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 526729 | J 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 528039 | J 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 526696 | J 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 534363 | J 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 527848 | Bioorg 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 525785 | Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. | ||||
Ref 528210 | J 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 533638 | J 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 530558 | Bioorg 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 528039 | J 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 534467 | J 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 526618 | Bioorg 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 534160 | J 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 534160 | J 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 533638 | J 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 534315 | J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. | ||||
Ref 553212 | Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol. 1993 Aug;109(4):1282-9. | ||||
Ref 527512 | J 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 527512 | J 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 533375 | J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. | ||||
Ref 526618 | Bioorg 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 526778 | J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. | ||||
Ref 526778 | J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. | ||||
Ref 533638 | J 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 525720 | J 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 533800 | J 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 533509 | J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. | ||||
Ref 533509 | J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. | ||||
Ref 531079 | J 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 534160 | J 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 533638 | J 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 533638 | J 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 533638 | J 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 534160 | J 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 526729 | J 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 533805 | J 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 533682 | J 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 534315 | J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. | ||||
Ref 533805 | J 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 533682 | J 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 525785 | Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. | ||||
Ref 533800 | J 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 533638 | J 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 534532 | J 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 533739 | J 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 533378 | J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. | ||||
Ref 534093 | J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. | ||||
Ref 533509 | J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. | ||||
Ref 525785 | Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. | ||||
Ref 531171 | J 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 533638 | J 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 534160 | J 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 526729 | J 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 534160 | J 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 553110 | The 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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