Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T92609 Target Info
Target Name Adrenergic receptor alpha-1A (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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Target Type Successful Target
Gene Name ADRA1A
Biochemical Class GPCR rhodopsin
UniProt ID
ADA1A_HUMAN
Co-Targets of This Target  Top
Co-Target Name Adrenergic receptor alpha-1D (ADRA1D) Successful Target
UniProt ID ADA1D_HUMAN
Gene Name 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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Representative Drug(s) Tamsulosin Drug Info Ki = 0.058 nM Click to Show More [1]
2 NAFTOPIDIL Drug Info Ki = 1.202 nM [4]
3 SILODOSIN Drug Info Ki = 1.995 nM [5]
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) Tamsulosin Drug Info EC50 = 0.13 nM Click to Show More [2]
2 SILODOSIN Drug Info Ki = 19.95 nM [5]
3 NAFTOPIDIL Drug Info Ki = 19.95 nM [4]
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) Tamsulosin Drug Info Ki = 0.28 nM [3]
Co-Target Name 5-HT 1A receptor (HTR1A) Successful Target
UniProt ID 5HT1A_HUMAN
Gene Name HTR1A
Synonyms
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) Tamsulosin Drug Info Ki = 0.79 nM [3]
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 [6]
2 MEDETOMIDINE Drug Info EC50 = 3 nM [6]
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) Tamsulosin Drug Info Ki = 7.9 nM [1]
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) Tamsulosin Drug Info Ki = 13 nM [3]
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) Tamsulosin Drug Info Ki = 13.4 nM [1]
Co-Target Name Norepinephrine transporter (NET) Successful Target
UniProt ID SC6A2_HUMAN
Gene Name SLC6A2
Synonyms
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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Representative Drug(s) Besipirdine Drug Info IC50 = 430 nM [7]
Co-Target Name 5-HT 7 receptor (HTR7) Clinical trial Target
UniProt ID 5HT7R_HUMAN
Gene Name HTR7
Synonyms
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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Representative Drug(s) Tamsulosin Drug Info Ki = 84 nM [3]
References  Top
REF 1 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 2 Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as alpha. Bioorg Med Chem. 2016 Nov 1;24(21):5582-91.
REF 3 Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists. J Med Chem. 2000 Jun 1;43(11):2183-95.
REF 4 Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on alpha. Bioorg Med Chem Lett. 2018 Feb 15;28(4):547-51.
REF 5 Pharmacological options in the treatment of benign prostatic hyperplasia. J Med Chem. 1997 Apr 25;40(9):1293-315.
REF 6 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 7 Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeu... J Med Chem. 1996 Jan 19;39(2):570-81.

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