Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T81183 Target Info
Target Name Adrenergic receptor Alpha-1 (ADRA1)
Synonyms
Alpha1-adrenoceptor; Alpha(1)-adrenoceptor
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class GPCR rhodopsin
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name 5-HT 1D receptor (HTR1D) Successful Target
UniProt ID 5HT1D_HUMAN
Gene Name HTR1D
Synonyms
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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Representative Drug(s) Prazosin Drug Info Ki = 0.33 nM Click to Show More [1]
2 Ergotamine Drug Info Ki = 0.8 nM [2]
Co-Target Name 5-HT 1B receptor (HTR1B) Successful Target
UniProt ID 5HT1B_HUMAN
Gene Name HTR1B
Synonyms
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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Representative Drug(s) Ergotamine Drug Info Ki = 2.1 nM [3]
Co-Target Name Quinone reductase 2 (NQO2) Successful Target
UniProt ID NQO2_HUMAN
Gene Name NQO2
Synonyms
Quinone oxidoreductase 2; Qui reductase 2; QR2; NRH:quinone oxidoreductase 2; NRH:qui oxidoreductase 2; NQO2; NAD(P)H qui oxidoreductase 2
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Representative Drug(s) Prazosin Drug Info IC50 = 7.8 nM [4]
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) Prazosin Drug Info Ki ~ 10 nM Click to Show More [5]
2 Urapidil Drug Info Ki = 213 nM [9]
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) Prazosin Drug Info Ki = 13 nM [6]
Co-Target Name 5-HT 5A receptor (HTR5A) Successful Target
UniProt ID 5HT5A_HUMAN
Gene Name HTR5A
Synonyms
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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Representative Drug(s) Ergotamine Drug Info Ki = 14 nM [7]
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) Prazosin Drug Info Ki = 24 nM [6]
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) Prazosin Drug Info Ki = 34 nM Click to Show More [8]
2 Prazosin Drug Info Ki = 34 nM [8]
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) Prazosin Drug Info Ki = 210 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) Carvedilol Drug Info IC50 = 350 nM [10]
References  Top
REF 1 Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. J Med Chem. 1998 Dec 17;41(26):5320-33.
REF 2 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 3 A novel potential therapeutic avenue for autism: design, synthesis and pharmacophore generation of SSRIs with dual action. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6714-23.
REF 4 Design and synthesis of naphthalenic derivatives as new ligands at the melatonin binding site MT3. Eur J Med Chem. 2011 May;46(5):1622-9.
REF 5 Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. J Med Chem. 2001 Jul 19;44(15):2403-10.
REF 6 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 7 CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. Bioorg Med Chem. 2011 Oct 1;19(19):5756-62.
REF 8 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 9 Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2039-2049.
REF 10 The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4771-7.

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