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Found 1346 with Last Name = 'gomtsyan' and Initial = 'a'
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20458(1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-...)
Affinity DataKi:  7nM ΔG°:  -46.5kJ/mole EC50:  5nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20464((2E)-3-[2-(piperidin-1-yl)-6-(trifluoromethyl)pyri...)
Affinity DataKi:  27nM ΔG°:  -43.2kJ/mole EC50:  34nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20334(1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-ur...)
Affinity DataKi:  47nM ΔG°:  -41.8kJ/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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20465(1-[(1R,2S)-6-fluoro-1-{[3-(trifluoromethyl)phenyl]...)
Affinity DataKi:  58nM ΔG°:  -41.3kJ/mole EC50:  46nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20285(Resiniferatoxin | [(1R,2R,6R,10S,11R,15R,17R)-13-b...)
Affinity DataKi:  65nM ΔG°:  -41.0kJ/mole EC50:  24nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20466(A-784168 | CHEMBL482834 | N-[4-(trifluoromethane)s...)
Affinity DataKi:  71nM ΔG°:  -40.8kJ/mole EC50:  74nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20467(3-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-1-...)
Affinity DataKi:  112nM ΔG°:  -39.7kJ/mole EC50:  34nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20459(Tinyatoxin | [(1R,2R,6R,10S,11R,15R,17R)-13-benzyl...)
Affinity DataKi:  589nM ΔG°:  -35.6kJ/mole EC50:  129nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20468(3-(2-bromophenyl)-1-{2-[ethyl(3-methylphenyl)amino...)
Affinity DataKi:  603nM ΔG°:  -35.5kJ/mole EC50:  95nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20284(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Affinity DataKi:  1.29E+3nM ΔG°:  -33.6kJ/mole EC50:  282nMpH: 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
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20460((9Z)-N-[(4-hydroxy-3-methoxyphenyl)methyl]octadec-...)
Affinity DataKi:  1.59E+3nM ΔG°:  -33.1kJ/mole EC50:  132nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20462((5Z,8Z,11Z,14Z)-N-[2-(3,4-dihydroxyphenyl)ethyl]ic...)
Affinity DataKi: >6.31E+3nM ΔG°: >-29.7kJ/mole EC50:  1.48E+3nMpH: 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 DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM20461((6E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methy...)
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
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201834(5-benzo[b]thiophen-2-yl-6-(6-morpholin-4-ylpyridin...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50232114((R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(...)
Affinity DataIC50:  0.700nMpH: 5.5Assay Description:Blockade of pH 5.5-induced activation of TRPV1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM14486((2R,3R,4S,5R)-2-(2-amino-9-iodo-3,5,7-triazabicycl...)
Affinity DataIC50:  0.900nMpH: 7.5 T: 2°CAssay Description:ADK activity was monitored by a radiochemical assay, which measures the conversion of radioactive Ado ([U-14C] adenosine or [2-3H] adenosine) to AMP ...More data for this Ligand-Target Pair
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201814(5-benzofuran-2-yl-6-(6-morpholin-4-ylpyridin-3-yle...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM143965(US8969325, 166)
Affinity DataIC50:  1nMAssay Description:The cDNA for human TRPV1 (hTRPV1) was isolated by reverse transcriptase-polymerase chain reaction (RT-PCR) from human small intestine poly A+ RNA sup...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201825(5-(4-chlorophenyl)-6-{6-[(2-methoxyethyl)methylami...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201865(1-(4-{5-[6-amino-5-(4-chlorophenyl)pyrimidin-4-yle...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50321857(8-{4-(4-Fluorophenyl)-5-[4-(trifluoromethyl)phenyl...)
Affinity DataIC50:  1.30nMAssay Description:Antagonist activity at human recombinant TRPV1 receptor expressed in human 1321 cells assessed as inhibition of capsaicin-induced in intracellular ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50102928(5-(3-Bromo-phenyl)-7-(6-thiomorpholin-4-yl-pyridin...)
Affinity DataIC50:  1.30nMAssay Description:In vitro concentration required for 50% inhibition against Adenosine Kinase (AK) in the presence of intact cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50102925(5-(3-Bromo-phenyl)-7-[6-(1,4-dioxa-8-aza-spiro[4.5...)
Affinity DataIC50:  1.40nMAssay Description:In vitro concentration required for 50% inhibition against Adenosine Kinase (AK) in the presence of enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50094703(5-(3-Bromo-phenyl)-7-(6-morpholin-4-yl-pyridin-3-y...)
Affinity DataIC50:  1.70nMAssay Description:Tested for inhibitory activity against AK in an in vitro cell-free enzyme assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50102927(5'-[4-Amino-5-(3-bromo-phenyl)-pyrido[2,3-d]pyrimi...)
Affinity DataIC50:  1.80nMAssay Description:In vitro concentration required for 50% inhibition against Adenosine Kinase (AK) in the presence of enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM50117165(5-[(Benzyl-methyl-amino)-methyl]-6-(6-morpholin-4-...)
Affinity DataIC50:  2nMAssay Description:Evaluated in vitro for inhibitory activity against Adenosine kinase (AK)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50321856(4-{2-[7-Hydroxy-5,6,7,8-tetrahydronaphthalen-1-yla...)
Affinity DataIC50:  2nMAssay Description:Antagonist activity at human recombinant TRPV1 receptor expressed in human 1321 cells assessed as inhibition of capsaicin-induced in intracellular ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM14488(5-[4-(dimethylamino)phenyl]-6-{2-[6-(morpholin-4-y...)
Affinity DataIC50:  2nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50056351(CHEMBL3326569)
Affinity DataIC50:  2nMAssay Description:Antagonist activity against human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM50117169(5-[3-(4-Bromo-phenyl)-propyl]-6-(6-morpholin-4-yl-...)
Affinity DataIC50:  2nMAssay Description:Evaluated in vitro for inhibitory activity against Adenosine kinase (AK)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM128907(US8802711, 76)
Affinity DataIC50:  2nMAssay Description:The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescenc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50321853(8-{4-Ethyl-5-[4-(trifluoromethyl)phenyl]oxazol-2-y...)
Affinity DataIC50:  2.10nMAssay Description:Antagonist activity at human recombinant TRPV1 receptor expressed in human 1321 cells assessed as inhibition of capsaicin-induced in intracellular ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM128912(US8802711, 81)
Affinity DataIC50:  2.30nMAssay Description:The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescenc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM50117175(5-[3-(2-Chloro-phenyl)-propyl]-6-(6-morpholin-4-yl...)
Affinity DataIC50:  2.5nMAssay Description:Evaluated in vitro for inhibitory activity against Adenosine kinase (AK)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM14494(6-{2-[6-(morpholin-4-yl)pyridin-3-yl]ethynyl}-5-(3...)
Affinity DataIC50:  2.5nMAssay Description:Evaluated in vitro for inhibitory activity against Adenosine kinase (AK)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM14494(6-{2-[6-(morpholin-4-yl)pyridin-3-yl]ethynyl}-5-(3...)
Affinity DataIC50:  2.5nMpH: 7.5 T: 2°CAssay Description:ADK activity was monitored by a radiochemical assay, which measures the conversion of radioactive Ado ([U-14C] adenosine or [2-3H] adenosine) to AMP ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201823(5-(4-chlorophenyl)-6-(6-morpholin-4-ylpyridin-3-yl...)
Affinity DataIC50:  3nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201821(5-(4-bromophenyl)-6-(4-dimethylaminophenylethynyl)...)
Affinity DataIC50:  3nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50232114((R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(...)
Affinity DataIC50:  3nMAssay Description:Blockade of N-arachidonoyl-dopamine-induced activation of TRPV1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50201849(5-(4-chlorophenyl)-6-(4-dimethylaminophenylethynyl...)
Affinity DataIC50:  3nMAssay Description:Inhibition of cytosolic adenosine kinaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50232113(1-(1H-indazol-4-yl)-3-(5-(trifluoromethyl)-2,3-dih...)
Affinity DataIC50:  3nMAssay Description:Blockade of human TRPV1 receptor assessed as inhibition of capsaicin-induced calcium fluxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50232113(1-(1H-indazol-4-yl)-3-(5-(trifluoromethyl)-2,3-dih...)
Affinity DataIC50:  3nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50056358(CHEMBL3326581)
Affinity DataIC50:  3nMAssay Description:Antagonist activity against human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50338002((R)-1-(8-tert-butylchroman-4-yl)-3-(1H-indazol-4-y...)
Affinity DataIC50:  3nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM143964(US8969325, 165)
Affinity DataIC50:  3nMAssay Description:The cDNA for human TRPV1 (hTRPV1) was isolated by reverse transcriptase-polymerase chain reaction (RT-PCR) from human small intestine poly A+ RNA sup...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM50321850(8-{5-[3-Methyl-4-(trifluoromethyl)phenyl]oxazol-2-...)
Affinity DataIC50:  3.20nMAssay Description:Antagonist activity at human recombinant TRPV1 receptor expressed in human 1321 cells assessed as inhibition of capsaicin-induced in intracellular ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM128913(US8802711, 82)
Affinity DataIC50:  3.30nMAssay Description:The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescenc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetAdenosine kinase(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50102924(5-(3-Bromo-phenyl)-7-(6-pyrrolidin-1-yl-pyridin-3-...)
Affinity DataIC50:  3.40nMAssay Description:In vitro concentration required for 50% inhibition against Adenosine Kinase (AK) in the presence of intact cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAdenosine kinase(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM50117154(5-[3-(4-Methoxy-phenyl)-propyl]-6-(6-morpholin-4-y...)
Affinity DataIC50:  3.5nMAssay Description:Evaluated in vitro for inhibitory activity against Adenosine kinase (AK)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM128905(US8802711, 74)
Affinity DataIC50:  3.5nMAssay Description:The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescenc...More data for this Ligand-Target Pair
In DepthDetails US Patent
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