Co-Target(s) Information
| 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 | |||||
| Co-Targets of This Target | Top | |||||
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| 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 | Ketotifen | Drug Info | Ki = 15.85 nM | [3] | ||
| 3 | Promethazine | 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 | Ketotifen | 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 | Ketotifen | 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) | Promethazine | 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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