Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameAlpha-1D adrenergic receptor    
Type of TargetSuccessful target    
Drug Potency against TargetTerazosinIC50 = 2.5 nM[1]
AlfuzosinIC50 = 35 nM[2]
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarinIC50 = 10550 nM[3]
WAY-100135IC50 = 1490 nM[4]
SiramesineIC50 = 330 nM[5]
ABANOQUILKi = 0.03 nM[7]
WB-4101Ki = 0.35 nM[7]
FLUANISONEKi = 0.87 nM[10]
SK&F-106686;SK-106686Ki = 1.2 nM[11]
SNAP-8719Ki = 1.3 nM[12]
TIOSPIRONEKi = 1.5 nM[13]
BMY-7378Ki = 1.6 nM[12]
SK&F-104856;SK-104856Ki = 1.6 nM[11]
SNAP-5089Ki = 1047 nM[11]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amineKi = 11000 nM[14]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amineKi = 11000 nM[15]
MEDETOMIDINEKi = 1102 nM[16]
SK&F-86466;SK-86466Ki = 126 nM[11]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazineKi = 1490 nM[17]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diolKi = 15000 nM[18]
N-(5-Bromo-quinoxalin-6-yl)-guanidineKi = 17000 nM[15]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazoleKi = 1734 nM[19]
NIGULDIPINEKi = 191 nM[11]
1-Pyridin-2-yl-piperazineKi = 2400 nM[20]
Imidazolidin-2-ylidene-o-tolyl-amineKi = 2500 nM[15]
RX-821002Ki = 27 nM[21]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazineKi = 3100 nM[17]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinolineKi = 3200 nM[22]
BP-897Ki = 33 nM[23]
SK&F-104078;SK-104078Ki = 33 nM[11]
(+/-)-nantenineKi = 340 nM[24]
4-Benzo[b]thiophen-4-yl-1H-imidazoleKi = 343 nM[25]
sunepitronKi = 35 nM[26]
1-(2-Methoxy-phenyl)-piperazineKi = 3508 nM[27]
RWJ-38063Ki = 372 nM[28]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazoleKi = 387 nM[19]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi = 40 nM[29]
1',2',3',6'-Tetrahydro-[2,4']bipyridinylKi = 4000 nM[20]
AGN-193080Ki = 470 nM[15]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazineKi = 490 nM[20]
RWJ-68157Ki = 505 nM[28]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazoleKi = 536 nM[16]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazoleKi = 55 nM[19]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazoleKi = 57 nM[19]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazoleKi = 574 nM[19]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinolineKi = 5800 nM[22]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amineKi = 6000 nM[14]
UH-301Ki = 6080 nM[4]
INDORAMINKi = 611 nM[7]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diolKi = 6700 nM[18]
1-(2-Chloro-phenyl)-piperazineKi = 710 nM[27]
SK&F-105854;SK-105854Ki = 72 nM[11]
4-(4-Methyl-indan-1-yl)-1H-imidazoleKi = 73 nM[30]
4-Morpholin-2-yl-benzene-1,2-diolKi = 7400 nM[18]
RWJ-25730Ki = 8.2 nM[8]
RWJ-69736Ki = 80 nM[28]
AGN-192172Ki = 8900 nM[15]
Ref 1J Urol. 1988 Sep;140(3):664-7.The alpha adrenergic binding properties of terazosin in the human prostate adenoma and canine brain. To Reference
Ref 2Br J Pharmacol. 1993 Aug;109(4):1282-9.Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. To Reference
Ref 3Bioorg 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. To Reference
Ref 4J 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. To Reference
Ref 5J 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. To Reference
Ref 6J 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. To Reference
Ref 7J 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. To Reference
Ref 8J 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. To Reference
Ref 9J 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 (1)-adrenoceptors. To Reference
Ref 10J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. To Reference
Ref 11J 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. To Reference
Ref 12J 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. To Reference
Ref 13J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. To Reference
Ref 14J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. To Reference
Ref 15Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995) To Reference
Ref 16J 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. To Reference
Ref 17J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. To Reference
Ref 18J 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. To Reference
Ref 19J 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. To Reference
Ref 20J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. To Reference
Ref 21J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. To Reference
Ref 22Bioorg 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. To Reference
Ref 23J 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. To Reference
Ref 24Bioorg 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. To Reference
Ref 25J 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. To Reference
Ref 26J 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. To Reference
Ref 27J 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. To Reference
Ref 28Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. To Reference
Ref 29J 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. To Reference
Ref 30J 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". To Reference


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