BDBM426069 5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]pyrazin-3-yl]indolin-::US10513523, Example 63::US10513523, Example 8

SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2NC(=O)Cc2c1)N1CCOCC1

InChI Key InChIKey=XGMDENYCSCSWDX-UHFFFAOYSA-N

Data  5 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 5 hits for monomerid = 426069   

TargetGlutamate receptor 1(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50:  0.5nMAssay Description:This assay was used to test compounds for their ability to inhibit TARP γ8 dependent AMPA receptor activity. The AMPA receptor is a non-selectiv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor 1(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50:  0.200nMAssay Description:This assay was used to test compounds for their ability to inhibit TARP γ8 dependent AMPA receptor activity. The AMPA receptor is a non-selectiv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetVoltage-dependent calcium channel gamma-8 subunit(Rattus norvegicus)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50: <1.00E+4nMAssay Description:Negative allosteric modulation of TARPgamma8 in rat hippocampal neurons assessed as inhibition of glutamate-induced current at 10 uM at -60 mV holdin...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50:  500nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate measured after 15 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Homo sapiens (Human))
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50:  0.501nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed