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Found 6331 Enz. Inhib. hit(s) with Target = '11-beta-hydroxysteroid dehydrogenase 1'
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50507371(BMS-823778)
Affinity DataKi:  0.900nMAssay Description:Inhibition of recombinant human 11beta-HSD1 expressed in HEK293 cell microsomes using [3H]cortisone as substrate after 4 hrs by homogeneous immuno-ra...More data for this Ligand-Target Pair
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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))
Bristol-Myers Squibb

Curated by ChEMBL
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))
Bristol-Myers Squibb

Curated by ChEMBL
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(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))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50248569((1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydr...)
Affinity DataKi:  1.10nMAssay Description:Inhibition of human 11beta-HSD1 using variable cofactor NADPH concentration by Lineweaver burk plotMore data for this Ligand-Target Pair
Target11-beta-hydroxysteroid dehydrogenase 1(Rattus norvegicus (rat))
Merck & Co.

Curated by ChEMBL
LigandPNGBDBM50174298(3-(4-(3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl)bicy...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of rat 11beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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))
Bristol-Myers Squibb

Curated by ChEMBL
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))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197399(2-(2-chloro-phenoxy)-2-methyl-N-(5-sulfamoyl-adama...)
Affinity DataKi:  2nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50202094(CHEMBL375341 | N-(5-hydroxy-adamantan-2-yl)-2-(3-t...)
Affinity DataKi:  2nMAssay Description:Inhibition of mouse 11beta-HSD1 expressed in E. coli by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197404(2-(2,6-dichloro-4-fluoro-phenoxy)-2-methyl-N-(5-su...)
Affinity DataKi:  2nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197418(2-(2-chloro-phenoxy)-N-(5-methanesulfonyl-adamanta...)
Affinity DataKi:  2nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50195289(1-piperidin-1-yl-cyclopropanecarboxylic acid (5-hy...)
Affinity DataKi:  2nMAssay Description:Inhibition of human truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50195289(1-piperidin-1-yl-cyclopropanecarboxylic acid (5-hy...)
Affinity DataKi:  2nMAssay Description:Inhibition of mouse truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50248569((1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydr...)
Affinity DataKi:  2.70nMAssay Description:Inhibition of human 11beta-HSD1 using variable substrate cortisol concentration by Lineweaver burk plotMore data for this Ligand-Target Pair
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197403(CHEMBL393167 | N-(5-methanesulfonyl-adamantan-2-yl...)
Affinity DataKi:  3nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM13746(2-((S)-1-(2-fluorophenyl)ethylamino)-5-isopropyl-5...)
Affinity DataKi:  3nM ΔG°:  -48.2kJ/molepH: 7.2 T: 2°CAssay Description:Enzyme assays were performed using purified recombinant human or mouse11beta-HSD1. The fractional conversion of cortisone to cortisol was used to det...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50195298(4-[2-(3,3-difluoro-piperidin-1-yl)-butyrylamino]-a...)
Affinity DataKi:  3nMAssay Description:Inhibition of mouse truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50195299(4-({1-[4-(5-trifluoromethyl-pyridin-2-yl)-piperazi...)
Affinity DataKi:  3nMAssay Description:Inhibition of mouse truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197416(2-(2-chloro-4-fluoro-phenoxy)-2-methyl-N-(5-sulfam...)
Affinity DataKi:  3nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50197404(2-(2,6-dichloro-4-fluoro-phenoxy)-2-methyl-N-(5-su...)
Affinity DataKi:  3nMAssay Description:Inhibition of human HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197410(2-methyl-N-(5-sulfamoyl-adamantan-2-yl)-2-(2-trifl...)
Affinity DataKi:  3nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM22473(2-(hexahydro-2,5-methanopentalen-3a(1H)-ylamino)-1...)
Affinity DataKi:  3nM ΔG°:  -48.2kJ/molepH: 7.2 T: 2°CAssay Description:The 11beta-HSD1 enzyme assay was carried out in the replica plates of the compounds in reaction buffer containing substrate mixture [3H]-cortisone/NA...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Rattus norvegicus (rat))
Merck & Co.

Curated by ChEMBL
LigandPNGBDBM50202094(CHEMBL375341 | N-(5-hydroxy-adamantan-2-yl)-2-(3-t...)
Affinity DataKi:  3nMAssay Description:Inhibitory activity against rat 11beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50202094(CHEMBL375341 | N-(5-hydroxy-adamantan-2-yl)-2-(3-t...)
Affinity DataKi:  3nMAssay Description:Inhibition of human 11beta-HSD1 expressed in E. coli by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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(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))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50239606(CHEMBL4080667)
Affinity DataKi:  3.80nMAssay Description:Inhibition of 11beta-HSD1 in human microsomes using [3H]cortisone as substrate preincubated for 10 mins followed by substrate addition measured after...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Rattus norvegicus (rat))
Merck & Co.

Curated by ChEMBL
LigandPNGBDBM50340378(3-(4-(2-(ethylsulfonyl)ethyl)bicyclo[2.2.2]octan-1...)
Affinity DataKi:  3.90nMAssay Description:Inhibition of rat 11beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Rattus norvegicus (rat))
Merck & Co.

Curated by ChEMBL
LigandPNGBDBM50195481((1s,4s)-ethyl 4-(4-amino-3,5-dichloro-N-cyclopropy...)
Affinity DataKi:  4nMAssay Description:Inhibition of rat 11beta-HSD1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50216921(2-(1-adamantylamino)-1-oxa-3-azaspiro[4.4]non-2-en...)
Affinity DataKi:  4nMAssay Description:Binding affinity to human 11beta-HSD1 by SPA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50195504((4-amino-3,5-dichlorophenyl)(1,3,3-trimethyl-6-aza...)
Affinity DataKi:  4nMAssay Description:Inhibition of human 11beta-HSD1 expressed in Escherichia coli by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50195506((4-amino-3,5-dichloro-phenyl)-(2-aza-tricyclo[3.3....)
Affinity DataKi:  4nMAssay Description:Inhibition of human 11beta-HSD1 expressed in Escherichia coli by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50197408(2-(3-chloro-phenoxy)-2-methyl-N-(5-sulfamoyl-adama...)
Affinity DataKi:  4nMAssay Description:Inhibition of human HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50197414(2-(2-chloro-4-fluoro-phenoxy)-N-(5-methanesulfonyl...)
Affinity DataKi:  4nMAssay Description:Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM13749((5S)-2-{[(1S)-1-(2-fluorophenyl)ethyl]amino}-5-met...)
Affinity DataKi:  4nM ΔG°:  -47.5kJ/molepH: 7.2 T: 2°CAssay Description:Enzyme assays were performed using purified recombinant human or mouse11beta-HSD1. The fractional conversion of cortisone to cortisol was used to det...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target11-beta-hydroxysteroid dehydrogenase 1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
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
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