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Found 1149 with Last Name = 'costanzo' and Initial = 'mj'
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14073((2S)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimi...)
Affinity DataKi:  0.000650nM ΔG°:  -72.4kJ/mole IC50:  4.5nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14073((2S)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimi...)
Affinity DataKi:  0.000650nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14065((2S)-1-[(2R)-2-amino-3-phenylpropanoyl]-N-[1-(1,3-...)
Affinity DataKi:  0.00550nM ΔG°:  -66.9kJ/mole IC50:  21nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14127(2-(5-carbamimidamido-2-{[(2S)-1-[(2R)-2-(methylami...)
Affinity DataKi:  0.00700nM IC50:  5nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50328697((R)-5-guanidino-N-(2-((S)-5-guanidino-1-oxo-1-(thi...)
Affinity DataKi:  0.0140nMAssay Description:Inhibition of human factor 10aMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14076((2S)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimi...)
Affinity DataKi:  0.0180nM ΔG°:  -63.8kJ/mole IC50:  5.30nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50095523(CHEMBL285231 | [(S)-2-methyl-1-((S)-2-{(S)-2-methy...)
Affinity DataKi:  0.0250nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50374350(CHEMBL403098)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50076232((1S,7S)-7-Amino-7-benzyl-8-oxo-hexahydro-pyrazolo[...)
Affinity DataKi:  0.0710nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50161518(1-(oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one...)
Affinity DataKi:  0.0940nMAssay Description:Inhibition of human recombinant FAAHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50031203(2-{(S)-2-[((S)-1-{(S)-2-[4-(4-Chloro-benzenesulfon...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14066((2S)-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamid...)
Affinity DataKi:  0.120nM ΔG°:  -58.9kJ/mole IC50:  15nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14123((2S)-N-[5-carbamimidamido-1-(6-methoxy-1,3-benzoth...)
Affinity DataKi:  0.140nM IC50:  5nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(1A) dopamine receptor(RAT)
TBA

Curated by ChEMBL
LigandPNGBDBM82247(8-Chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-b...)
Affinity DataKi:  0.140nMAssay Description:Binding affinity towards Dopamine receptor D1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50374357(CHEMBL404043)
Affinity DataKi:  0.140nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14125((2S)-N-[5-carbamimidamido-1-(6-fluoro-1,3-benzothi...)
Affinity DataKi:  0.150nM IC50:  7.5nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50374356(CHEMBL404042)
Affinity DataKi:  0.150nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransporter(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50367554(CHEMBL1743782)
Affinity DataKi:  0.160nMAssay Description:Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14068((2S)-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamid...)
Affinity DataKi:  0.180nM ΔG°:  -57.9kJ/mole IC50:  48nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50228853((S)-1-((R)-2-Methylamino-3-phenyl-propionyl)-pyrro...)
Affinity DataKi:  0.190nMAssay Description:Inhibition of human alpha-thrombin.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14071((2S)-1-(2-amino-2-benzylpropanoyl)-N-[1-(1,3-benzo...)
Affinity DataKi:  0.200nM ΔG°:  -57.6kJ/mole IC50:  3.5nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14063((2S)-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamid...)
Affinity DataKi:  0.200nM ΔG°:  -57.6kJ/mole IC50:  29nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50031198(1-(4-(((S)-1-((S)-2-(((S)-1-(benzo[d]oxazol-2-yl)-...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1 [30-579](Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50161518(1-(oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of rat FAAHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50374347(CHEMBL270680)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50374345(CHEMBL256253)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50228853((S)-1-((R)-2-Methylamino-3-phenyl-propionyl)-pyrro...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1 [30-579](Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50228837(2-(3-(biphenyl-4-yl)propanoyl)oxazole-5-carbonitri...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of rat FAAHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransporter(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50367584(CHEMBL1743810)
Affinity DataKi:  0.200nMAssay Description:Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14124((2S)-N-[5-carbamimidamido-1-(6-hydroxy-1,3-benzoth...)
Affinity DataKi:  0.230nM IC50:  3nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50228837(2-(3-(biphenyl-4-yl)propanoyl)oxazole-5-carbonitri...)
Affinity DataKi:  0.260nMAssay Description:Inhibition of human recombinant FAAHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1 [30-579](Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50161512(7-Phenyl-1-(5-(pyridin-2-yl)-1,3,4-oxadiazol-2-yl)...)
Affinity DataKi:  0.290nMAssay Description:Inhibition of rat FAAHMore data for this Ligand-Target Pair
TargetSerine protease 1(Bos taurus (bovine))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14127(2-(5-carbamimidamido-2-{[(2S)-1-[(2R)-2-(methylami...)
Affinity DataKi:  0.300nMAssay Description:Trypsin-catalyzed hydrolysis rates were measured spectrophotometrically using bovine trypsin, a chromogenic substrate in aqueous buffer, and a microp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine protease 1(Bos taurus (bovine))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14065((2S)-1-[(2R)-2-amino-3-phenylpropanoyl]-N-[1-(1,3-...)
Affinity DataKi:  0.300nMAssay Description:Trypsin-catalyzed hydrolysis rates were measured spectrophotometrically using bovine trypsin, a chromogenic substrate in aqueous buffer, and a microp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50031209((S)-1-{(S)-2-[4-(4-Chloro-benzenesulfonylaminocarb...)
Affinity DataKi:  0.330nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14086((2S)-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamid...)
Affinity DataKi:  0.340nM IC50:  38nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50031217(CHEMBL262516 | N-((S)-1-{(S)-2-[(S)-1-(Benzooxazol...)
Affinity DataKi:  0.340nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50374351(CHEMBL404910)
Affinity DataKi:  0.350nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14072(2-ketobenzothiazole 12 | 2-{[(2R)-1-[(2S)-2-{[1-(1...)
Affinity DataKi:  0.360nM ΔG°:  -56.1kJ/mole IC50:  29nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14126((2S)-N-{5-carbamimidamido-1-[6-(hydroxymethyl)-1,3...)
Affinity DataKi:  0.370nM IC50:  7nMAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransporter(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50021874(6-Phenyl-1,2,3,5,6,10b-hexahydro-pyrrolo[2,1-a]iso...)
Affinity DataKi:  0.370nMAssay Description:Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransporter(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50021874(6-Phenyl-1,2,3,5,6,10b-hexahydro-pyrrolo[2,1-a]iso...)
Affinity DataKi:  0.370nMAssay Description:Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium-dependent dopamine transporter(MOUSE)
Mcneil Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50014237(6-(4-Methylsulfanyl-phenyl)-1,2,3,5,6,10b-hexahydr...)
Affinity DataKi:  0.390nMAssay Description:Tested in vitro for serotonin(5-HT) neuronal uptake inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFatty-acid amide hydrolase 1 [30-579](Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50204512(2-(7-phenylheptanoyl)oxazole-5-carbonitrile | CHEM...)
Affinity DataKi:  0.400nMAssay Description:Inhibition of rat FAAHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM50118731((2-{2-[5-Amino-1-(oxazole-2-carbonyl)-pentylcarbam...)
Affinity DataKi:  0.420nMAssay Description:Inhibition of human alpha-thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium-dependent dopamine transporter(MOUSE)
Mcneil Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM22416((3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-f...)
Affinity DataKi:  0.440nMAssay Description:Tested in vitro for dopamine(DA) neuronal uptake inhibitionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTransporter(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50367582(CHEMBL1743790)
Affinity DataKi:  0.450nMAssay Description:Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM14075((2S)-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamid...)
Affinity DataKi:  0.460nM ΔG°:  -55.4kJ/mole IC50:  34nMpH: 7.4 T: 2°CAssay Description:Thrombin-catalyzed hydrolysis rates were measured spectrophotometrically using human alpha-thrombin, a chromogenic substrate in aqueous buffer, and a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50095526(CHEMBL24058 | [(S)-2-methyl-1-((S)-2-{(S)-2-methyl...)
Affinity DataKi:  0.490nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50095530((S)-2-(5-amino-2-(4-fluorophenyl)-6-oxopyrimidin-1...)
Affinity DataKi:  0.520nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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