Target Validation Information
Target ID T01777
Target Name Alpha-2C adrenergic receptor
Target Type
Successful
Drug Potency against Target 3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 3800 nM [527365]
CONESSINE Drug Info Ki = 10.6 nM [529632]
TRACIZOLINE Drug Info Ki = 7413 nM [526918]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info Ki = 24 nM [533805]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 516 nM [526994]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline Drug Info Ki = 840 nM [534531]
MEDETOMIDINE Drug Info Ki = 19 nM [533805]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 1100 nM [534315]
SNAP-5089 Drug Info Ki = 912 nM [525611]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info IC50 = 3600 nM [534087]
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine Drug Info Ki = 8800 nM [534315]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info Ki = 8.8 nM [534467]
MOXONIDINE Drug Info Ki = 2000 nM [534128]
MEZILAMINE Drug Info Ki = 12 nM [533406]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info IC50 = 2300 nM [534087]
R-226161 Drug Info Ki = 0.7 nM [528772]
PIPEROXAN Drug Info Ki = 95 nM [533545]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol Drug Info Ki = 78 nM [534531]
SK&F-64139 Drug Info Ki = 21 nM [528403]
Butyl-indol-1-yl-pyridin-4-yl-amine Drug Info IC50 = 630 nM [534087]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine Drug Info Ki = 4100 nM [534195]
2,3-Dihydro-1H-isoindole Drug Info Ki = 820 nM [534195]
Ethyl-indol-1-yl-pyridin-4-yl-amine Drug Info IC50 = 110 nM [534087]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 2800 nM [525507]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine Drug Info IC50 = 500 nM [534087]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene Drug Info Ki = 4600 nM [534195]
SNAP-5150 Drug Info Ki = 324 nM [525611]
WB-4101 Drug Info Ki = 200 nM [533545]
GNF-PF-2857 Drug Info Ki = 1700 nM [528472]
GNF-PF-3878 Drug Info Ki = 37 nM [528472]
1,2,3,4-tetrahydroisoquinoline Drug Info Ki = 350 nM [528403]
GNF-PF-3427 Drug Info Ki = 28 nM [528472]
C-(6-Methoxy-naphthalen-1-yl)-methylamine Drug Info Ki = 4600 nM [534531]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info IC50 = 330 nM [534087]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 840 nM [534195]
5-Aminomethyl-naphthalen-2-ol Drug Info Ki = 2100 nM [534531]
TRYPTOLINE Drug Info Ki = 710 nM [526918]
Indol-1-yl-pyridin-4-yl-amine Drug Info IC50 = 8 nM [534087]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 520 nM [534195]
C-Naphthalen-1-yl-methylamine Drug Info Ki = 1600 nM [534531]
METHYLNORADRENALINE Drug Info Ki = 7.7 nM [533545]
S-34324 Drug Info Ki = 19 nM [527481]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info IC50 = 2500 nM [534087]
Indol-1-yl-methyl-pyridin-4-yl-amine Drug Info IC50 = 24 nM [534087]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine Drug Info Ki = 2600 nM [534195]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 6200 nM [534195]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine Drug Info Ki = 11000 nM [534195]
2-BFi Drug Info Ki = 1900 nM [525733]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine Drug Info Ki = 16000 nM [534195]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol Drug Info Ki = 6600 nM [525507]
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 400 nM [534315]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 8840 nM [526918]
A-80426 Drug Info Ki = 2.1 nM [527481]
TRAMAZOLINE Drug Info Ki = 4.2 nM [533545]
(+/-)-nantenine Drug Info Ki = 181 nM [530558]
1,2,3,4-Tetrahydro-isoquinolin-7-ol Drug Info Ki = 2200 nM [534531]
RX-821002 Drug Info Ki = 0.36 nM [533375]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 2400 nM [534315]
MAZAPERTINE Drug Info Ki = 17 nM [533800]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline Drug Info IC50 = 130 nM [534719]
SK&F-104078 Drug Info Ki = 64 nM [533682]
INDORAMIN Drug Info Ki = 476 nM [533682]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 4700 nM [527952]
References
Ref 527365J Med Chem. 2005 Jan 13;48(1):134-40.3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
Ref 529632J Med Chem. 2008 Sep 11;51(17):5423-30. Epub 2008 Aug 7.The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 533805J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
Ref 526994Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 533805J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 525611Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.Design and synthesis of novel dihydropyridine alpha-1a antagonists.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 534467J Med Chem. 1997 Sep 12;40(19):3014-24.Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".
Ref 534128J Med Chem. 1996 Mar 15;39(6):1193-5.Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.
Ref 533406J Med Chem. 1986 Aug;29(8):1394-8.4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Ref 533545J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 528403J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamineN-methyltransferase.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 525507J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 525611Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.Design and synthesis of novel dihydropyridine alpha-1a antagonists.
Ref 533545J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
Ref 528472J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Ref 528472J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Ref 528403J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamineN-methyltransferase.
Ref 528472J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 533545J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
Ref 527481J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534087J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 525733Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7.Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
Ref 534195J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Ref 525507J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 527481J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Ref 533545J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 534531J Med Chem. 1997 Dec 5;40(25):3997-4005.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.
Ref 533375J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 533800J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Ref 534719J Med Chem. 1998 Oct 8;41(21):4165-70.N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.
Ref 533682J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Ref 533682J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.

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