BDBM50400047 BIIB-057::CHEMBL2177736::US9579320, Example 87

SMILES N[C@H]1CCCC[C@H]1Nc1ncc(C(N)=O)c(Nc2cccc(c2)-n2nccn2)n1

InChI Key InChIKey=TXGKRVFSSHPBAJ-JKSUJKDBSA-N

Data  36 IC50

PDB links: 3 PDB IDs match this monomer.

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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 36 hits for monomerid = 50400047   

TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase Fgr(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  81nMAssay 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 DepthDetails US Patent
TargetTyrosine-protein kinase Yes(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  123nMAssay 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 DepthDetails US Patent
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  139nMAssay 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 DepthDetails US Patent
TargetSerine/threonine-protein kinase PAK 5(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  166nMAssay 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 DepthDetails US Patent
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  199nMAssay 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 DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  244nMAssay 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 DepthDetails US Patent
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  300nMAssay 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 DepthDetails US Patent
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  8.60E+3nMAssay Description:Inhibition of human ERG by Q-patch assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  238nMAssay Description:Inhibition of Lyn (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ZAP-70(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  60nMAssay Description:Inhibition of ZAP70 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  1.75E+3nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase ZAP-70(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  68nMAssay Description:Inhibition of human ZAP70More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ZAP-70(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  1.81E+3nMAssay Description:Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-C...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibition of human ERG by manual patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein kinase C alpha type(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  90nMAssay Description:Inhibition of human PKCalphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  8.60E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  9.10E+3nMAssay Description:Inhibition of human ERG channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  223nMAssay Description:Inhibition of SYK in human Ramos cellsMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  540nMAssay Description:Inhibition of SYK in human whole bloodMore data for this Ligand-Target Pair
TargetCytochrome P450 3A4(Homo sapiens (Human))
Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | 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
TargetMitogen-activated protein kinase kinase kinase 9(Homo sapiens (Human))
Portola Pharmaceuticals

US Patent
LigandPNGBDBM50400047(BIIB-057 | CHEMBL2177736 | US9579320, Example 87)
Affinity DataIC50:  60nMAssay 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 DepthDetails US Patent