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Found 31 Enz. Inhib. hit(s) with Target = 'Transient receptor potential cation channel subfamily V member 1' and Ligand = 'BDBM50133817'
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataKi:  2.5nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataKi:  4.30nMAssay 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataKi:  11nMAssay 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.150nMAssay Description:Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.180nMAssay Description:Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accum...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.400nMAssay Description:Antagonist activity against capsaicin-induced 45calcium ion uptake in CHO cells expressing rat TRPV1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity against acid-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 at pH5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.600nMAssay 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  1.80nMAssay Description:Antagonist activity at recombinant human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  1.90nMAssay 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  2.10nMAssay Description:Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  4.80nMAssay Description:Vanilloid receptor subtype 1 antagonist activity based on its ability to block low pH-induced activation of the rat VR1 channel in a HEK293 cell lineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  4.90nMAssay Description:Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  5nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in human 1321N1 cells assessed as inhibition of capsaicin-induced calcium influx by FLIPR as...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  6.70nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as decrease in intracellular calcium levelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  7nMAssay Description:Displacement of [3H]RTX from human TRPV1 expressed in HEK293 cell membranes after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  9.60nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced intracellular calcium level preincubated for 2.5 mins followed by caps...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  16nMAssay Description:Inhibition of human TRPV1 expressed in HEK293 cells assessed as reduction in capsaicin-induced activity pretreated for 2.5 mins followed by capsaicin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at capsaicin-stimulated human TRPV1 receptor in aequorin expressing cells preincubated for 2.5 mins followed by capsaicin additio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  24nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced channel activationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  30nMpH: 5.5Assay Description:Inhibition of human vanilloid receptor 1 in HEK293 cells in pH 5.5-induced FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  34nMAssay Description:Inhibition of human vanilloid receptor 1 in HEK293 cells in capsaicin-induced FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Amgen

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  35nMAssay Description:Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50133817(4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic ...)
Affinity DataIC50:  35nMAssay Description:Inhibition of TRPV1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed