Target Validation Information
TTD ID T53381
Target Name Adrenergic receptor alpha-1D (ADRA1D)
Type of Target
Successful
Drug Potency against Target Alfuzosin Drug Info IC50 = 35 nM [29]
Terazosin Drug Info IC50 = 2.5 nM [28]
Drug Info Ki = 3508 nM [9]
Drug Info Ki = 574 nM [23]
Drug Info IC50 = 330 nM [19]
Drug Info Ki = 372 nM [2]
(+/-)-nantenine Drug Info Ki = 340 nM [11]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 6000 nM [24]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 11000 nM [24]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info Ki = 4000 nM [16]
1-(2-Chloro-phenyl)-piperazine Drug Info Ki = 710 nM [9]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info Ki = 490 nM [16]
1-(pyridin-2-yl)piperazine Drug Info Ki = 2400 nM [16]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 5800 nM [3]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 387 nM [23]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 57 nM [23]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info Ki = 536 nM [21]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole Drug Info Ki = 1734 nM [23]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole Drug Info Ki = 55 nM [23]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info Ki = 3200 nM [3]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol Drug Info Ki = 15000 nM [5]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki = 40 nM [12]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol Drug Info Ki = 6700 nM [5]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info Ki = 73 nM [26]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info Ki = 343 nM [1]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info Ki = 7400 nM [5]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 1490 nM [6]
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarin Drug Info IC50 = 10550 nM [8]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 3100 nM [6]
AGN-192172 Drug Info Ki = 8900 nM
AGN-193080 Drug Info Ki = 470 nM
BMY-7378 Drug Info Ki = 1.6 nM [7]
BP-897 Drug Info Ki = 33 nM [4]
CORYNANTHEINE Drug Info Ki = 253 nM [17]
FLUANISONE Drug Info Ki = 0.87 nM [15]
Imidazolidin-2-ylidene-o-tolyl-amine Drug Info Ki = 2500 nM
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine Drug Info Ki = 11000 nM
INDORAMIN Drug Info Ki = 611 nM [18]
ISOCLOZAPINE Drug Info IC50 = 64 nM [27]
LEVONORDEFRIN Drug Info Ki = 9221 nM [23]
MAZAPERTINE Drug Info Ki = 0.2 nM [20]
MEDETOMIDINE Drug Info Ki = 1102 nM [21]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info Ki = 17000 nM
NIGULDIPINE Drug Info Ki = 191 nM [17]
OCTOCLOTHEPIN Drug Info Ki = 0.77 nM [13]
RWJ-25730 Drug Info Ki = 8.2 nM [20]
RWJ-68157 Drug Info Ki = 505 nM [2]
RWJ-69736 Drug Info Ki = 80 nM [2]
SK&F-104078 Drug Info Ki = 33 nM [17]
SK&F-104856 Drug Info Ki = 1.6 nM [17]
SK&F-105854 Drug Info Ki = 72 nM [17]
SK&F-106686 Drug Info Ki = 1.2 nM [17]
SK&F-86466 Drug Info Ki = 126 nM [17]
SNAP-5089 Drug Info Ki = 1047 nM [17]
SNAP-8719 Drug Info Ki = 1.3 nM [7]
Sunepitron Drug Info Ki = 35 nM [10]
TIOSPIRONE Drug Info Ki = 1.5 nM [22]
UH-301 Drug Info Ki = 6080 nM [25]
WB-4101 Drug Info Ki = 0.35 nM [18]
[3H]RX821002 Drug Info Ki = 27 nM [14]
References
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REF 2 Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.
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REF 4 Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of... J Med Chem. 2003 Aug 28;46(18):3822-39.
REF 5 Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic rece... J Med Chem. 1992 Mar 20;35(6):1009-18.
REF 6 Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. J Med Chem. 1992 Oct 16;35(21):3845-57.
REF 7 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 ... J Med Chem. 2005 Apr 21;48(8):3076-9.
REF 8 Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids. Bioorg Med Chem Lett. 2006 Jan 15;16(2):257-61.
REF 9 Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. J Med Chem. 1991 Jun;34(6):1850-4.
REF 10 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
REF 11 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 12 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 13 Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.
REF 14 Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. J Med Chem. 1986 Oct;29(10):2000-3.
REF 15 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. J Med Chem. 1987 Nov;30(11):2099-104.
REF 16 Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. J Med Chem. 1984 Sep;27(9):1182-5.
REF 17 Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
REF 18 Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44.
REF 19 Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995 May 26;38(11):1998-2008.
REF 20 A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
REF 21 A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
REF 22 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
REF 23 Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene deriva... J Med Chem. 1996 Jul 19;39(15):3001-13.
REF 24 Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. J Med Chem. 1997 Jan 3;40(1):18-23.
REF 25 N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. J Med Chem. 1997 Apr 11;40(8):1252-7.
REF 26 Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potent... J Med Chem. 1997 Sep 12;40(19):3014-24.
REF 27 Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. J Med Chem. 1997 Dec 5;40(25):4146-53.
REF 28 The alpha adrenergic binding properties of terazosin in the human prostate adenoma and canine brain. J Urol. 1988 Sep;140(3):664-7.
REF 29 Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol. 1993 Aug;109(4):1282-9.

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