Simple Search Results

Query String: CORTISONE

Cortone Cortisone acetate BDBM50455157 Cortisone
BDBM50378799 CORTISONE
BDBM28362 [3H]-cortisone
[3H]cortisone BDBM22452
BDBM13739 cortisone [3H]cortisone [3H]-cortisone (1S,2R,10S,11S,14R,15S)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-ene-5,17-dione

Pan, Y; Weng, J; Kabaleeswaran, V; Li, H; Cao, Y; Bhosle, RC; Zhou, M Cortisone dissociates the Shaker family K+ channels from their beta subunits. Nat Chem Biol 4: 708-14 (2008)
Xiang, J; Wan, ZK; Li, HQ; Ipek, M; Binnun, E; Nunez, J; Chen, L; McKew, JC; Mansour, TS; Xu, X; Suri, V; Tam, M; Xing, Y; Li, X; Hahm, S; Tobin, J; Saiah, E Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model. J Med Chem 51: 4068-71 (2008)

ChEMBL_1297897 Inhibition of recombinant human 11beta-HSD1 using cortisone/[3H]-cortisone as substrate after 5 hrs by reverse-phase HPLC analysis
ChEMBL_453205 Inhibition of human HSD1 assessed as interconversion of cortisone to cortisol
ChEMBL_453206 Inhibition of human HSD2 assessed as interconversion of cortisone to cortisol
ChEMBL_453207 Inhibition of mouse HSD1 assessed as interconversion of cortisone to cortisol
ChEMBL_453208 Inhibition of mouse HSD2 assessed as interconversion of cortisone to cortisol
ChEMBL_1362858 Inhibition of rat 11betaHSD1 assessed as reduction of cortisone to cortisol by ELISA
ChEMBL_607151 Inhibition of 11beta-HSD1 in rat liver assessed as cortisone level
ChEMBL_1931745 Inhibition of mouse microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol using [3H]cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_1931748 Inhibition of human microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol using [3H]cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_877516 Inhibition of 11beta-HSD2 assessed as conversion of cortisol to cortisone by fluorescence based assay
ChEMBL_450657 Inhibition of human 11-beta-HSD1 in CHO cells assessed as conversion of cortisone to cortisol
ChEMBL_607152 Inhibition of rat renal 11beta-HSD2 in rat liver assessed as inhibition of cortisone production
ChEMBL_877503 Inhibition of 11betaHSD1 in human adipocytes assessed as cortisone to cortisol conversion by scintillation counting method
ChEMBL_1813302 Inhibition of 11beta-HSD1 in human microsomes using [3H] cortisone as substrate by scintillation proximity assay
ChEMBL_362617 Inhibition of 11-beta-HSD1-dependent cortisone conversion to cortisol in mouse intact C2C12 cells
ChEMBL_424846 Inhibition of human truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPA
ChEMBL_424847 Inhibition of mouse truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPA
ChEMBL_561233 Inhibition of human 11beta-HSD1 expressed in CHO cells assessed as conversion of cortisone to cortisol by ELISA
ChEMBL_561244 Inhibition of mouse 11beta-HSD1 expressed in CHO cells assessed as conversion of cortisone to cortisol by ELISA
ChEMBL_561245 Inhibition of rat 11beta-HSD1 expressed in CHO cells assessed as conversion of cortisone to cortisol by ELISA
ChEMBL_561246 Inhibition of dog 11beta-HSD1 expressed in CHO cells assessed as conversion of cortisone to cortisol by ELISA
ChEMBL_675393 Inhibition of 11betaHSD1 in human platelet assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader
ChEMBL_942935 Inhibition of 11beta-HSD1 in human liver microsomes using cortisone and NADPH as substrate by HTRF assay
ChEMBL_1518302 Inhibition of 11beta-HSD1 in human mixed sex human liver microsomes assessed as reduction in conversion of [3H]-cortisone to [3H]-cortisol pre-incubated for 15 mins before [3H]-cortisone addition in presence of NADPH by scintillation proximity assay
ChEMBL_362618 Inhibition of 11-beta-HSD1-dependent cortisone conversion to cortisol in mouse intact 3T3 L1 cells
ChEMBL_741128 Inhibition of human recombinant 11beta-HSD1 assessed as conversion of radiolabeled-cortisone to cortisol by scintillation proximity assay
ChEMBL_741129 Inhibition of mouse recombinant 11beta-HSD1 assessed as conversion of radiolabeled-cortisone to cortisol by scintillation proximity assay
ChEMBL_942934 Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells using cortisone and NADPH as substrate by HTRF assay
ChEMBL_1293356 Inhibition of 11beta-HSD1 in mouse liver microsomes using cortisone as substrate after 2 hrs by HTRF assay
ChEMBL_1293357 Inhibition of 11beta-HSD1 in human liver microsomes using cortisone as substrate after 2 hrs by HTRF assay
ChEMBL_1297614 Inhibition of rat 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by competitive HTRF assay
ChEMBL_514765 Inhibition of 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to cortisol by SPA assay
ChEMBL_514766 Inhibition of 11beta-HSD2 expressed in CHO-K1 cells assessed as conversion of [3H]cortisol to cortisone by SPA assay
ChEMBL_561232 Inhibition of human recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay
ChEMBL_561240 Inhibition of mouse recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay
ChEMBL_561241 Inhibition of rat recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay
ChEMBL_561242 Inhibition of dog recombinant 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone by scintillation proximity assay
ChEMBL_675392 Inhibition of recombinant 11betaHSD1 expressed in CHO cells assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader
ChEMBL_699064 Inhibition of rat 11beta-HSD1 assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_814877 Inhibition of human 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay
ChEMBL_814879 Inhibition of mouse 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay
ChEMBL_1367112 Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of [3H]cortisone to [3H]cortisol conversion by SPA
ChEMBL_1461696 Inhibition of human 11beta-HSD1 transfected in HEK293 cells assessed as conversion of cortisone to cortisol after 30 mins by ELISA
ChEMBL_1466123 Inhibition of human 11beta-HSD1 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_1466125 Inhibition of mouse 11beta-HSD1 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_1466126 Inhibition of human 11beta-HSD2 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_190 Ability to convert [3H]cortisol to the tritium labeled cortisone in the presence of human 11 beta hydroxysteroid dehydrogenase type 2
ChEMBL_609376 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as reduction of cortisone to cortisol conversion by scintillation counting
ChEMBL_609881 Inhibition of human recombinant 11beta-HSD1 expressed in CHO cells assessed as conversion of [3H]cortisone to [3H]cortisol by SPA
ChEMBL_609882 Inhibition of 11beta-HSD1 in human adipocytes assessed as conversion of [3H]cortisone to [3H]cortisol after 2 hrs by SPA
ChEMBL_634656 Displacement of [3H]-cortisone human 17beta-HSD1 expressed in Escherichia coli after 30 mins by scintillation proximity assay
ChEMBL_634657 Displacement of [3H]-cortisone human 17beta-HSD1 expressed in HEK293 cells after 30 mins by scintillation proximity assay
ChEMBL_821475 Inhibition of human 11beta-HSD1 using [3H]cortisone as substrate assessed as production of [3H]-cortisol by scintillation proximity assay
ChEMBL_850500 Inhibition of 11betaHSD1 in human isolated adipocytes using [3H]cortisone as substrate after 6 hrs by flow scintillation analysis
ChEMBL_965017 Inhibition of human microsomal 11beta-HSD2 assessed as inhibition of conversion of radiolabeled cortisone to radiolabeled cortisol by cell-based assay
ChEMBL_965019 Inhibition of human microsomal 11beta-HSD1 assessed as inhibition of conversion of radiolabeled cortisone to radiolabeled cortisol by cell-based assay
ChEMBL_1437990 Inhibition of human 11beta-HSD1 in expressed in HEK293 cells microsomal fractions incubated with NADPH and [3H]-cortisone by scintillation proximity assay
ChEMBL_1437991 Inhibition of mouse 11beta-HSD1 in expressed in HEK293 cells microsomal fractions incubated with NADPH and [3H]-cortisone by scintillation proximity assay
ChEMBL_1466124 Inhibition of human 11beta-HSD1 expressed in HEK293 cells using NADPH assessed as conversion of cortisone to cortisol by cell-based assay
ChEMBL_674863 Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-3H]-cortisol to cortisone by scintillation counting
ChEMBL_674864 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]-cortisone to cortisol by scintillation counting
ChEMBL_675406 Inhibition of recombinant 11betaHSD1 expressed in CHO cells assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader in presence of plasma
ChEMBL_699052 Inhibition of human full length 11beta-HSD1 assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_740555 Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation counting
ChEMBL_740556 Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation counting
ChEMBL_775553 Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]-cortisone to [3H]-cortisol by scintillation plate reader
ChEMBL_821679 Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
ChEMBL_821680 Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
ChEMBL_821681 Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
ChEMBL_821682 Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
ChEMBL_821912 Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay
ChEMBL_821913 Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay
ChEMBL_835666 Inhibition of 11beta-HSD1 in mouse 3T3L1 cells assessed as conversion of cortisone to cortisol level after 150 mins by HTRF assay
ChEMBL_1453118 Inhibition of human recombinant 11beta-HSD-1 expressed in HEK293 EBNA cells using [3H]-cortisone and NADPH by scintillation proximity assay
ChEMBL_1453121 Inhibition of human recombinant 11beta-HSD-2 expressed in HEK293 EBNA cells assessed as reduction in cortisone formation ESI mass spectroscopy
ChEMBL_1453940 Inhibition of mouse recombinant 11beta-HSD-1 expressed in HEK293 EBNA cells using [3H]-cortisone and NADPH by scintillation proximity assay
ChEMBL_2027334 Inhibition of human 11beta-HSD1 expressed in HEK293 cells using cortisone in presence of NADPH regenerating-system incubated for 1 hr by ELISA
ChEMBL_582390 Inhibition of mouse liver microsome 11betaHSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
ChEMBL_584481 Inhibition of human microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_584482 Inhibition of mouse microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_584483 Inhibition of human microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_584484 Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_740937 Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisone to [3H]-cortisol by scintillation proximity assay
ChEMBL_740938 Inhibition of mouse 11beta-HSD2 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisol to [3H]-cortisone by scintillation proximity assay
ChEMBL_740939 Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisone to [3H]-cortisol by scintillation proximity assay
ChEMBL_740940 Inhibition of human 11beta-HSD2 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisol to [3H]-cortisone by scintillation proximity assay
ChEMBL_768815 Inhibition of 11 beta-HSD1 in differentiated human adipocytes assessed as conversion of [3H]-cortisone to [3H]-cortisol after 10 mins by HPLC
ChEMBL_791472 Inhibition of human 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_791473 Inhibition of mouse 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_791474 Inhibition of human 11beta-HSD2 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_1540426 Inhibition of 11beta-HSD1 in human liver microsomes assessed as conversion of [3H]-cortisone to [3H]-cortisol after 30 mins by scintillation proximity assay
ChEMBL_1742397 Inhibition of human 11beta-HSD1 expressed in HEK293 cell lysates using radiolabeled cortisone as substrate incubated for 10 mins by scintillation counting method
ChEMBL_500342 Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
ChEMBL_500343 Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
ChEMBL_617122 Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay
ChEMBL_617123 Displacement of [3H]cortisone from mouse 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay
ChEMBL_735656 Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-[3H]cortisol to cortisone after 10 mins by scintillation counting
ChEMBL_768819 Inhibition of human 11 beta-HSD2 expressed in CHO cells assessed as conversion of [3H]cortisol to [3H]cortisone after 1 hr by HPLC
ChEMBL_835662 Inhibition of human recombinant 11beta-HSD1 expressed in Escherichia coli assessed as conversion of cortisone to cortisol level after 150 mins by HTRF assay
ChEMBL_853405 Inhibition of mouse 11betaHSD1 in 3T3L1 cells assessed as conversion of [1,2-(N)3H]-cortisone to cortisol after 1 hr by liquid scintillation counter
ChEMBL_854804 Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol after 2 hrs by scintillation counting
ChEMBL_971356 Inhibition of human 11beta-HSD1 expressed in HEK293 cell microsomes assessed as inhibition of [3H]cortisone conversion to [3H]cortisol by scintillation proximity assay
ChEMBL_971357 Inhibition of mouse 11beta-HSD1 expressed in HEK293 cell microsomes assessed as inhibition of [3H]cortisone conversion to [3H]cortisol by scintillation proximity assay
ChEMBL_1556012 Inhibition of full length human 11beta-HSD2 expressed in HEK293 cells using cortisone as substrate incubated for 2 hrs by HTRF assay in presence of NAD+
ChEMBL_1813255 Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay
ChEMBL_735653 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol after 10 mins by scintillation counting
ChEMBL_821476 Inhibition of human 11beta-HSD1 expressed in human HEK293 cells using [3H]cortisone as substrate assessed as production of [3H]-cortisol by scintillation proximity assay
ChEMBL_938865 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cell using [1,2-3H]Cortisone as substrate after 10 mins by scintillation counting analysis
ChEMBL_969404 Inhibition of 11beta-HSD1 in human liver microsomes using [3H]-cortisone as substrate assessed as formation of cortisol after 60 to 90 mins by radiometric analysis
ChEMBL_1666539 Inhibition of 11beta-HSD1 in human microsomes using [3H]cortisone as substrate preincubated for 10 mins followed by substrate addition measured after 4 hrs by SPA
ChEMBL_1702993 Inhibition of full-length mouse 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
ChEMBL_1702996 Inhibition of full-length human 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
ChEMBL_1702997 Inhibition of full-length mouse 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
ChEMBL_1702998 Inhibition of full-length human 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
ChEMBL_699053 Inhibition of human recombinant full length 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
ChEMBL_768814 Inhibition of human 11 beta-HSD1 expressed in CHO cells assessed as conversion of [3H]cortisone to [3H]cortisol after 1 hr by scintillation proximity assay
ChEMBL_982342 Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as [1,2-3H]-cortisone reduction to [1,2,6,7-3H]-cortisol after 10 mins in presence of NADPH
ChEMBL_1297892 Inhibition of N-terminal 6-His-tagged full-length mouse 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by competitive HTRF assay
ChEMBL_1297893 Inhibition of N-terminal 6-His-tagged full-length human 11beta-HSD1 assessed as conversion of cortisone to cortisol after 25 mins by competitive HTRF assay
ChEMBL_1474762 Inhibition of human 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_1474764 Inhibition of mouse 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_850498 Inhibition of N-terminal His6-tagged full length dog 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay
ChEMBL_852659 Inhibition of N-terminal His6-tagged full length human 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay
ChEMBL_852716 Inhibition of N-terminal His6-tagged full length mouse 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay
ChEMBL_852717 Inhibition of N-terminal His6-tagged full length rat 11betaHSD1 expressed in baculovirus infected cells using cortisone as substrate after 25 mins by HTRF assay
ChEMBL_974557 Inhibition of mouse microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol by scintillation proximity assay in presence of NADPH
ChEMBL_974620 Inhibition of human microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol by scintillation proximity assay in presence of NADPH
ChEMBL_1829814 Inhibition of recombinant human 11beta-HSD1 expressed in HEK293 cell microsomes using [3H]cortisone as substrate after 4 hrs by homogeneous immuno-radiometric scintillation proximity assay
ChEMBL_1829815 Inhibition of recombinant mouse 11beta-HSD1 expressed in HEK293 cell microsomes using [3H]cortisone as substrate after 4 hrs by homogeneous immuno-radiometric scintillation proximity assay
ChEMBL_771464 Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay
ChEBML_1717698 Inhibition of 11beta-HSD1 in human liver microsomes using [3H]cortisone as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by scintillation proximity assay
ChEBML_1717704 Inhibition of 11beta-HSD1 in CD1 mouse liver microsomes using cortisone as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by LC-MS analysis
ChEMBL_1781518 Inhibition of human 11beta-HSD1 expressed in HEK293 cell lysate using [1,2-3H]-cortisone as substrate preincubated for 10 mins followed by substrate addition in presence of NADPH by scintillation counting
ChEMBL_543009 Inhibition of full length human recombinant 11beta-HSD1 expressed in baculovirus insect cell system assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
ChEMBL_768816 Inhibition of human 11 beta-HSD1 expressed in CHO cells assessed as conversion of [3H]-cortisone to [3H]-cortisol after 1 hr by scintillation proximity assay in presence of human plasma
ChEMBL_990495 Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of [1,2,-3H]-cortisone to [3H]cortisol preincubated for 10 mins before substrate addition by scintillation counting
ChEMBL_990496 Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as inhibition of [1,2,6,7-3H]-cortisol to [3H]cortisone preincubated for 10 mins before substrate addition by scintillation counting
ChEMBL_1364761 Inhibition of N-terminal His-tagged full length human 11beta-HSD1 assessed as inhibition of cortisone to cortisol conversion preincubated for 25 mins measured after 2 hrs by HTRF assay
ChEMBL_1364762 Inhibition of N-terminal His-tagged full length mouse 11beta-HSD1 assessed as inhibition of cortisone to cortisol conversion preincubated for 25 mins measured after 2 hrs by HTRF assay
ChEMBL_1364763 Inhibition of N-terminal His-tagged full length rat 11beta-HSD1 assessed as inhibition of cortisone to cortisol conversion preincubated for 25 mins measured after 2 hrs by HTRF assay
ChEMBL_1685711 Inhibition of 11beta-HSD1 in human omental adipocytes using [3H]cortisone as substrate preincubated for 1 hr followed by substrate addition measured after 3 to 4 hrs by scintillation proximity assay
ChEMBL_821477 Inhibition of human 11beta-HSD1 expressed in human HEK293 cells using [3H]cortisone as substrate assessed as production of [3H]-cortisol by scintillation proximity assay in presence of 3% human serum albumin
ChEMBL_938071 Inhibition of human 11beta-HSD2 expressed in CHO cells using [3H]-Cortisone as substrate incubated for 30 mins prior to substrate addition measured after 120 mins by scintillation counting analysis
ChEMBL_699054 Inhibition of human recombinant full length 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of 3% human serum albumin
ChEMBL_699055 Inhibition of human recombinant full length 11beta-HSD1 expressed in human adipocytes assessed as inhibition of conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of 3% human serum albumin
ChEMBL_947108 Inhibition of human 11-beta HSD1 transfected in HEK293 cell microsomes assessed as decrease in [3H]cortisol generation using [3H]cortisone as substrate measured after 60 mins by scintillation proximity assay
ChEMBL_543487 Inhibition of FLAG-tagged full length human 11beta-HSD1 expressed in baculovirus-infected Trichoplusia ni Hi5 cells assessed as reduction of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH
ChEBML_1685710 Inhibition of human 11beta-HSD1 expressed in CHO cell microsomes using [3H]cortisone as substrate preincubated with substrate for 10 mins followed by enzyme addition measured after 90 mins by microbeta scintillation proximity assay
ChEMBL_1685710 Inhibition of human 11beta-HSD1 expressed in CHO cell microsomes using [3H]cortisone as substrate preincubated with substrate for 10 mins followed by enzyme addition measured after 90 mins by microbeta scintillation proximity assay
ChEMBL_2027541 Inhibition of active recombinant human N-terminal His-tagged 11-betaHSD1 expressed in Escherichia coli using cortisone, NADPH and glucose-6-phosphate incubated for 2 hrs by glucose-6-phosphate dehydrogenase based coupled HTRF immuno-competitive assay
11beta-HSD1 Homogeneous Time-Resolved Fluorescence (HTRF) Assay 11beta-HSD1 enzyme activity was assessed in buffer containing a substrate mixture cortisone/NADPH in the presence of test compound. Reaction was initiated by addition of 11beta-HSD1 and terminated with addition of 18beta-glycyrrhetinic acid stop solution. Determinations of cortisol levels were monitored by HTRF assay (Cisbio International).
11beta-HSD1 SPA Assay Enzyme assays were performed using purified recombinant human 11beta-HSD1. The fractional conversion of cortisone to cortisol was used to determine enzyme activities. The radioactive cortisol generated in the assay was captured by a monoclonal anti-cortisol antibody and SPA beads coated with anti-mouse antibodies. Radiometric quantitation was determined on a TopCount NXT instrument.
Homogenous Time-Resolved Fluorescence (HTRF) Assay The in vitro inhibitory activities of the novel compounds to human 11β-HSD1 were evaluated in accordance with homogenous time-resolved fluorescence (HTRF). The human 11β-HSD1 overexpressing cells were subcultured at the number of 2.5�104 cells in 96-well plate and stabilized for 24 hr. The cells in each well were incubated with 100 μl of medium containing 160 nM cortisone (Sigma) and diluted compound for 3 hr at 37� C. in an incubator. Then, samples of the medium (10 μl) were transferred to 384-well plate and the amounts of cortisol produced were measured using a cortisol kit (Cisbio international) in accordance with manufacturer's instruction. The control group was incubated with 160 nM cortisone and 0.1% DMSO.
Human and Mouse 11beta-HSD1 SPA Assay Enzyme assays were performed using purified recombinant human or mouse11beta-HSD1. The fractional conversion of cortisone to cortisol was used to determine enzyme activities. The radioactive cortisol generated in the assay was captured by a monoclonal anti-cortisol antibody and SPA beads coated with anti-mouse antibodies. Radiometric quantitation was determined on a TopCount NXT instrument.
Time Resolved Fluorescence Assay The conversion of cortisone to the active steroid cortisol by 11βHSD1 oxo-reductase activity, can be measured using a competitive homogeneous time resolved fluorescence assay (HTRF) (CisBio International, R&D, Administration and Europe Office, In Vitro Technologies HTRF/Bioassays BP 84175, 30204 Bagnols/Cèze Cedex, France. Cortisol bulk HTRF kit: Cat No. 62CORPEC).
Human and Mouse 11beta-HSD1 SPA Assay Enzyme assays were performed using purified recombinant human or mouse11beta-HSD1. The fractional conversion of cortisone to cortisol was used to determine enzyme activities. The radioactive cortisol generated in the assay was captured by a monoclonal anti-cortisol antibody and SPA beads coated with anti-mouse antibodies. The plate was read using a liquid scintillation counter, The percent inhibition was calculated relative to a noninhibited control and plotted against compound concentration to generate the IC50 results.
Human 11beta-HSD1 SPA Assay Enzyme assays were performed using purified recombinant human 11beta-HSD1. The fractional conversion of cortisone to cortisol was used to determine enzyme activities. The radioactive cortisol generated in the assay was captured by a monoclonal anti-cortisol antibody and SPA beads coated with anti-mouse antibodies. Radiometric quantitation was determined on a TopCount NXT instrument. EC50/IC50 was obtained from cell-based enzyme assays (h-293) utilized HEK293 cells stably expressing recombinant human full-length 11beta-HSD1 as the enzyme source without supplementation of NADPH.
Mouse and Rat 11beta-HSD1 SPA Assay Enzyme assays were performed using purified recombinant enzymes, incubating with test compound and [3H]cortisone/NADPH. After incubation, the amount of the product, [3H]-cortisol, captured on the anticortisol antibody-coated SPA beads was determined in a microplate liquid scintillation counter. Kinetic constants were calculated using the Microsoft Excel integrated application XLfit (Version 5.3.0.19, ID Business Solutions Ltd.) using the sigmoidal dose-response model 205, which is based on the nonlinear curve fitting based on Levenberg-Marquardts algorithm.
Human 11beta-HSD1 Scintillation Proximity Assay (SPA) The 11beta-HSD1 enzyme assay was carried out in the replica plates of the compounds in reaction buffer containing substrate mixture [3H]-cortisone/NADPH. Reactions were initiated by the addition of the enzyme. After incubation, the amount of the product, [3H]-cortisol, captured on the anticortisol antibody-coated SPA beads was determined in a microplate liquid scintillation counter. Kinetic constants were calculated using the Microsoft Excel integrated application XLfit (Version 5.3.0.19, ID Business Solutions Ltd.) using the sigmoidal dose-response model 205, which is based on the nonlinear curve fitting based on Levenberg-Marquardts algorithm.
Measurement of 11beta-HSD1 Activity 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 inhibitor. Next, the reaction is initiated by adding a regenerating system (consisting of glucose-6-phosphate, glucose-6-phosphate dehydrogenase, and MgCl2), and labeled 3H-cortisone substrate. After the incubation, the substrate and product peaks are separated and analyzed by using an HPLC system. The initial reaction velocities recorded were in the linear range and were determined by measuring the peak area for cortisol formation with time. The inhibition of 11beta-HSD was analyzed by fitting the data to an equation to determine apparent inhibition constant Ki.
Scintillation Proximity Assay (SPA) 11beta-HSD1 microsomes isolated from HEK 293 cells over-expressing human 11beta-HSD1 were incubated with the substrate cortisone and cofactor NADPH at room temperature. The reactions were terminated with the addition of a nonspecific 11beta-HSD1 inhibitor (18beta-glycyrrhetinic acid). The product cortisol was quantified in an immuno-competition SPA wherein the [3H]-cortisol bound to anti-rabbit antibody Yitrium silicate SPA beads coated with polyclonal anti-cortisol antibody was competed by cortisol produced in the reaction, and the reaction mixture was read in a scintillation plate reader (TopCount). The amount of cortisol was determined from a cortisol standard curve.
HTRF Assay The inhibiting activity of 11β-HSD1 derived from microsomal fractions was measured using the HTRF assay (62CO2PEB, Cisbio). Different concentrations of compounds were added to 96-well plates, followed by the addition of TE buffer (20 mM Tris buffer and 5 mM EDTA, pH 6.0) containing 200 μM NADPH (N1630, Sigma) and 160 nM cortisone (C2755, Sigma), The reactions were initiated by the addition of human microsomal fractions (M0317, Sigma), and were allowed to incubate for 2 h at 37� C. Europium (Eu3+) cryptate and XL665-conjugated cortisol were then added to each well and incubated for an additional 2 h at room temperature.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay n vitro inhibition of 11β-HSD1 by test compounds is determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds are incubated for 1 hour at 37� C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 μM) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction is typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm).
Homogeneous Time Resolved Fluorescence Assay Vitro inhibition of 11.beta.-HSDl by test compounds, HTRF detecting cortisol generated from Koruchisuteron (cortisterone) by human liver microsomes (Homogeneous Time Resolved Fluorescence (Homogeneous Time-Resolved Fluorescence)) Method (cisbio international, France) in was measured. Briefly, the compound, tris buffer containing NADPH (200uM) and cortisone (80nM) (20mM Tris, 5 mM EDTA, pH 6.0) in and incubated for 1 hour at 37 °C. Then, cortisol generated in the reaction was detected by competitive immunoassay comprising two HTRF conjugates (anti-cortisol antibody labeled with bound cortisol and europium cryptate to the XL665). Incubation period for detection reaction was typically 2 hours. The amount of Cortisol, time-resolved fluorescence of the wells; was determined by reading the (Ex 320 / 75nm Em 615 / 8.5nm and 665 / 7.5nm). Then, the ratio of the two light-emitting signal was calculated (Em665 * 10000 / Em615).
Homogeneous Time-Resolved Fluorescence (HTRF) In vitro inhibition of 11beta -HSD1 by test compounds was determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds were incubated for 1 hour at 37 C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 uM) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction was typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals is then calculated (Em665*10000/Em615).
Homogeneous Time-Resolved Fluorescence Assay In vitro inhibition of 11beta -HSD1 by test compounds is determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds are incubated for 1 hour at 37C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 uM) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction is typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals is then calculated (Em665X10000/Em615).
Enzyme Assay The 11-β-HSD-1 enzyme assay was carried out in 96 well microtiter plates in a total volume of 100 μl containing 30 mM Hepes buffer, pH 7.4 with 1 mM EDTA, substrate mixture cortisone/NADPH (200 nM/200 μM), G-6-P (1 mM) and inhibitors in serial dilutions. Reactions were initiated by addition of 10 μl 11-β-HSD-1 (3 μg) from E. coli, either as microsome fractions from rat and mice liver (2.5 μg). Following mixing, the plates were shaken for 150 minutes at 37° C. The reactions were terminated with 10 μl Acid-18beta glycyrrhetinic stop solution. Determinations of cortisol levels in 11-β-HSD-1 preparations were monitored by HTRF (HTRF cortisol assay from Cis bio international).
Enzyme Inhibition Assay A reaction was performed on a 384-well plate (Greiner Bio One) using a reaction volume of 24 �L, and all the samples were diluted with an assay buffer (50 mM tris buffer, pH 7.4, 10% glycerol). 0.8 mM NADPH, 6 mM glucose 6-phosphate, 0.35 units/mL glucose 6-phosphate dehydrogenase (Sigma Chemical), and 3 mM magnesium chloride and a microsome fraction as an enzyme source were added to the plate, and a solution containing a test compound dissolved in a dimethyl sulfoxide/methanol solution was added at a final concentration of 0.1%. After the addition of the test compound, cortisone at a final concentration of 160 nM was added to start the reaction, and the reaction was performed at room temperature for 3 h. 25 �L of 100 mM carbenoxolone (Sigma Chemical) was added to terminate the reaction, and the amount of cortisol produced was measured with RUBYstar (BMG LABTECH JAPAN Ltd.) using a cortisol prototype kit (Cisbio International) according to the package insert.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay In vitro inhibition of 11beta -HSD1 was determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisolgenerated from cortisterone by human liver microsomes. Compounds were incubated for 1 hour at 37 C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 uM) and cortisone (80 nM). Cortisol generated in the reaction was then detected by a competitive immunoassay involving two HTRF conjugates: cortisol linked to XL665 and anticortisol antibody labeled with Europium cryptate. The incubation period for detection reaction was 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals was then calculated (Em665*10000/Em615). Each assay contained incubations with vehicle controls instead of compound as controls for non-inhibited cortisol generation.
Scintillation Proximity Assay Inhibition of microsomal preparations of 11.beta.-HSDl by compounds of the present invention, as described essentially previously (K. Solly, SS Mundt, HJ Zokian, GJ Ding, A. Hermanowski-Vosatka, B. Strulovici, and W. Zheng, High-Throughput Screening of 11-Beta-Hydroxyseroid Dehydrogenase Type 1 in Scintillation Proximity Assay Format. Assay Drug Dev Technol 3 (2005) 377-384) was measured. All reactions were carried out in a clear flexible PET Microbeta plates 96-well at room temperature (PerkinElmer). Assay, substrate solution (50mM HEPES, pH7.4,100mM KCl, 5mM NaCl, 2mM MgCl 2, 2mM NADPH and 160nM [3 H] cortisone (1Ci / mmol)) a 49ul and distribution, and starting from the 0.1mM on to start by combining the semi-log (half-log) multiple of the incremental test compound 1uL in DMSO previously diluted (8 points). After pre-incubation of 10 minutes, incubated human 11-HSD1 overexpress the enzyme containing CHO cells isolated from microsomes solution 50uL.
Scintillation Proximity Assay The inhibition of a microsomal preparation of 11beta -HSD1 by compounds of the invention was measured essentially as previously described (K. Solly, S. S. Mundt, H. J. Zokian, G. J. Ding, A. Hermanowski-Vosatka, B. Strulovici, and W. Zheng, High-Throughput Screening of 11-Beta-Hydroxyseroid Dehydrogenase Type 1 in Scintillation Proximity Assay Format. Assay Drug Dev Technol 3 (2005) 377-384). All reactions were carried out at rt in 96 well clear flexible PET Microbeta plates (PerkinElmer). The assay begins by dispensing 49 ul of substrate solution (50 mM HEPES, pH 7.4, 100 mM KCl, 5 mM NaCl, 2 mM MgCl2, 2 mM NADPH and 160 nM [3H]cortisone (1 Ci/mmol)) and mixing in 1 uL of the test compounds in DMSO previously diluted in half-log increments (8 points) starting at 0.1 mM. After a 10 minute pre-incubation, 50 uL of enzyme solution containing microsomes isolated from CHO cells overexpressing human 11beta -HSD1 (10-20 ug/ml of total protein) was added.
Homogeneous Time-Resolved Fluorescence (HTRF) In vitro inhibition of 11β-HSD1 by test compounds is determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds are incubated for 1 hour at 37� C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (20011M) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction is typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals is then calculated (Em665*10000/Em615). Each assay contains incubations with vehicle controls instead of compound as controls for non-inhibited cortisol generation (100% CTL; high values) and incubations with carbenoxolone as controls for fully inhibited enzyme and cortisol background (0% CTL; low values). Each assay also contains a calibration curve with cortisol to transform the fluorescent data into cortisol concentrations.
Inhibition Assay The procedure for measuring the 11β-HSD1-inhibitory activity is as follows. The enzyme reaction and the measurement were carried out using a 384-well plate. The enzyme was prepared in accordance with Journal of Biological Chemistry, 2001, Vol. 276, p. 21343-21350. The reaction was carried out by adding a test compound at various concentrations to a reaction liquid consisting of a 5 mM phosphate buffer (pH 6.6), 200 nM cortisone, 40 μM reduced nicotinamide adenine dinucleotide phosphate (NADPH), and rat recombinant 11β-HSD1, followed by incubating at room temperature for one hour (10 μl/well). The test compound was prepared by dissolving in dimethyl sulfoxide (DMSO) such that a DMSO concentration reached 1% in the reaction liquid. After the enzyme reaction was completed, the enzyme inhibitory action was measured by detecting cortisol using a homogeneous time-resolved fluorescence (HTRF) method. Each of a d2-labeled cortisol containing 400 μM carbenoxolone and a cryptate-labeled cortisol antibody (CIS Bio International Co., Ltd.) was added at 5 μl/well, followed by incubating at room temperature for 2 hours, and then the fluorescence intensity was measured using a fluorophotometer (trade name: ARVO HTS 1420, Perkin Elmer/Wallac), and the enzyme inhibitory activity was calculated from the fluorescence intensity ratio of two wavelengths (665 nm/620 nm).The measurement results were calculated by averaging the values of 3 wells of the same condition. The ratio when DMSO was added instead of the test compound was taken as 0% and the ratio when 11β-HSD1 was not added was taken as 100%, thereby calculating the 50% inhibition concentration of the test compound as IC50 of the compound inhibitory activity.