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 | |||||
REF 1 | alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a ... J Med Chem. 2000 Mar 9;43(5):765-8. | ||||
REF 2 | Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6. | ||||
REF 3 | 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 an... Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62. | ||||
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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