Target Validation Information
Target ID T53381
Target Name Alpha-1D adrenergic receptor
Target Type
Successful
Drug Potency against Target Imidazolidin-2-ylidene-o-tolyl-amine Drug Info Ki = 2500 nM
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine Drug Info Ki = 11000 nM
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol Drug Info Ki = 6700 nM [526729]
1-(2-Chloro-phenyl)-piperazine Drug Info Ki = 710 nM [528039]
BP-897 Drug Info Ki = 33 nM [526696]
UH-301 Drug Info Ki = 6080 nM [534363]
AGN-192172 Drug Info Ki = 8900 nM
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarin Drug Info IC50 = 10550 nM [527848]
RWJ-68157 Drug Info Ki = 505 nM [525785]
Sunepitron Drug Info Ki = 35 nM [528210]
CORYNANTHEINE Drug Info Ki = 253 nM [533638]
(+/-)-nantenine Drug Info Ki = 340 nM [530558]
1-(2-Methoxy-phenyl)-piperazine Drug Info Ki = 3508 nM [528039]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info Ki = 73 nM [534467]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 5800 nM [526618]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 57 nM [534160]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole Drug Info Ki = 55 nM [534160]
SNAP-5089 Drug Info Ki = 1047 nM [533638]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 11000 nM [534315]
Alfuzosin Drug Info IC50 = 35 nM [553212]
BMY-7378 Drug Info Ki = 1.6 nM [527512]
SNAP-8719 Drug Info Ki = 1.3 nM [527512]
RX-821002 Drug Info Ki = 27 nM [533375]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info Ki = 3200 nM [526618]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 1490 nM [526778]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 3100 nM [526778]
NIGULDIPINE Drug Info Ki = 191 nM [533638]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info Ki = 343 nM [525720]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info Ki = 17000 nM
AGN-193080 Drug Info Ki = 470 nM
MAZAPERTINE Drug Info Ki = 0.2 nM [533800]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info Ki = 490 nM [533509]
1-(pyridin-2-yl)piperazine Drug Info Ki = 2400 nM [533509]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki = 40 nM [531079]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole Drug Info Ki = 574 nM [534160]
SK&F-104078 Drug Info Ki = 33 nM [533638]
SK&F-105854 Drug Info Ki = 72 nM [533638]
SK&F-104856 Drug Info Ki = 1.6 nM [533638]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole Drug Info Ki = 1734 nM [534160]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol Drug Info Ki = 15000 nM [526729]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info Ki = 536 nM [533805]
INDORAMIN Drug Info Ki = 611 nM [533682]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 6000 nM [534315]
MEDETOMIDINE Drug Info Ki = 1102 nM [533805]
WB-4101 Drug Info Ki = 0.35 nM [533682]
RWJ-69736 Drug Info Ki = 80 nM [525785]
RWJ-25730 Drug Info Ki = 8.2 nM [533800]
SK&F-106686 Drug Info Ki = 1.2 nM [533638]
ISOCLOZAPINE Drug Info IC50 = 64 nM [534532]
Siramesine Drug Info IC50 = 330 nM [533739]
FLUANISONE Drug Info Ki = 0.87 nM [533378]
TIOSPIRONE Drug Info Ki = 1.5 nM [534093]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info Ki = 4000 nM [533509]
RWJ-38063 Drug Info Ki = 372 nM [525785]
OCTOCLOTHEPIN Drug Info Ki = 0.77 nM [531171]
SK&F-86466 Drug Info Ki = 126 nM [533638]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 387 nM [534160]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info Ki = 7400 nM [526729]
LEVONORDEFRIN Drug Info Ki = 9221 nM [534160]
Terazosin Drug Info IC50 = 2.5 nM [553110]
References
Ref 526729J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
Ref 528039J Med Chem. 1991 Jun;34(6):1850-4.Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
Ref 526696J Med Chem. 2003 Aug 28;46(18):3822-39.Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.
Ref 534363J Med Chem. 1997 Apr 11;40(8):1252-7.N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
Ref 527848Bioorg Med Chem Lett. 2006 Jan 15;16(2):257-61. Epub 2005 Nov 3.Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids.
Ref 525785Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
Ref 528210J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
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 528039J Med Chem. 1991 Jun;34(6):1850-4.Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
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 526618Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 553212Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol. 1993 Aug;109(4):1282-9.
Ref 527512J Med Chem. 2005 Apr 21;48(8):3076-9.Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
Ref 527512J Med Chem. 2005 Apr 21;48(8):3076-9.Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
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 526618Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Ref 526778J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Ref 526778J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 525720J Med Chem. 2000 Mar 9;43(5):765-8.alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
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 533509J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Ref 533509J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 526729J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic 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 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 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
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 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 525785Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
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 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 534532J Med Chem. 1997 Dec 5;40(25):4146-53.Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Ref 533739J Med Chem. 1995 May 26;38(11):1998-2008.Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Ref 533378J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
Ref 534093J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Ref 533509J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Ref 525785Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
Ref 531171J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 526729J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 553110The alpha adrenergic binding properties of terazosin in the human prostate adenoma and canine brain. J Urol. 1988 Sep;140(3):664-7.

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