Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T52522 Target Info
Target Name Adrenergic receptor beta-2 (ADRB2)
Synonyms
Beta-2 adrenoreceptor; Beta-2 adrenoceptor; Beta-2 adrenergic receptor; B2AR; ADRB2R
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Target Type Successful Target
Gene Name ADRB2
Biochemical Class GPCR rhodopsin
UniProt ID
ADRB2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Adrenergic receptor beta-1 (ADRB1) Successful Target
UniProt ID ADRB1_HUMAN
Gene Name ADRB1
Synonyms
Beta-1 adrenoreceptor; Beta-1 adrenoceptor; Beta-1 adrenergic receptor; B1AR; ADRB1R
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Representative Drug(s) Isoproterenol Drug Info EC50 = 0.084 nM Click to Show More [1]
2 Formoterol Drug Info EC50 = 12.59 nM [6]
3 Indacaterol Drug Info Ki = 91 nM [9]
4 Salmeterol Drug Info EC50 = 199.53 nM [10]
5 L-796568 Drug Info IC50 = 1000 nM [4]
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) ICI 118,551 Drug Info IC50 = 0.5 nM [2]
Co-Target Name Adrenergic receptor beta-3 (ADRB3) Successful Target
UniProt ID ADRB3_HUMAN
Gene Name ADRB3
Synonyms
Beta3AR; Beta3-AR; Beta-3 adrenoreceptor; Beta-3 adrenoceptor; Beta-3 adrenergic receptor; B3AR; ADRB3R
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Representative Drug(s) Isoproterenol Drug Info EC50 = 0.97 nM Click to Show More [1]
2 L-796568 Drug Info EC50 = 2 nM [4]
3 Formoterol Drug Info EC50 = 25.12 nM [7]
4 Salmeterol Drug Info EC50 = 1000 nM [11]
Co-Target Name Muscarinic acetylcholine receptor M3 (CHRM3) Successful Target
UniProt ID ACM3_HUMAN
Gene Name CHRM3
Synonyms
M3 receptor; CHRM3
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Representative Drug(s) GSK961081 Drug Info IC50 = 1.585 nM [3]
Co-Target Name Cholinesterase (BCHE) Successful Target
UniProt ID CHLE_HUMAN
Gene Name BCHE
Synonyms
Pseudocholinesterase; Choline esterase II; CHE1; Butyrylcholine esterase; Acylcholine acylhydrolase
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Representative Drug(s) Bambuterol Drug Info IC50 = 3 nM [5]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) BUCINDOLOL Drug Info IC50 = 50 nM [8]
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) L-796568 Drug Info IC50 = 220 nM [4]
Co-Target Name HUAMN alpha-1 adrenergic receptor (ADRA1) Literature-reported Target
UniProt ID ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN
Gene Name ADRA1A; ADRA1B; ADRA1D
Synonyms
Alpha-1 adrenoreceptor
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Representative Drug(s) Isoproterenol Drug Info EC50 = 1.5 nM [12]
References  Top
REF 1 Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I. J Med Chem. 2008 Mar 27;51(6):1925-44.
REF 2 Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. Bioorg Med Chem. 2013 May 15;21(10):2764-71.
REF 3 Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). J Med Chem. 2019 Jul 11;62(13):5944-5978.
REF 4 Discovery of Vibegron: A Potent and Selective 3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. J Med Chem. 2016 Jan 28;59(2):609-23.
REF 5 Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease. Eur J Med Chem. 2017 May 26;132:294-309.
REF 6 Discovery of TD-4306, a long-acting beta2-agonist for the treatment of asthma and COPD. Bioorg Med Chem Lett. 2014 Jul 1;24(13):2871-6.
REF 7 The discovery of long-acting saligenin beta? adrenergic receptor agonists incorporating hydantoin or uracil rings. Bioorg Med Chem. 2011 Jul 15;19(14):4192-201.
REF 8 A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3816-20.
REF 9 The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting beta2-adrenoceptor agonist. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4341-7.
REF 10 Hybridization of beta-Adrenergic Agonists and Antagonists Confers G Protein Bias. J Med Chem. 2019 May 23;62(10):5111-5131.
REF 11 Multivalent design of long-acting (2)-adrenoceptor agonists incorporating biarylamines. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2625-30.
REF 12 Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J Med Chem. 1992 Aug 7;35(16):3081-4.

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