BDBM50332843 2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)phenyl)-7-(3-(trifluoromethyl)pyridin-2-yl)-6,7,8,9-tetrahydro-5H-pyrimido[5,4-d]azepin-4-amine::CHEMBL1630296::US9422293, 92B::US9738649, Example 92B

SMILES CN1CCN(CC1)c1nc2CCN(CCc2c(Nc2ccc(cc2)C(F)(F)F)n1)c1ncccc1C(F)(F)F

InChI Key InChIKey=FXFWLGLXQDHULE-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 50332843   

TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 160nMT: 2°CAssay Description:HEK293 cells were transfected with human TRPV1 cloned in pcDNA3.1zeo(+) using the Effectene non-liposomal lipid based transfection kit (Qiagen) (hTRP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 270nMT: 2°CAssay Description:The assay was performed as described below, using HEK293 cells transfected with rat TRPV1 (rTRPV1/HEK293). These cells had a geneticin selection mark...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 367nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ level by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 506nMAssay Description:Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ level by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 160nMAssay Description:HEK293 cells were transfected with human TRPV1 cloned in pcDNA3.1zeo(+) using the Effectene non-liposomal lipid based transfection kit (Qiagen) (hTRP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

LigandPNGBDBM50332843(2-(4-methylpiperazin-1-yl)-N-(4-(trifluoromethyl)p...)
Affinity DataIC50: 270nMAssay Description:The assay was performed as described above, using HEK293 cells transfected with rat TRPV1 (rTRPV1/HEK293). These cells had a geneticin selection mark...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent