 24n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of BTK phosphorylation in human whole blood assessed as reduction in BTK phosphorylation incubated for 30 mins

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00926
BindingDB Entry DOI: 10.7270/Q23B641C
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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/an/an/a


TBA

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

Citation and Details

BindingDB Entry DOI: 10.7270/Q2KD22RG
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))		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
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