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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 36 hits for monomerid = 50400047
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
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
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
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
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Portola Pharmaceuticals
US Patent
Portola Pharmaceuticals
US Patent
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
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
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
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
Portola Pharmaceuticals
US Patent
Portola Pharmaceuticals
US Patent
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
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
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
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
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
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 8.60E+3nMAssay Description:Inhibition of human ERG by Q-patch assayMore data for this Ligand-Target Pair
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
Affinity DataIC50: 238nMAssay Description:Inhibition of Lyn (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase ZAP-70(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 60nMAssay Description:Inhibition of ZAP70 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 1.75E+3nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
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
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
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 68nMAssay Description:Inhibition of human ZAP70More data for this Ligand-Target Pair
TargetTyrosine-protein kinase ZAP-70(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human ERG by manual patch clamp assayMore data for this Ligand-Target Pair
TargetProtein kinase C alpha type(Homo sapiens (Human))
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 90nMAssay Description:Inhibition of human PKCalphaMore 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
Novartis Institutes For Biomedical Research
Curated by ChEMBL
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
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
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
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
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
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
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
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of human ERG channelMore data for this Ligand-Target Pair
Affinity DataIC50: 223nMAssay Description:Inhibition of SYK in human Ramos cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 540nMAssay Description:Inhibition of SYK in human whole bloodMore data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
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
Portola Pharmaceuticals
US Patent
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