Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T55815 Target Info
Target Name Neuronal acetylcholine receptor alpha-2 (CHRNA2)
Synonyms
CHRNA2
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Target Type Successful Target
Gene Name CHRNA2
Biochemical Class Neurotransmitter receptor
UniProt ID
ACHA2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2) Successful Target
UniProt ID ACHA4_HUMAN-ACHB2_HUMAN
Gene Name CHRNA4-CHRNB2
Synonyms
CHRN; nAChR
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Representative Drug(s) CYTISINE Drug Info Ki = 0.23 nM [1]
Co-Target Name Muscarinic acetylcholine receptor M4 (CHRM4) Successful Target
UniProt ID ACM4_HUMAN
Gene Name CHRM4
Synonyms
M4 receptor; CHRM4
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Representative Drug(s) Carbachol Drug Info IC50 = 0.4 nM [2]
Co-Target Name Opioid receptor mu (MOP) Successful Target
UniProt ID OPRM_HUMAN
Gene Name OPRM1
Synonyms
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Representative Drug(s) Levallorphan Drug Info Ki = 0.48 nM Click to Show More [3]
2 Levallorphan Drug Info IC50 = 0.67 nM [4]
Co-Target Name Opioid receptor kappa (OPRK1) Successful Target
UniProt ID OPRK_HUMAN
Gene Name OPRK1
Synonyms
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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Representative Drug(s) Levallorphan Drug Info IC50 = 0.67 nM [4]
Co-Target Name Muscarinic acetylcholine receptor M2 (CHRM2) Successful Target
UniProt ID ACM2_HUMAN
Gene Name CHRM2
Synonyms
M2 receptor; CHRM2
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Representative Drug(s) Carbachol Drug Info IC50 = 3.8 nM Click to Show More [2]
2 Carbachol Drug Info EC50 = 190 nM [8]
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) Carbachol Drug Info EC50 = 70 nM Click to Show More [5]
2 Carbachol Drug Info EC50 = 190 nM [8]
Co-Target Name Muscarinic acetylcholine receptor (CHRM) Successful Target
UniProt ID ACM1_HUMAN; ACM2_HUMAN; ACM3_HUMAN; ACM4_HUMAN; ACM5_HUMAN
Gene Name NO-GeName
Representative Drug(s) Carbachol Drug Info EC50 = 100 nM [6]
Co-Target Name Muscarinic acetylcholine receptor M1 (CHRM1) Successful Target
UniProt ID ACM1_HUMAN
Gene Name CHRM1
Synonyms
M1 receptor
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Representative Drug(s) Carbachol Drug Info Ki = 170 nM [7]
Co-Target Name Neuronal acetylcholine receptor alpha-3/beta-4 (CHRNA3/B4) Successful Target
UniProt ID ACHA3_HUMAN-ACHB4_HUMAN
Gene Name CHRNA3-CHRNB4
Synonyms
Neuronal acetylcholine receptor
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Representative Drug(s) CYTISINE Drug Info Ki = 280 nM [9]
Co-Target Name Muscarinic acetylcholine receptor M5 (CHRM5) Successful Target
UniProt ID ACM5_HUMAN
Gene Name CHRM5
Synonyms
CHRM5
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Representative Drug(s) Carbachol Drug Info EC50 = 360 nM [10]
Co-Target Name Acetylcholine receptor alpha-1/beta-1/delta/gamma (CHRNA1/CHRNA1/CHRND/CHRNG) Co-Target
UniProt ID ACHA_HUMAN-ACHB_HUMAN-ACHD_HUMAN-ACHG_HUMAN
Gene Name CHRNA1-CHRNB1-CHRND-CHRNG
Representative Drug(s) CYTISINE Drug Info EC50 = 11 nM [11]
Co-Target Name Muscarinic acetylcholine receptor M1/M5 fusion protein (CHRM1-CHRM5) Co-Target
UniProt ID ACM1_HUMAN-ACM5_HUMAN
Gene Name CHRM1-CHRM5
Representative Drug(s) Carbachol Drug Info EC50 = 1000 nM [12]
References  Top
REF 1 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.
REF 2 Identification and characterization of m4 selective muscarinic antagonists. Bioorg Med Chem Lett. 1998 Aug 4;8(15):1991-6.
REF 3 Generation of novel radiolabeled opiates through site-selective iodination. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4001-4.
REF 4 Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. J Med Chem. 1989 Feb;32(2):418-21.
REF 5 A novel class of conformationally restricted heterocyclic muscarinic agonists. J Med Chem. 1986 Jun;29(6):1004-9.
REF 6 Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. J Med Chem. 1990 Dec;33(12):3182-9.
REF 7 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. J Med Chem. 2000 Jun 29;43(13):2514-22.
REF 8 Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity. J Med Chem. 1994 Nov 25;37(24):4085-99.
REF 9 (+)-Laburnamine, a natural selective ligand and partial agonist for the alpha42 nicotinic receptor subtype. J Nat Prod. 2013 Apr 26;76(4):727-31.
REF 10 Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. J Med Chem. 1995 Jun 9;38(12):2188-95.
REF 11 Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1221-4.
REF 12 Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the binding and activity at muscarinic receptor subtypes and chimeras. J Med Chem. 2006 Dec 14;49(25):7518-31.

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