BDBM292485 (S)-N-(2-(diethylamino)propyl)-2-(3-methoxyazetidin-1-yl)-6-(5-(thiophen-2-yl)pyrazolo[1,5-a]pyrimidin-3-yl)isonicotinamide::US10100058, Example 141

SMILES CCN(CC)[C@@H](C)CNC(=O)c1cc(nc(c1)-c1cnn2ccc(nc12)-c1cccs1)N1CC(C1)OC

InChI Key InChIKey=UCHOYOABTVPSLZ-UHFFFAOYSA-N

Data  8 IC50  3 EC50

  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 11 hits for monomerid = 292485   

LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 0.100nMAssay Description:The biochemical activity of recombinant CaMKIIδ was measured by monitoring the phosphorylation of a target peptide using Homogenous Time Resolve...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2019
Entry Details
Go to US Patent

LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataEC50:  13.7nMAssay Description:CaMKII activity in neonatal rat ventricular myocytes (NRVM) was measured by monitoring the phosphorylation level of phospholamban using high-content ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2019
Entry Details
Go to US Patent

TargetCytochrome P450 2C19(Human)TBA
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of recombinant human full length His-tagged CaMK2delta expressed in baculovirus using Biotin labelled STK1 as substrate after 1 hr in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataEC50:  120nMAssay Description:Inhibition of CaMK2alpha/beta in neonatal rat cortical neurons assessed as phospholamban phosphorylation after 4 hrs by Hoechst 33342 fluorescence-ba...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)TBA
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)TBA
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)TBA
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)TBA
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataEC50:  7.40nMAssay Description:Inhibition of CaMK2gamma/delta in neonatal rat ventricular myocytes assessed as phospholamban phosphorylation after 4 hrs by Hoechst 33342 fluorescen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM292485(US10100058, Example 141 | (S)-N-(2-(diethylamino)p...)
Affinity DataIC50: 4.16E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed