Compile Data Set for Download or QSAR
Report error Found 43 Enz. Inhib. hit(s) for PDB: 7LR0
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  45nMAssay Description:Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of calcium uptake by 45Ca2+ uptake assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rat)
Sandoz Institute For Medical Research

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  300nMAssay Description:In vitro effective concentration for [Ca2+] uptake into dorsal root ganglia neurones in cultureMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rat)
Sandoz Institute For Medical Research

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  300nMAssay Description:In vitro effective concentration for [Ca2+] uptake into dorsal root ganglia neurones in cultureMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rat)
Sandoz Institute For Medical Research

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  300nMAssay Description:Effective concentration for [Ca2+] uptake into dorsal root ganglia neurones in rat cultured spinal sensory neuronesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rat)
Sandoz Institute For Medical Research

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  30nMAssay Description:In vitro agonist activity, increased [Ca2+] influx, at vanilloid receptor of rat dorsal root gangliaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2018
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  5.30nMAssay Description:Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  2.51nMAssay Description:Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as increase in intracellular calcium levels by fluorimetri...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  44.8nMAssay Description:Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptakeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at human recombinant TRPV1 expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  3.90nMAssay Description:Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  5nMAssay Description:Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  29nMAssay Description:Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium accumulation measured at 180 sec by fluoresce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  44.8nMAssay Description:In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  3.02E+4nMAssay Description:Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as effect on intracellular calcium level by FLOU-4 dye based fluoresce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  5.30nMAssay Description:Agonist activity at human TRPV1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  7.20nMAssay Description:Agonist activity at human TRPV1 expressed in HEK293T cells assessed as increase in Ca2+ transport incubated for 5 mins by calcium-5 fluorescence dye-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  20nMAssay Description:The effect of the substances on Ca2+ influx was determined by using HEK-293 cells stably overexpressing recombinant human TRPV1 cDNA. The cells were ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  871nMAssay Description:Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  45nMAssay Description:Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting meth...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  870nMAssay Description:Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  26nMAssay Description:Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting me...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  1.00E+3nMAssay Description:Agonist activity at TRPV1 (unknown origin) expressed in human SH-SY5Y cells assessed as increase in calcium influx after 25 mins by Fluo-4 NW dye-bas...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rat)
Sandoz Institute For Medical Research

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  300nMAssay Description:Compound tested in vitro for [Ca2+] influx into neonatal rat dorsal root ganglia (DRG)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  20nMAssay Description:Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataEC50:  2.32E+3nMAssay Description:Agonist activity at rat TRPV1 expressed in human SH-SY5Y cells assessed as intracellular calcium accumulation by Fluo-4 NW dye based fluorescence ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 8nMAssay Description:Antagonist activity at human TRPV1 stably transfected in HEK293 cells assessed as decrease in calcium influx preincubated for 5 mins followed by caps...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 8nMAssay Description:Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx pre-treated 5 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 8nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as desensitization by measuring inhibition of capsaicin-induced int...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 19nMAssay Description:Binding affinity to rat TRPV1More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 313nMAssay Description:Activation of human TRPV1 expressed in HEK293F cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataIC50: 420nMAssay Description:Inhibition of TRPV1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  6nMAssay Description:Binding affinity to human recombinant TRPV1More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.07E+3nMAssay Description:Displacement of [3H]-RTX from human TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.14E+3nMAssay Description:Displacement of [3H]RTX from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/10/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.70E+3nMAssay Description:In vitro binding to Rat Vanilloid receptor 1 (VR1) expressing CHO cells compared to capsaicinMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.80E+3nMAssay Description:In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]RTX displacement.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.81E+3nMAssay Description:Displacement of [3H]RTX form rat TRPV1 receptor expressed in CHO/VR1 cell systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  1.81E+3nMAssay Description:Displacement of [3H]-RTX from rat TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting me...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  2.00E+3nMAssay Description:Binding affinity against Vanilloid receptor in dorsal Root Ganglion (DRG) membranes using [3H]RTX binding assay.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Rat)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  2.00E+3nMAssay Description:Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  2.53E+3nMAssay Description:Displacement of [3H]MPOU from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/10/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM20461(Zostrix | (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl...)
Affinity DataKi:  2.00E+4nM ΔG°:  -26.8kJ/mole EC50:  29nMpH: 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
PubMedPDB3D3D Structure (crystal)