Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T77913 Target Info
Target Name Histamine H1 receptor (H1R)
Synonyms
HH1R; H1R
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Target Type Successful Target
Gene Name HRH1
Biochemical Class GPCR rhodopsin
UniProt ID
HRH1_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) Cyproheptadine Drug Info Ki = 0.46 nM Click to Show More [1]
2 Drug Info Ki = 15.85 nM [3]
3 Drug Info IC50 = 23 nM [6]
4 Hydroxyzine Drug Info Ki = 50 nM [9]
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) Cyproheptadine Drug Info Ki = 11 nM Click to Show More [2]
2 Drug Info Ki = 199.53 nM [3]
3 Azelastine Drug Info Ki = 501.19 nM [4]
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) Azelastine Drug Info Ki = 19.95 nM Click to Show More [4]
2 Doxepin Drug Info Ki = 25.3 nM [7]
3 Drug Info Ki = 31.62 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) Ethopropazine Drug Info Ki = 20 nM [5]
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) Dimethindene Drug Info Ki = 44.67 nM [8]
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) Azelastine Drug Info Ki = 50.12 nM [10]
Co-Target Name Adrenergic receptor alpha-1A (ADRA1A) Successful Target
UniProt ID ADA1A_HUMAN
Gene Name 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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Representative Drug(s) Azelastine Drug Info Ki = 50.12 nM [11]
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) Oxatomide Drug Info Ki = 62.7 nM [12]
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) Loratadine Drug Info IC50 < 100 nM Click to Show More [13]
2 Azelastine Drug Info IC50 = 1000 nM [15]
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) Drug Info IC50 = 100 nM Click to Show More [6]
2 Cyproheptadine Drug Info Ki = 112 nM [2]
3 Hydroxyzine Drug Info Ki = 378 nM [9]
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) Fexofenadine Drug Info IC50 ~ 100 nM Click to Show More [14]
2 Azelastine Drug Info IC50 = 100 nM [15]
3 Loratadine Drug Info IC50 = 169.82 nM [16]
4 Mizolastine Drug Info IC50 = 350 nM [18]
5 Brompheniramine Drug Info IC50 = 891.25 nM [20]
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) Dimethindene Drug Info Ki = 190.55 nM [8]
Co-Target Name Acetylcholinesterase (AChE) Successful Target
UniProt ID ACES_HUMAN
Gene Name ACHE
Synonyms
YT; N-ACHE; ARACHE
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Representative Drug(s) Ethopropazine Drug Info IC50 = 260 nM [17]
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) Dimethindene Drug Info Ki = 263.03 nM [8]
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) Cyproheptadine Drug Info Ki = 290 nM [2]
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) Dimethindene Drug Info Ki = 407.38 nM [8]
Co-Target Name Histamine H2 receptor (H2R) Successful Target
UniProt ID HRH2_HUMAN
Gene Name HRH2
Synonyms
Histamine receptor 2; HH2R; Gastric receptor I
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Representative Drug(s) Ergotidine Drug Info EC50 = 463 nM [19]
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) Dimethindene Drug Info Ki = 794.33 nM [8]
Co-Target Name Histamine H4 receptor (H4R) Clinical trial Target
UniProt ID HRH4_HUMAN
Gene Name HRH4
Synonyms
SP9144; Pfi-013; HH4R; H4 receptor; GPRv53; GPCR105; G protein-coupled receptor 105; AXOR35
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Representative Drug(s) Ergotidine Drug Info Ki = 1.6 nM Click to Show More [21]
2 Mepyramine Drug Info Ki < 47 nM [23]
Co-Target Name Histamine H3 receptor (H3R) Clinical trial Target
UniProt ID HRH3_HUMAN
Gene Name HRH3
Synonyms
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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Representative Drug(s) Ergotidine Drug Info EC50 = 2.512 nM Click to Show More [22]
2 Azelastine Drug Info Ki = 147.91 nM [11]
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) Cyproheptadine Drug Info Ki = 50.12 nM [24]
Co-Target Name Pregnane X receptor (NR1I2) Literature-reported Target
UniProt ID NR1I2_HUMAN
Gene Name NR1I2
Synonyms
Steroid and xenobiotic receptor; SXR; PXR; Orphan nuclear receptor PXR; Orphan nuclear receptor PAR1; Nuclear receptor subfamily 1 group I member 2
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Representative Drug(s) Oxatomide Drug Info EC50 = 400 nM [25]
Co-Target Name Multidrug resistance protein 4 (ABCC4) Literature-reported Target
UniProt ID MRP4_HUMAN
Gene Name ABCC4
Synonyms
Multispecific organic anion transporter B; Multidrug resistanceassociated protein 4; MRP/cMOATrelated ABC transporter; MOATB; ATPbinding cassette subfamily C member 4; ABCC4
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Representative Drug(s) Tranilast Drug Info IC50 = 1000 nM [26]
Co-Target Name Histone-lysine N-methyltransferase SETD7 (SETD7) Literature-reported Target
UniProt ID SETD7_HUMAN
Gene Name SETD7
Synonyms
SET9; SET7/9; SET7; SET domain-containing protein 7; Lysine N-methyltransferase 7; KMT7; KIAA1717; Histone H3-K4 methyltransferase SETD7; H3-K4-HMTase SETD7
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Representative Drug(s) Cyproheptadine Drug Info IC50 = 1000 nM [27]
Co-Target Name Brain sodium channel alpha (Types I, II, III) Co-Target
UniProt ID SCN1A_HUMAN; SCN2A_HUMAN; SCN3A_HUMAN
Gene Name SCN1A; SCN2A; SCN3A
Representative Drug(s) Cinnarizine Drug Info IC50 = 440 nM Click to Show More [28]
2 Cyproheptadine Drug Info IC50 = 1000 nM [28]
References  Top
REF 1 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem. 2012 Jun 28;55(12):5749-59.
REF 2 Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA). Bioorg Med Chem Lett. 2004 May 3;14(9):2279-83.
REF 3 Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders. J Med Chem. 2010 Nov 11;53(21):7778-95.
REF 4 Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4914-9.
REF 5 Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. J Med Chem. 2003 Jan 2;46(1):1-4.
REF 6 Polypharmacology-foe or friend? J Med Chem. 2013 Nov 27;56(22):8955-71.
REF 7 Exploring Halogen Bonds in 5-Hydroxytryptamine 2B Receptor-Ligand Interactions. ACS Med Chem Lett. 2018 Oct 1;9(10):1019-24.
REF 8 Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands. Bioorg Med Chem Lett. 2001 May 7;11(9):1241-3.
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 Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. Bioorg Med Chem. 2012 Oct 15;20(20):6097-108.
REF 11 The discovery of quinoline based single-ligand human H 1 and H 3 receptor antagonists. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5855-5859.
REF 12 Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybri... J Med Chem. 2003 Oct 9;46(21):4377-92.
REF 13 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.
REF 14 Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7.
REF 15 The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. J Med Chem. 2011 Apr 14;54(7):2183-95.
REF 16 Support vector machines classification of hERG liabilities based on atom types. Bioorg Med Chem. 2008 Jun 1;16(11):6252-60.
REF 17 Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. J Med Chem. 2014 Oct 9;57(19):8167-79.
REF 18 Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. J Med Chem. 2002 Aug 29;45(18):3844-53.
REF 19 Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist f... J Med Chem. 2003 May 8;46(10):1980-8.
REF 20 Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30.
REF 21 Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5263-6.
REF 22 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H 3 Receptor Agonists with in Vivo Central Nervous System Activity. J Med Chem. 2019 Dec 12;62(23):10848-10866.
REF 23 Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6274-80.
REF 24 Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives. J Med Chem. 2003 Dec 18;46(26):5638-50.
REF 25 Identification of clinically used drugs that activate pregnane X receptors. Drug Metab Dispos. 2011 Jan;39(1):151-9.
REF 26 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
REF 27 Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. J Med Chem. 2016 Apr 28;59(8):3650-60.
REF 28 [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8.

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