Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T53381 Target Info
Target Name Adrenergic receptor alpha-1D (ADRA1D)
Synonyms
Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A
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Target Type Successful Target
Gene Name ADRA1D
Biochemical Class GPCR rhodopsin
UniProt ID
ADA1D_HUMAN
Co-Targets of This Target  Top
Co-Target Name Adrenergic receptor alpha-1B (ADRA1B) Successful Target
UniProt ID ADA1B_HUMAN
Gene Name ADRA1B
Synonyms
Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
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Representative Drug(s) Terazosin Drug Info EC50 = 0.5 nM Click to Show More [1]
2 Doxazosin Drug Info Ki = 0.631 nM [3]
3 Alfuzosin Drug Info Ki = 2.8 nM [6]
Co-Target Name Adrenergic receptor alpha-1A (ADRA1A) Successful Target
UniProt ID ADA1A_HUMAN
Gene Name ADRA1A
Synonyms
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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Representative Drug(s) Doxazosin Drug Info Ki = 0.537 nM Click to Show More [2]
2 Terazosin Drug Info Ki = 2 nM [4]
3 Alfuzosin Drug Info Ki = 8.2 nM [6]
Co-Target Name Dopamine D2 receptor (D2R) Successful Target
UniProt ID DRD2_HUMAN
Gene Name DRD2
Synonyms
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) Armodafinil Drug Info IC50 = 2.1 nM Click to Show More [5]
2 DL-017 Drug Info Ki ~ 50 nM [10]
Co-Target Name Adrenergic receptor Alpha-2 (ADRA2) Successful Target
UniProt ID ADA2A_HUMAN; ADA2B_HUMAN; ADA2C_HUMAN
Gene Name NO-GeName
Synonyms
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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Representative Drug(s) MEDETOMIDINE Drug Info EC50 = 3 nM Click to Show More [7]
2 MEDETOMIDINE Drug Info EC50 = 3 nM [7]
Co-Target Name Acetylcholinesterase (AChE) Successful Target
UniProt ID ACES_HUMAN
Gene Name ACHE
Synonyms
YT; N-ACHE; ARACHE
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Representative Drug(s) Alfuzosin Drug Info IC50 = 18 nM [8]
Co-Target Name Adrenergic receptor alpha-2B (ADRA2B) Successful Target
UniProt ID ADA2B_HUMAN
Gene Name ADRA2B
Synonyms
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) Terazosin Drug Info Ki = 26 nM [9]
Co-Target Name Dopamine D3 receptor (D3R) Successful Target
UniProt ID DRD3_HUMAN
Gene Name DRD3
Synonyms
D(3) dopamine receptor
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Representative Drug(s) DL-017 Drug Info Ki ~ 50 nM [10]
Co-Target Name Adrenergic receptor alpha-2C (ADRA2C) Successful Target
UniProt ID ADA2C_HUMAN
Gene Name ADRA2C
Synonyms
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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Representative Drug(s) Terazosin Drug Info Ki = 78 nM Click to Show More [11]
2 Doxazosin Drug Info Ki = 280 nM [6]
Co-Target Name Opioid receptor sigma 1 (OPRS1) Successful Target
UniProt ID SGMR1_HUMAN
Gene Name SIGMAR1
Synonyms
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) DL-017 Drug Info Ki = 451 nM [10]
Co-Target Name Adrenergic receptor alpha-2A (ADRA2A) Successful Target
UniProt ID ADA2A_HUMAN
Gene Name ADRA2A
Synonyms
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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Representative Drug(s) Terazosin Drug Info Ki = 549.54 nM Click to Show More [12]
2 Doxazosin Drug Info Ki = 729 nM [6]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) Doxazosin Drug Info IC50 = 588.84 nM [13]
Co-Target Name Dopamine transporter (DAT) Successful Target
UniProt ID SC6A3_HUMAN
Gene Name SLC6A3
Synonyms
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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Representative Drug(s) Armodafinil Drug Info Ki = 647 nM [5]
References  Top
REF 1 alpha-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one. Bioorg Med Chem. 2015 May 1;23(9):2104-11.
REF 2 Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity. J Med Chem. 2009 Aug 13;52(15):4951-4.
REF 3 Quinazoline based alpha1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines. Eur J Med Chem. 2017 Aug 18;136:259-69.
REF 4 Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2467-72.
REF 5 Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. J Med Chem. 2016 Dec 8;59(23):10676-10691.
REF 6 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 7 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 8 In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. Bioorg Med Chem. 2018 May 1;26(8):1511-22.
REF 9 Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. J Med Chem. 1995 May 12;38(10):1579-81.
REF 10 Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists. J Med Chem. 1998 Aug 13;41(17):3128-41.
REF 11 Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prostatic hyperplasia. J Med Chem. 1997 Sep 26;40(20):3141-3.
REF 12 Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate. J Med Chem. 1998 Jul 2;41(14):2643-50.
REF 13 Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30.

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