Assay ID | Title | Year | Journal | Article |
AID155143 | In vitro inhibitory activity against bovine adrenal phenylethanolamine N-methyl-transferase (PNMT) | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1
| Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and th |
AID156051 | Ability to inhibit phenylethanolamine N-methyl-transferase (PNMT) | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID282850 | Binding affinity to human PNMT K57A mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID155157 | Epinephrine to norepinephrine ratio at dose 100 mg/kg | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID25585 | Dissociation constant was determined | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
| Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. |
AID155148 | Binding selectivity against PNMT and alpha-2-adrenoceptors, measured as a ratio of respective in vitro Ki's. | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1
| Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and th |
AID293030 | Displacement of [3H]clonidine from adrenergic alpha2 receptor in Sprague-Dawley rat cortex membrane | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors. |
AID156064 | Inhibitory activity against bovine adrenal phenylethanolamine N-methyl-transferase (PNMT) | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT. |
AID37366 | Compound was tested in vitro for its affinity towards rat Alpha-2 adrenergic receptor | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID35395 | Inhibition of [3H]clonidine binding to the rat alpha-2-adrenoceptor | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT. |
AID233905 | Selectivity was expressed as the ratio is Ki of alpha 2-Adrenoceptor to that of PNMT | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
| Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. |
AID21842 | Calculated partition coefficient (clogP) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID244103 | Ratio of Ki for PNMT to that of alpha-2-adrenoceptor was determined | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity tow |
AID234631 | Selectivity ratio (alpha2/PNMT) | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID239080 | In vitro binding affinity against human phenylethanolamine N-Methyltransferase | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. |
AID155306 | Inhibitory constant against bovine phenylethanolamine N-methyl-transferase | 2001 | Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
| Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme. |
AID37094 | Binding affinity to alpha-2 adrenergic receptor by displacement of [3H]clonidine | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID155146 | Inhibition of PNMT (Phenylethanolamine N-Methyltransferase) in vitro | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
| Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID35770 | Inhibitory potency against alpha-2 adrenergic receptor | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID155154 | In vitro % inhibition of Phenylethanolamine N-Methyltransferase at 10 E-4M, using partially purified, lyophilized PNMT preparation derived from rabbit adrenals | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID155159 | Epinephrine to norepinephrine ratio at dose 50 mg/kg | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID155150 | Phenylethanolamine N-Methyltransferase inhibition assay in a 7-day mouse study was determined by epinephrine level at 100 mg/kg dose | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID257556 | Displacement of [3H]clonidine from Adrenergic alpha-2 receptor | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity. |
AID393044 | Binding affinity to wild type human PNMT by liquid scintillation spectrometry in presence of [3H]AdoMet | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline. |
AID298195 | Ratio of Ki for wild type human PNMT to Ki for human PNMT K57 mutant | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
| Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase. |
AID282848 | Binding affinity to human wild type his-tagged PNMT | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID37371 | Inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
| Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. |
AID237342 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity tow |
AID155152 | Phenylethanolamine N-Methyltransferase inhibition assay in a 7-day mouse study was determined by epinephrine level at 50 mg/kg dose | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID282853 | Binding affinity to human free PNMT | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID42827 | Apparent permeability value through blood-brain barrier was evaluated using bovine brain microvessel endothelial cells (BBMEC) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID293031 | Selectivity for human PNMT over Sprague-Dawley rat adrenergic alpha-2 receptor | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors. |
AID293029 | Binding affinity to human PNMT | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors. |
AID155337 | Ki ratio of human versus bovine phenylethanolamine N-methyl-transferase | 2001 | Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
| Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme. |
AID155308 | Inhibitory potency against bovine phenylethanolamine N-Methyltransferase (PNMT) | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID313558 | Inhibition of bovine PNMT by radiochemical assay | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase. |
AID282849 | Binding affinity to human PNMT V53A mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID282852 | Binding affinity to human PNMT D267A mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID155155 | In vitro % inhibition of Phenylethanolamine N-Methyltransferase at 10 E-6M, using partially purified, lyophilized PNMT preparation derived from rabbit adrenals | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID239958 | Binding affinity against alpha 2 adrenergic receptor in rat cortex using [3H]clonidine as radioligand | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines. |
AID393046 | Selectivity for wild type human PNMT to human PNMT K57A mutant | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline. |
AID271161 | Displacement of [3H]clonidine from Sprague-Dawley rat cortex adrenergic alpha 2 receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. |
AID37379 | In vitro binding affinity towards cortical membranes of male Sprague-Dawley rats alpha-2 adrenergic receptor by replacing [3H]clonidine | 1999 | Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
| 3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor. |
AID155151 | Phenylethanolamine N-Methyltransferase inhibition assay in a 7-day mouse study was determined by epinephrine level at 25 mg/kg dose | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID257555 | Inhibitory activity against human PNMT | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity. |
AID155141 | In vitro inhibitory activity against bovine adrenal phenylethanolamine N-methyl transferase | 1999 | Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
| 3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor. |
AID155158 | Epinephrine to norepinephrine ratio at dose 25 mg/kg | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
| Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. |
AID293032 | Ratio of Ki of drug to 1,2,3,4-tetrahydroisoquinoline for Sprague-Dawley rat adrenergic alpha-2 receptor | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors. |
AID233623 | Ratio of binding affinity of PNMT to alpha-2 receptors. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
| Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID35195 | In vitro inhibition of [3H]clonidine binding at the alpha-2 adrenergic receptor. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
| Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID239041 | Inhibition of [3H]clonidine binding to rat Alpha2 adrenoceptor | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity tow |
AID35335 | Selectivity determined by Ki of alpha 2 receptor / Ki of PNMT | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
| Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID155136 | Affinity for bovine Phenylethanolamine N-Methyltransferase | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID37365 | Compound was tested in vitro for binding affinity against Alpha-2 adrenergic receptor using [3H]clonidine | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
| Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID271160 | Binding affinity to human PNMT expressed in Escherichia coli by radiochemical assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. |
AID155320 | Inhibitory constant against human phenylethanolamine N-methyl-transferase over-expressed in Escherichia coli | 2001 | Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
| Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme. |
AID243071 | Selectivity ratio for binding to alpha-2-adrenoceptor and phenylethanolamine N-Methyltransferase | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. |
AID239340 | Binding affinity against human alpha 2A adrenergic receptor in CHO cells using [3H]RX-821002 as radioligand | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines. |
AID155138 | Inhibition of Phenylethanolamine N-methyl-transferase (PNMT) | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
| Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. |
AID393045 | Binding affinity to human PNMT K57A mutant by liquid scintillation spectrometry in presence of [3H]AdoMet | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline. |
AID37384 | In vitro inhibitory activity against Alpha-2 adrenergic receptor using [3H]clonidine as radioligand in male Sprague-Dawley rats | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1
| Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and th |
AID239195 | In vitro inhibition of [3H]clonidine from alpha-2 adrenergic receptor of rat cortex | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. |
AID257557 | Selectivity of Adrenergic alpha-2 receptor over human PNMT | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity. |
AID282851 | Binding affinity to human PNMT E219A mutant | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID282854 | Binding affinity to human PNMT-S-adenosyl-L-methionine complex | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase. |
AID155145 | In vitro inhibition of PNMT (Phenylethanolamine N-Methyltransferase). | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
| Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID16300 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID313560 | Selectivity of Ki for bovine PNMT over Ki for rat alpha-2 adrenoceptor | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase. |
AID239072 | Inhibitory binding affinity for phenylethanolamine N-methyl-transferase (PNMT) | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
| Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data. |
AID35216 | Ratio for binding affinity towards alpha-2 adrenoceptor to PNMT | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. |
AID271162 | Selectivity for human PNMT over rat Adrenergic alpha-2 receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. |
AID239624 | Inhibition of [3H]methyl-AdoMet binding to human phenylethanolamine N-methyl-transferase expressed in Escherichia coli BL21 | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity tow |
AID313559 | Displacement of [3H]clonidine from adrenergic alpha-1 receptor in Sprague-Dawley rat cortex | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase. |
AID156055 | In vitro inhibition of bovine phenylethylamine N-methyl-transferase (PNMT) using radiochemical assay. | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
| Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4,-tetrahydroisoquinolines: further studies on the hydrophilic pocket of the aromatic ring binding region of the active site. |
AID233871 | Selectivity expressed as the ratio of Ki of alpha-2-adrenoceptor to that of PNMT | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID1797149 | alpha-Adrenoceptor Radioligand Binding Assay from Article 10.1021/jm0205752: \\Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.\\ | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID1797148 | Radiochemical Assay for PNMT Activity from Article 10.1021/jm0205752: \\Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.\\ | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase. |
AID1796978 | Radiochemical Assay of PNMT Inhibitors from Article 10.1021/jm060466d: \\Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.\\ | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2001 | Structure (London, England : 1993), Oct, Volume: 9, Issue:10
| Getting the adrenaline going: crystal structure of the adrenaline-synthesizing enzyme PNMT. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2001 | Structure (London, England : 1993), Oct, Volume: 9, Issue:10
| Getting the adrenaline going: crystal structure of the adrenaline-synthesizing enzyme PNMT. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |