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Found 771 with Last Name = 'doherty' and Initial = 'em'
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036257(((S)-1-{(1S,2R)-3-[Benzenesulfonyl-(3-methyl-butyl...)
Affinity DataKi:  0.5nMAssay Description:Binding affinity of the compound for HIV-1 protease was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036261((S)-N*1*-{(1S,2R)-3-[Benzenesulfonyl-(3-methyl-but...)
Affinity DataKi:  1nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined in vitroMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036251(CHEMBL141265 | [(1S,2R)-3-(Benzenesulfonyl-isobuty...)
Affinity DataKi:  3.20nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined in vitroMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036252(CHEMBL347671 | {(1S,2R)-1-Benzyl-3-[(4-chloro-benz...)
Affinity DataKi:  4.10nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036262(CHEMBL348282 | [(1S,2R)-3-(Benzenesulfonyl-cyclohe...)
Affinity DataKi:  6.70nMAssay Description:Binding affinity of the compound for HIV-1 protease was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036253(CHEMBL347431 | {(1S,2R)-3-[Benzenesulfonyl-(3-meth...)
Affinity DataKi:  10nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined in vitro.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036259((S)-N*1*-{(1S,2R)-1-Benzyl-2-hydroxy-3-[methanesul...)
Affinity DataKi:  13nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined in vitroMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036258(((S)-1-{(1S,2R)-1-Benzyl-2-hydroxy-3-[methanesulfo...)
Affinity DataKi:  57nMAssay Description:Binding affinity of the compound for HIV-1 protease was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036260(CHEMBL156424 | {(1S,2R)-1-Benzyl-3-[(3-chloro-benz...)
Affinity DataKi:  61nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036255(CHEMBL154197 | [(1S,2R)-3-(Benzenesulfonyl-benzyl-...)
Affinity DataKi:  125nMAssay Description:Binding affinity of the compound for HIV-1 protease was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036254(CHEMBL155051 | {(1S,2R)-1-Benzyl-2-hydroxy-3-[(3-m...)
Affinity DataKi:  128nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036264(CHEMBL154600 | {(1S,2R)-1-Benzyl-3-[(2-chloro-benz...)
Affinity DataKi:  227nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036263(CHEMBL154638 | {(1S,2S)-3-[Benzenesulfonyl-(3-meth...)
Affinity DataKi:  295nMAssay Description:Binding affinity of the compound for HIV-1 protease was determined.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Searle Discovery Research

Curated by ChEMBL
LigandPNGBDBM50036256(CHEMBL154798 | {(1S,2R)-1-Benzyl-2-hydroxy-3-[meth...)
Affinity DataKi:  1.87E+3nMAssay Description:Binding affinity of the compound for HIV-1 protease was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Amgen

LigandPNGBDBM35317(4-Methyl-3-(2-(methylamino)quinazolin-6-yl)-N-(3-(...)
Affinity DataIC50:  0.270nMAssay Description:The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...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
LigandPNGBDBM50261646((R)-3-Amino-5-(2-(1-methoxypropan-2-ylamino)-6-(4-...)
Affinity DataIC50:  0.300nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261646((R)-3-Amino-5-(2-(1-methoxypropan-2-ylamino)-6-(4-...)
Affinity DataIC50:  0.300nMpH: 5.0Assay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20531(N-{6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}qui...)
Affinity DataIC50:  0.300nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20464((2E)-3-[2-(piperidin-1-yl)-6-(trifluoromethyl)pyri...)
Affinity DataIC50:  0.420nMAssay Description:Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf [V600E](Homo sapiens (Human))
Amgen

LigandPNGBDBM14971(4-Methyl-3-(3-(pyrimidin-4-yl)pyridin-2-ylamino)-N...)
Affinity DataIC50:  0.460nM EC50:  15nMpH: 7.0 T: 2°CAssay Description:The in vitro kinase activities of wild type or mutants were determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer s ...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
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.5nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.5nMpH: 5.0Assay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influxMore 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
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.5nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.570nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.570nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50372585(CHEMBL404165)
Affinity DataIC50:  0.580nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of low pH-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20531(N-{6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}qui...)
Affinity DataIC50:  0.600nMpH: 7.4 T: 2°CAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM50261150(3-Amino-5-(2-(2-methoxyethylamino)-6-(4-(trifluoro...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.620nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50372585(CHEMBL404165)
Affinity DataIC50:  0.620nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore 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
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.640nMpH: 7.4 T: 2°CAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.640nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50372585(CHEMBL404165)
Affinity DataIC50:  0.650nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50372586(CHEMBL255420)
Affinity DataIC50:  0.650nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore 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
LigandPNGBDBM50261266(CHEMBL466743 | N-(2-(6-(3-Amino-2-oxo-1,2-dihydroq...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261266(CHEMBL466743 | N-(2-(6-(3-Amino-2-oxo-1,2-dihydroq...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261295(3-Amino-5-(6-(2-(2-methoxyethylamino)-6-(trifluoro...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261295(3-Amino-5-(6-(2-(2-methoxyethylamino)-6-(trifluoro...)
Affinity DataIC50:  0.700nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.760nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.760nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM50261149((S)-3-Amino-5-(2-(1-methoxypropan-2-ylamino)-6-(4-...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.800nMpH: 7.4 T: 2°CAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM50261150(3-Amino-5-(2-(2-methoxyethylamino)-6-(4-(trifluoro...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261296(3-Amino-5-(6-(2-((R)-tetrahydrofuran-3-ylamino)-6-...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore 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
LigandPNGBDBM50261294(3-Amino-5-(6-(2-amino-6-(trifluoromethyl)pyridin-3...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influxMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM20554(3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin...)
Affinity DataIC50:  0.900nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.900nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...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
LigandPNGBDBM20557(AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N...)
Affinity DataIC50:  0.900nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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