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Found 236 with Last Name = 'ermolieff' and Initial = 'j'
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361649(CHEMBL1938415)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361648(CHEMBL1940246)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361642(CHEMBL1940251)
Affinity DataKi:  0.700nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361641(CHEMBL1940247)
Affinity DataKi:  0.900nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29864(N-(Pyridin-2-yl) arylsulfonamide, 26)
Affinity DataKi: <1nM ΔG°: <-50.9kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317221((2R)-N-(adamantan-2-yl)-1-[(3-cyanophenyl)methyl]p...)
Affinity DataKi:  1nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317213((2R)-N-(adamantan-2-yl)-1-(cyclopentylmethyl)pyrro...)
Affinity DataKi:  1nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317211((2R)-N-(adamantan-2-yl)-1-propylpyrrolidine-2-carb...)
Affinity DataKi:  1nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317217((2R)-N-(adamantan-2-yl)-1-(2,2,2-trifluoroethyl)py...)
Affinity DataKi:  1nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317224((2R)-N-(adamantan-2-yl)-1-(oxan-4-ylmethyl)pyrroli...)
Affinity DataKi:  1nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317223((2R)-N-(adamantan-2-yl)-1-(pyridin-2-yl)pyrrolidin...)
Affinity DataKi:  1nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361652(CHEMBL1940250)
Affinity DataKi:  1nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317218((2R)-N-(adamantan-2-yl)-1-(3,3,3-trifluoropropyl)p...)
Affinity DataKi:  1nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361650(CHEMBL1940248)
Affinity DataKi:  1.30nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317211((2R)-N-(adamantan-2-yl)-1-propylpyrrolidine-2-carb...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317209((2R)-N-(adamantan-2-yl)-1-ethylpyrrolidine-2-carbo...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361644(CHEMBL1940253)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361643(CHEMBL1940252)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
University of Illinois At Chicago

LigandPNGBDBM16047((4S)-4-[(2S)-2-[(2R,4S,5S)-5-[(2S)-2-[(2S)-2-[(4S)...)
Affinity DataKi:  1.60nM ΔG°:  -52.2kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317212((2R)-N-(adamantan-2-yl)-1-(propan-2-yl)pyrrolidine...)
Affinity DataKi:  1.60nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29863(N-(Pyridin-2-yl) arylsulfonamide, 25)
Affinity DataKi:  1.70nM ΔG°:  -49.6kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92906(CHK1 compound 1)
Affinity DataKi:  1.75nM ΔG°:  -49.5kJ/molepH: 7.4 T: 2°CAssay Description:The inhibitors reported in this study bind to CHK1 according to a general mechanism illustrated in Scheme 1 where E, S, and I stand for enzyme, subst...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29862(N-(Pyridin-2-yl) arylsulfonamide, 24)
Affinity DataKi:  1.90nM ΔG°:  -49.3kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361653(CHEMBL1940245)
Affinity DataKi:  2nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317219((2R)-N-(adamantan-2-yl)-1-[(4-chlorophenyl)methyl]...)
Affinity DataKi:  2nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317210((2R)-N-(adamantan-2-yl)-1-methylpyrrolidine-2-carb...)
Affinity DataKi:  2.40nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317216((2R)-N-(adamantan-2-yl)-1-(cyclohexylmethyl)pyrrol...)
Affinity DataKi:  2.40nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
University of Illinois At Chicago

LigandPNGBDBM16250(CHEMBL290001 | N-(tert-butoxycarbonyl)-L-valyl-N-[...)
Affinity DataKi:  2.5nM ΔG°:  -51.1kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361651(CHEMBL1940249)
Affinity DataKi:  2.5nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317208(CHEMBL1088115 | N-(adamantan-2-yl)-2-[cyclohexyl(e...)
Affinity DataKi:  3.10nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317216((2R)-N-(adamantan-2-yl)-1-(cyclohexylmethyl)pyrrol...)
Affinity DataKi:  3.5nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317218((2R)-N-(adamantan-2-yl)-1-(3,3,3-trifluoropropyl)p...)
Affinity DataKi:  3.60nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317222((2R)-N-(adamantan-2-yl)-1-(2-hydroxyethyl)pyrrolid...)
Affinity DataKi:  3.60nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29860(N-(Pyridin-2-yl) arylsulfonamide, 22)
Affinity DataKi:  4nM ΔG°:  -47.5kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29866(N-(Pyridin-2-yl) arylsulfonamide, 28)
Affinity DataKi:  4.80nM ΔG°:  -47.0kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92906(CHK1 compound 1)
Affinity DataKi:  5.14nM ΔG°:  -46.5kJ/molepH: 8.0 T: 2°CAssay Description:Surface plasmon resonance (SPR) biosensor binding studies were conducted using a Biacore 3000 instrument (GE Healtchare).More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317210((2R)-N-(adamantan-2-yl)-1-methylpyrrolidine-2-carb...)
Affinity DataKi:  5.40nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29858(N-(Pyridin-2-yl) arylsulfonamide, 20)
Affinity DataKi:  5.80nM ΔG°:  -46.5kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
University of Illinois At Chicago

LigandPNGBDBM16777(Substrate-based BACE-1 inhibitor, 16 | tert-butyl ...)
Affinity DataKi:  5.90nM ΔG°:  -48.9kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317219((2R)-N-(adamantan-2-yl)-1-[(4-chlorophenyl)methyl]...)
Affinity DataKi:  6.30nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29861(N-(Pyridin-2-yl) arylsulfonamide, 23)
Affinity DataKi:  6.60nM ΔG°:  -46.2kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
University of Illinois At Chicago

LigandPNGBDBM16781(Substrate-based BACE-1 inhibitor, 23 | tert-butyl ...)
Affinity DataKi:  8nM ΔG°:  -48.1kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
University of Illinois At Chicago

LigandPNGBDBM16779(Substrate-based BACE-1 inhibitor, 18 | tert-butyl ...)
Affinity DataKi:  9.40nM ΔG°:  -47.7kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317212((2R)-N-(adamantan-2-yl)-1-(propan-2-yl)pyrrolidine...)
Affinity DataKi:  9.40nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29865(N-(Pyridin-2-yl) arylsulfonamide, 27)
Affinity DataKi:  9.80nM ΔG°:  -45.3kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361651(CHEMBL1940249)
Affinity DataKi:  10nMAssay Description:Inhibition of His-tagged AKT1 using 5FAM-GRPRTSSFAEGCONH2 as substrate by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50317207(CHEMBL1088517 | N-cyclohexyl-2-(7,8-dihydro-4H-iso...)
Affinity DataKi:  15nMAssay Description:Inhibition of human 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317224((2R)-N-(adamantan-2-yl)-1-(oxan-4-ylmethyl)pyrroli...)
Affinity DataKi:  16nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50317225((2R)-N-(adamantan-2-yl)-1-[(1-hydroxycyclopentyl)m...)
Affinity DataKi:  17nMAssay Description:Inhibition of mouse 11-beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM29857(N-(Pyridin-2-yl) arylsulfonamide, 19)
Affinity DataKi:  20nM ΔG°:  -43.5kJ/molepH: 8.0 T: 2°CAssay Description:The enzyme assay was performed in a round-bottom 96-well plate. The enzyme was pre-incubated in the assay buffer in the presence of NADPH and inhibit...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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