Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T34429 Target Info
Target Name Neuronal acetylcholine receptor alpha-7 (CHRNA7)
Synonyms
Nicotinic acetylcholine receptor subunit alpha 7; Nicotinic acetylcholine receptor alpha7; CHRNA7; Alpha7 nicotinic receptor; Alpha7 nAChR; Alpha-7 nAChR; Alpha(7) nicotinic receptor
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Target Type Successful Target
Gene Name CHRNA7
Biochemical Class Neurotransmitter receptor
UniProt ID
ACHA7_HUMAN
Co-Targets of This Target  Top
Co-Target Name 5-HT 2A receptor (HTR2A) Successful Target
UniProt ID 5HT2A_HUMAN
Gene Name HTR2A
Synonyms
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Representative Drug(s) Ziprasidone Drug Info Ki = 0.08 nM [1]
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 Click to Show More [2]
2 GTS-21 Drug Info Ki = 51 nM [8]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name HTR2C
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) Ziprasidone Drug Info Ki = 0.55 nM [3]
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) Ziprasidone Drug Info Ki = 0.8 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) Ziprasidone Drug Info Ki = 1.585 nM [5]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) Ziprasidone Drug Info Ki = 1.585 nM [5]
Co-Target Name Histamine H1 receptor (H1R) Successful Target
UniProt ID HRH1_HUMAN
Gene Name HRH1
Synonyms
HH1R; H1R
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Representative Drug(s) Ziprasidone Drug Info Ki = 5.3 nM [6]
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) Ziprasidone Drug Info Ki = 6.31 nM [5]
Co-Target Name Dopamine D1 receptor (D1R) Successful Target
UniProt ID DRD1_HUMAN
Gene Name DRD1
Synonyms
D(1A) dopamine receptor
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Representative Drug(s) Ziprasidone Drug Info Ki = 9.5 nM [3]
Co-Target Name Dopamine D4 receptor (D4R) Successful Target
UniProt ID DRD4_HUMAN
Gene Name DRD4
Synonyms
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Representative Drug(s) Ziprasidone Drug Info Ki = 32 nM [7]
Co-Target Name Serotonin transporter (SERT) Successful Target
UniProt ID SC6A4_HUMAN
Gene Name SLC6A4
Synonyms
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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Representative Drug(s) Ziprasidone Drug Info Ki = 53 nM [7]
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) Ziprasidone Drug Info IC50 = 120.23 nM [9]
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 [10]
Co-Target Name 5-HT 3A receptor (HTR3A) Successful Target
UniProt ID 5HT3A_HUMAN
Gene Name HTR3A
Synonyms
Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
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Representative Drug(s) EVP-6124 Drug Info IC50 = 299 nM [11]
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) Ziprasidone Drug Info Ki = 390 nM Click to Show More [3]
2 Ziprasidone Drug Info Ki = 390 nM [3]
Co-Target Name 5-HT 3 receptor (5HT3R) Successful Target
UniProt ID 5HT3A_HUMAN; 5HT3B_HUMAN; 5HT3C_HUMAN; 5HT3D_HUMAN; 5HT3E_HUMAN
Gene Name NO-GeName
Synonyms
5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3
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Representative Drug(s) Ziprasidone Drug Info Ki = 398.11 nM [5]
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) Ziprasidone Drug Info Ki = 5 nM [4]
Co-Target Name 5-HT 6 receptor (HTR6) Clinical trial Target
UniProt ID 5HT6R_HUMAN
Gene Name HTR6
Synonyms
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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Representative Drug(s) Ziprasidone Drug Info Ki = 20 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) Ziprasidone Drug Info Ki = 1.9 nM [3]
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 [12]
References  Top
REF 1 1-Aminoindanes as novel motif with potential atypical antipsychotic properties. Bioorg Med Chem Lett. 2008 Jan 15;18(2):489-93.
REF 2 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 3 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
REF 4 Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects. Eur J Med Chem. 2018 Feb 10;145:790-804.
REF 5 Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. J Med Chem. 2007 Oct 18;50(21):5103-8.
REF 6 Selective optimization of side activities: another way for drug discovery. J Med Chem. 2004 Mar 11;47(6):1303-14.
REF 7 Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. Bioorg Med Chem. 2008 Aug 1;16(15):7291-301.
REF 8 Discovery of novel alpha7 nicotinic acetylcholine receptor ligands via pharmacophoric and docking studies of benzylidene anabaseine analogs. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1179-86.
REF 9 Support vector machines classification of hERG liabilities based on atom types. Bioorg Med Chem. 2008 Jun 1;16(11):6252-60.
REF 10 (+)-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 11 Discovery and development of alpha7 nicotinic acetylcholine receptor modulators. J Med Chem. 2011 Dec 8;54(23):7943-61.
REF 12 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.

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