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Found 2032 with Last Name = 'williams' and Initial = 'r'
TargetMuscarinic acetylcholine receptor M4(RAT)
Dvanderbilt Program In Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50403547(ATROPEN | ATROPINE)
Affinity DataKi:  0.520nMAssay Description:Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M4(RAT)
Dvanderbilt Program In Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50403547(ATROPEN | ATROPINE)
Affinity DataKi:  0.520nMAssay Description:Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M4(RAT)
Dvanderbilt Program In Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50403547(ATROPEN | ATROPINE)
Affinity DataKi:  0.560nMAssay Description:Displacement of [3H]NMS from rat muscarinic M4 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M5(RAT)
Dvanderbilt Program In Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50403547(ATROPEN | ATROPINE)
Affinity DataKi:  0.860nMAssay Description:Displacement of [3H]NMS from rat recombinant muscarinic M5 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M5(RAT)
Dvanderbilt Program In Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50403547(ATROPEN | ATROPINE)
Affinity DataKi:  1.80nMAssay Description:Displacement of [3H]NMS from rat muscarinic M5 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11123((2S)-1-[(2S)-2-amino-3-[4-(2,4-difluorophenyl)phen...)
Affinity DataKi:  2.20nM ΔG°:  -49.4kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11121((2S)-1-[(2S)-2-amino-3-[4-(4-fluorophenyl)phenyl]p...)
Affinity DataKi:  3.10nM ΔG°:  -48.6kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14768((R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrol...)
Affinity DataKi:  4nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11122((2S)-1-[(2S)-2-amino-3-[4-(2-fluorophenyl)phenyl]p...)
Affinity DataKi:  5.30nM ΔG°:  -47.2kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50240973(CHEMBL4102855)
Affinity DataKi:  8.10nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50240989(CHEMBL4081904)
Affinity DataKi:  9.70nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14760((R)-6,7-Dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrol...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
LigandPNGBDBM14764((R)-6,7-Dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolid...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14766((R)-6,7-Dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolid...)
Affinity DataKi:  12nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(RAT)
Vanderbilt Institute Of Chemical Biology

Curated by ChEMBL
LigandPNGBDBM50231845(CHEMBL255523 | N-(3-chloro-4-(4-ethylpiperazin-1-y...)
Affinity DataKi:  12.7nMAssay Description:Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11118((2S)-1-[(2S)-2-amino-3-(4-phenylphenyl)propanoyl]p...)
Affinity DataKi:  13nM ΔG°:  -45.0kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50240991(CHEMBL4092165)
Affinity DataKi:  13nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14152(6-CHLORO-2-(2-HYDROXY-BIPHENYL-3-YL)-1H-INDOLE-5-C...)
Affinity DataKi:  14nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14150(APC-11417 | CA-12 | CRA-11417 | {amino[6-fluoro-2-...)
Affinity DataKi:  16nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14481(CA-23 | [amino({5-[(3,4-dihydroxynaphthalene-2-)am...)
Affinity DataKi:  17nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14754(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)
Affinity DataKi:  17nM ΔG°:  -43.9kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
LigandPNGBDBM50240975(CHEMBL4084907)
Affinity DataKi:  17nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14763((R)-6,7-Dimethoxy-4-[3-(7-methoxy-naphthalen-2-ylo...)
Affinity DataKi:  17nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14765((R)-6,7-Dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)...)
Affinity DataKi:  18nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14762((R)-6,7-Dimethoxy-4-[3-(6-methoxy-naphthalen-2-ylo...)
Affinity DataKi:  18nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14767((R)-4-[3-(Isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,...)
Affinity DataKi:  19nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11119((2S)-1-[(2S)-2-amino-3-[4-(4-methylphenyl)phenyl]p...)
Affinity DataKi:  20nM ΔG°:  -43.9kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14755(6,7-dimethoxy-4-[8-(4-methylpiperazin-1-yl)sulfony...)
Affinity DataKi:  25nM ΔG°:  -43.0kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11120((2S)-1-[(2S)-2-amino-3-[4-(3,4-dimethoxyphenyl)phe...)
Affinity DataKi:  26nM ΔG°:  -43.3kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11113(6-{[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl...)
Affinity DataKi:  27nM ΔG°:  -43.2kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14350(2-{5-[amino(iminiumyl)methyl]-6-fluoro-1H-1,3-benz...)
Affinity DataKi:  30nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14142(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phe...)
Affinity DataKi:  33nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11116((2S)-1-[(2S)-2-amino-3-(4-iodophenyl)propanoyl]pyr...)
Affinity DataKi:  34nM ΔG°:  -42.6kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11124((2S)-1-[(2S)-2-amino-3-[4-(furan-2-yl)phenyl]propa...)
Affinity DataKi:  36nM ΔG°:  -42.5kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14481(CA-23 | [amino({5-[(3,4-dihydroxynaphthalene-2-)am...)
Affinity DataKi:  41nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14756((R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1...)
Affinity DataKi:  44nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50240992(CHEMBL4097282)
Affinity DataKi:  46nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14761((R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrol...)
Affinity DataKi:  48nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14748((R)-4-[3-(4-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  54nM ΔG°:  -41.1kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14745((R)-4-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidi...)
Affinity DataKi:  56nM ΔG°:  -41.0kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3B(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14761((R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrol...)
Affinity DataKi:  56nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14751((R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Affinity DataKi:  61nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50240977(CHEMBL4071150)
Affinity DataKi:  61nMAssay Description:Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
University Of Basel

Curated by ChEMBL
LigandPNGBDBM50240975(CHEMBL4084907)
Affinity DataKi:  62nMAssay Description:Inhibition of human C-terminal GST-tagged mTOR (1360 to 2549 residues) expressed in baculovirus expression system using after 1 hr AlexaFluor647-labe...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM11115((2S)-1-[(2S)-2-amino-3-phenylpropanoyl]pyrrolidine...)
Affinity DataKi:  63nM ΔG°:  -41.1kJ/molepH: 7.4 T: 2°CAssay Description:The progress of DPPIV inhibition by compounds was measured by recording the liberation of free pNA at 405 nm. IC50 was determined from the slope of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14753((R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-...)
Affinity DataKi:  67nM ΔG°:  -40.5kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14752((R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dime...)
Affinity DataKi:  68nM ΔG°:  -40.5kJ/molepH: 7.5 T: 2°CAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M3(RAT)
Vanderbilt Institute Of Chemical Biology

Curated by ChEMBL
LigandPNGBDBM50231845(CHEMBL255523 | N-(3-chloro-4-(4-ethylpiperazin-1-y...)
Affinity DataKi:  74.8nMAssay Description:Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Pfizer

LigandPNGBDBM14757((R)-6,7-Dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidi...)
Affinity DataKi:  77nMAssay Description:PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine protease hepsin(Homo sapiens (Human))
Celera

LigandPNGBDBM14142(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phe...)
Affinity DataKi:  85nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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