BDBM20334 1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea::1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]methyl}urea::A-425619::CHEMBL104028::JMC48744 Compound 14a

SMILES FC(F)(F)c1ccc(CNC(=O)Nc2cccc3cnccc23)cc1

InChI Key InChIKey=SJGVXVZUSQLLJB-UHFFFAOYSA-N

Data  3 KI  6 IC50  5 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 13 hits for monomerid = 20334   

LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataEC50:  2.10nMpH: 7.4 T: 2°CAssay Description:The functional antagonist activity of compounds at the TRPV1 receptor was determined with a Ca2+ influx assay by measuring the effect on capsaicin (0...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2008
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataEC50:  4nMpH: 7.4 T: 2°CAssay Description:The functional antagonist activity of compounds at the TRPV1 receptor was determined with a Ca2+ influx assay by measuring the effect on capsaicin (0...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2008
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataEC50:  4nMpH: 7.4 T: 2°CAssay Description:The functional antagonist activity of compounds at the TRPV1 receptor was determined with a Ca2+ influx assay by measuring the effect on capsaicin (0...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataEC50:  24nMpH: 7.4 T: 2°CAssay Description:The functional antagonist activity of compounds at the TRPV1 receptor was determined with a Ca2+ influx assay by measuring the effect on capsaicin (0...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 3nMAssay Description:Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 4nMAssay Description:Blockade of human TRPV1 receptor assessed as inhibition of capsaicin-induced calcium fluxMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 5nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 2nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 4nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of calcium influxMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2011
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataIC50: 9nMAssay Description:Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataKi:  5nMAssay Description:Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataKi:  18nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced effect by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/4/2016
Entry Details Article
PubMed
LigandPNGBDBM20334(1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]m...)
Affinity DataKi:  47nM ΔG°:  -9.99kcal/mole EC50:  11nMpH: 7.4 T: 2°CAssay Description:The hTRPV1-expressing CHO cell membranes were incubated with [3H]A-778317 and test compounds to establish equilibrium. After incubation was terminate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2008
Entry Details Article
PubMed