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Found 20 hits Enz. Inhib. hit(s) with Target = 'Tyrosine-protein kinase SYK' and Ligand = 'BDBM212271'   
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))
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))
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



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/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/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/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/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))
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/an/an/a 26n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated BTK phosphorylation at Y223 residue


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))
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/an/an/a 34n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated AKT phosphorylation at S473 residue


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))
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/an/an/a 37n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated ERK phosphorylation at T202/Y204 residue


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))
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/an/an/a 51n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated MEK phosphorylation at S217/S221 residue


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))
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/an/an/a 112n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated B cells activation by measuring reduction in CD69 express...


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))
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/an/an/a 164n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated B cells activation by measuring reduction in CD86 express...


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))
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/an/an/a 24n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK in human Ramos cells assessed as reduction in antihuman IgM F(ab)2-induced phosphorylation of BLNK at Y96 residue preincubated for ...


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))
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/an/an/a 1.31E+3n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK-mediated alpha CD3/alpha CD28-stimulated human T lymphocytes proliferation measured after 90 hrs by EdU incorporation 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))
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/an/an/a 180n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated TNFalpha secretion


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))
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/an/an/a 90n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated IL-1 beta secretion


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))
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/an/an/a 700n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated IL-6 secretion


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))
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/an/an/a 73n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK in human whole blood assessed as reduction in anti-FCepsilonR1 mAb-induced basophil activation by measuring decrease in CD63 surfac...


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))
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/an/an/a 108n/an/an/an/a



Gilead Sciences

Curated by ChEMBL


Assay Description
Inhibition of SYK-mediated alpha IgM/alpha CD40-stimulated human B lymphocytes proliferation pretreated for 1 hr followed by stimulation with alpha I...


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)