BDBM212271 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine:::US10828299, Example Ex.-2::US10342794, Example Ex.-2::US11517570, Example Ex.-2::US9290505, Ex.-2::US9504684, Ex.-2::US9931338, Ex.-2

SMILES Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1

InChI Key InChIKey=XCIGZBVOUQVIPI-UHFFFAOYSA-N

Data  9 IC50  13 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 22 hits for monomerid = 212271   

TargetCD63 antigen(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  80nMpH: 7.0Assay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMAssay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMpH: 7.0 T: 2°CAssay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMAssay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMAssay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  6.20nMAssay Description:Inhibition of SYK (unknown origin) using XL665-labeled peptide as substrate in presence of ATP measured after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  24nMAssay 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 ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  73nMAssay Description:Inhibition of SYK in human whole blood assessed as reduction in anti-FCepsilonR1 mAb-induced basophil activation by measuring decrease in CD63 surfac...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  120nMAssay Description:Inhibition of wild-type human partial length JAK2 JH1 catalytic domain (A829 to G1132 residues) expressed in mammalian expression system by Kinomesca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  26nMAssay Description:Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated BTK phosphorylation at Y223 residueMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  34nMAssay Description:Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated AKT phosphorylation at S473 residueMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  37nMAssay Description:Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated ERK phosphorylation at T202/Y204 residueMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  51nMAssay Description:Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated MEK phosphorylation at S217/S221 residueMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  112nMAssay 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...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  164nMAssay 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...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  108nMAssay Description:Inhibition of SYK-mediated alpha IgM/alpha CD40-stimulated human B lymphocytes proliferation pretreated for 1 hr followed by stimulation with alpha I...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  1.31E+3nMAssay Description:Inhibition of SYK-mediated alpha CD3/alpha CD28-stimulated human T lymphocytes proliferation measured after 90 hrs by EdU incorporation assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  180nMAssay Description:Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated TNFalpha secretionMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  90nMAssay Description:Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated IL-1 beta secretionMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataEC50:  700nMAssay Description:Inhibition of SYK (unknown origin) in macrophages assessed as reduction in immune complex-stimulated IL-6 secretionMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMAssay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase SYK(Homo sapiens (Human))
Kronos Bio

US Patent
LigandPNGBDBM212271(6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piper...)
Affinity DataIC50:  13.5nMpH: 7.0Assay Description:Syk activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, Syk-ca...More data for this Ligand-Target Pair