Compile Data Set for Download or QSAR
Report error Found 17 Enz. Inhib. hit(s) for PDB: 4RX9
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 1nMAssay Description:Inhibition of human recombinant spleen tyrosine kinase (360 to 635 amino acid residues) after 10 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 1nMAssay Description:Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were dete...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/29/2015
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 1nMAssay Description:Inhibition of human recombinant truncated SYK (360 to 365 amino acid residues) using N-terminally biotinylated EPEGDYEEVLE peptide as substrate asses...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 5.5nMpH: 7.5 T: 2°CAssay Description:Potency of candidate molecules for inhibiting syk tyrosine phosphorylation activity is assessed by measuring the ability of a test compound to inhibi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2019
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 6nMAssay Description:SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/29/2015
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 10.5nMpH: 7.5 T: 2°CAssay Description:Briefly, 10 μL per well reactions contained ATP concentration at 25 μm for Syk,2 μm Tyr2 peptide substrate in 50 mm HEPES (PH 7.5), 0....More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 13nMAssay Description:Inhibition of Syk (unknown origin) using 4 uM peptide assessed as product formation after 60 mins incubation by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 13nMAssay Description:Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 13nMAssay Description:Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 178nMAssay Description:Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 178nMAssay Description:Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 178nMAssay Description:Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 223nMAssay Description:Inhibition of SYK in human Ramos cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 540nMAssay Description:Inhibition of SYK in human whole bloodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 952nMAssay Description:Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimul...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 952nMAssay Description:Inhibition of Syk in human whole blood assessed as inhibition of P-SLP76 in CD14+ monocytes by flow cytometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(CHEMBL2177736 | BIIB-057 | US9579320, Example 87)
Affinity DataIC50: 952nMAssay Description:Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes in presence of 90% human blood assessed as phospho-SLP76 level preincubated for 30 mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)