Target Information
| Target General Information | Top | |||||
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| Target ID |
T77913
(Former ID: TTDS00086)
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| Target Name |
Histamine H1 receptor (H1R)
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| Synonyms |
HH1R; H1R
Click to Show/Hide
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| Gene Name |
HRH1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 17 Target-related Diseases | + | ||||
| 1 | Allergic/hypersensitivity disorder [ICD-11: 4A80-4A8Z] | |||||
| 2 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
| 3 | Breathing abnormality [ICD-11: MD11] | |||||
| 4 | Conjunctiva disorder [ICD-11: 9A60] | |||||
| 5 | Cough [ICD-11: MD12] | |||||
| 6 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 7 | Episodic vestibular syndrome [ICD-11: AB31] | |||||
| 8 | Headache [ICD-11: 8A80-8A84] | |||||
| 9 | Insomnia [ICD-11: 7A00-7A0Z] | |||||
| 10 | Morning sickness disorder [ICD-11: SC00] | |||||
| 11 | Nasopharyngitis [ICD-11: CA00] | |||||
| 12 | Nausea/vomiting [ICD-11: MD90] | |||||
| 13 | Parkinsonism [ICD-11: 8A00] | |||||
| 14 | Pruritus [ICD-11: EC90] | |||||
| 15 | Rheumatoid arthritis [ICD-11: FA20] | |||||
| 16 | Sleep-wake disorder [ICD-11: 7A00-7B2Z] | |||||
| 17 | Vasomotor/allergic rhinitis [ICD-11: CA08] | |||||
| Function |
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK RILHIRS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A00273 ; BADD_A02979 ; BADD_A04075 | |||||
| HIT2.0 ID | T06N1B | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 54 Approved Drugs | + | ||||
| 1 | (S)-(+)-Dimethindene maleate | Drug Info | Approved | Pruritus | [2] | |
| 2 | Aceprometazine | Drug Info | Approved | Sleep-wake disorder | [3] | |
| 3 | Acrivastine | Drug Info | Approved | Allergic rhinitis | [4] | |
| 4 | Alcaftadine | Drug Info | Approved | Allergic conjunctivitis | [5], [6] | |
| 5 | Antazoline | Drug Info | Approved | Nasal congestion | [7], [8] | |
| 6 | Azatadine | Drug Info | Approved | Allergic rhinitis | [9], [10] | |
| 7 | Azelastine | Drug Info | Approved | Allergic conjunctivitis | [11], [12] | |
| 8 | Bepotastine | Drug Info | Approved | Allergic rhinitis | [12], [13] | |
| 9 | Bromodiphenhydramine | Drug Info | Approved | Hay fever | [14], [15], [16] | |
| 10 | Brompheniramine | Drug Info | Approved | Allergic rhinitis | [17], [18] | |
| 11 | Buclizine | Drug Info | Approved | Nausea | [19], [20] | |
| 12 | Carbinoxamine | Drug Info | Approved | Vasomotor/allergic rhinitis | [16] | |
| 13 | Cetirizine | Drug Info | Approved | Allergic rhinitis | [21], [4] | |
| 14 | Chlophedianol | Drug Info | Approved | Dry cough | [16] | |
| 15 | Chlorpheniramine | Drug Info | Approved | Allergic rhinitis | [22], [23] | |
| 16 | Cinnarizine | Drug Info | Approved | Vertigo meniere disease | [24] | |
| 17 | Clemastine | Drug Info | Approved | Allergic rhinitis | [25], [26] | |
| 18 | Cyclizine | Drug Info | Approved | Nausea | [27], [28] | |
| 19 | Cyproheptadine | Drug Info | Approved | Rhinitis | [16] | |
| 20 | Desloratadine | Drug Info | Approved | Allergic rhinitis | [29], [30] | |
| 21 | Dexbrompheniramine | Drug Info | Approved | Hay fever | [16], [31], [32] | |
| 22 | Dexchlorpheniramine Maleate | Drug Info | Approved | Rhinitis | [16] | |
| 23 | Dimenhydrinate | Drug Info | Approved | Nausea | [33] | |
| 24 | Dimethindene | Drug Info | Approved | Respiratory allergy | [2], [16] | |
| 25 | Diphenhydramine | Drug Info | Approved | Meniere disease | [16] | |
| 26 | Diphenylpyraline | Drug Info | Approved | Allergic rhinitis | [34], [35] | |
| 27 | Doxepin | Drug Info | Approved | Depression | [36], [37] | |
| 28 | Doxylamine | Drug Info | Approved | Morning sickness | [38], [39] | |
| 29 | Emedastine | Drug Info | Approved | Allergic conjunctivitis | [40], [12] | |
| 30 | Epinastine | Drug Info | Approved | Allergic conjunctivitis | [41], [12] | |
| 31 | Ergotidine | Drug Info | Approved | Respiratory allergy | [16], [42], [43] | |
| 32 | Ethopropazine | Drug Info | Approved | Parkinson disease | [44], [45] | |
| 33 | Fexofenadine | Drug Info | Approved | Allergic rhinitis | [46], [4] | |
| 34 | Hydroxyzine | Drug Info | Approved | Anxiety disorder | [47], [48] | |
| 35 | Ketotifen | Drug Info | Approved | Allergic conjunctivitis | [49], [12] | |
| 36 | Levocabastine | Drug Info | Approved | Allergic conjunctivitis | [50], [12] | |
| 37 | Levocetirizine dihydrochloride | Drug Info | Approved | Allergic rhinitis | [51], [52] | |
| 38 | Loratadine | Drug Info | Approved | Allergy | [53], [30] | |
| 39 | Mepyramine | Drug Info | Approved | Allergy | [54], [55] | |
| 40 | Mepyramine maleate | Drug Info | Approved | Headache | [56], [57] | |
| 41 | Mequitazine | Drug Info | Approved | Allergic rhinitis | [58] | |
| 42 | Methdilazine | Drug Info | Approved | Allergic rhinitis | [59], [60] | |
| 43 | Mizolastine | Drug Info | Approved | Allergic rhinitis | [61] | |
| 44 | Olopatadine | Drug Info | Approved | Allergic conjunctivitis | [62], [12] | |
| 45 | Oxatomide | Drug Info | Approved | Hay fever | [56] | |
| 46 | Pemirolast | Drug Info | Approved | Allergic conjunctivitis | [12], [16], [63] | |
| 47 | Phenindamine | Drug Info | Approved | Common cold | [64] | |
| 48 | Pheniramine | Drug Info | Approved | Hay fever | [65], [12] | |
| 49 | Promethazine | Drug Info | Approved | Nausea | [66], [67] | |
| 50 | Propiomazine | Drug Info | Approved | Insomnia | [16], [68], [69] | |
| 51 | Tranilast | Drug Info | Approved | Ocular allergy | [70], [12] | |
| 52 | Trimeprazine | Drug Info | Approved | Allergic rhinitis | [71], [72] | |
| 53 | Tripelennamine | Drug Info | Approved | Hypersensitivity | [16] | |
| 54 | Triprolidine | Drug Info | Approved | Hay fever | [73], [74] | |
| Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
| 1 | AC-170 | Drug Info | Phase 3 | Allergic conjunctivitis | [75] | |
| 2 | Carebastine | Drug Info | Phase 3 | Ocular allergy | [12] | |
| 3 | E-4716 | Drug Info | Phase 2 | Respiratory disease | [76] | |
| 4 | LY-2624803 | Drug Info | Phase 2 | Insomnia | [77] | |
| 5 | Noberastine | Drug Info | Phase 2 | Asthma | [78] | |
| 6 | OBE-101 | Drug Info | Phase 2 | Obesity | [79] | |
| 7 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [80] | |
| 8 | UCB-35440 | Drug Info | Phase 2 | Rhinitis | [81] | |
| 9 | Vapitadine | Drug Info | Phase 2 | Allergic skin disorder | [82] | |
| Discontinued Drug(s) | [+] 11 Discontinued Drugs | + | ||||
| 1 | Astemizole | Drug Info | Withdrawn from market | Allergic rhinitis | [83], [4] | |
| 2 | Terfenadine | Drug Info | Withdrawn from market | Allergy | [84], [4] | |
| 3 | GSK835726 | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [85] | |
| 4 | HSR-609 | Drug Info | Discontinued in Phase 2 | Rhinitis | [86] | |
| 5 | Mequitamium iodide | Drug Info | Discontinued in Phase 2 | Asthma | [87] | |
| 6 | ReN-1869 | Drug Info | Discontinued in Phase 2 | Pain | [88] | |
| 7 | SUN-1334H | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [89] | |
| 8 | AZD-1744 | Drug Info | Discontinued in Phase 1 | Asthma | [90] | |
| 9 | GSK1004723 | Drug Info | Discontinued in Phase 1 | Allergic rhinitis | [91] | |
| 10 | KA-398 | Drug Info | Terminated | Asthma | [92] | |
| 11 | Selenotifen | Drug Info | Terminated | Asthma | [93] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Antagonist | [+] 71 Antagonist drugs | + | ||||
| 1 | (S)-(+)-Dimethindene maleate | Drug Info | [2], [57], [94], [95] | |||
| 2 | Aceprometazine | Drug Info | [96] | |||
| 3 | Acrivastine | Drug Info | [97], [98] | |||
| 4 | Alcaftadine | Drug Info | [6] | |||
| 5 | Antazoline | Drug Info | [98], [99], [100], [101] | |||
| 6 | Azatadine | Drug Info | [102] | |||
| 7 | Azelastine | Drug Info | [56], [103] | |||
| 8 | Bepotastine | Drug Info | [104] | |||
| 9 | Bromodiphenhydramine | Drug Info | [105] | |||
| 10 | Brompheniramine | Drug Info | [106] | |||
| 11 | Buclizine | Drug Info | [107] | |||
| 12 | Carbinoxamine | Drug Info | [108] | |||
| 13 | Cetirizine | Drug Info | [109], [110] | |||
| 14 | Chlophedianol | Drug Info | [111] | |||
| 15 | Chlorpheniramine | Drug Info | [56], [112], [57] | |||
| 16 | Cinnarizine | Drug Info | [113], [114] | |||
| 17 | Clemastine | Drug Info | [1], [115] | |||
| 18 | Cyclizine | Drug Info | [116], [117], [118] | |||
| 19 | Cyproheptadine | Drug Info | [119], [120] | |||
| 20 | Desloratadine | Drug Info | [121], [122] | |||
| 21 | Dexbrompheniramine | Drug Info | [123] | |||
| 22 | Dimenhydrinate | Drug Info | [125], [126] | |||
| 23 | Dimethindene | Drug Info | [2], [57], [94], [95] | |||
| 24 | Diphenhydramine | Drug Info | [56], [127] | |||
| 25 | Diphenylpyraline | Drug Info | [128] | |||
| 26 | Doxylamine | Drug Info | [131], [132] | |||
| 27 | Emedastine | Drug Info | [133] | |||
| 28 | Epinastine | Drug Info | [134] | |||
| 29 | Fexofenadine | Drug Info | [122], [110] | |||
| 30 | Hydroxyzine | Drug Info | [135], [136] | |||
| 31 | Ketotifen | Drug Info | [56], [137] | |||
| 32 | Levocabastine | Drug Info | [138], [139] | |||
| 33 | Levocetirizine dihydrochloride | Drug Info | [122], [56], [137] | |||
| 34 | Loratadine | Drug Info | [140], [141], [142] | |||
| 35 | Mepyramine | Drug Info | [55], [143], [109] | |||
| 36 | Mepyramine maleate | Drug Info | [55], [56], [57], [109], [143] | |||
| 37 | Mequitazine | Drug Info | [144] | |||
| 38 | Methdilazine | Drug Info | [145] | |||
| 39 | Mizolastine | Drug Info | [146] | |||
| 40 | Olopatadine | Drug Info | [12] | |||
| 41 | Oxatomide | Drug Info | [56], [139] | |||
| 42 | Pemirolast | Drug Info | [147] | |||
| 43 | Phenindamine | Drug Info | [148] | |||
| 44 | Pheniramine | Drug Info | [149] | |||
| 45 | Promethazine | Drug Info | [56], [57] | |||
| 46 | Propiomazine | Drug Info | [150] | |||
| 47 | Tranilast | Drug Info | [12] | |||
| 48 | Trimeprazine | Drug Info | [151] | |||
| 49 | Tripelennamine | Drug Info | [152], [153], [154], [155] | |||
| 50 | Triprolidine | Drug Info | [156] | |||
| 51 | AC-170 | Drug Info | [158] | |||
| 52 | Carebastine | Drug Info | [12] | |||
| 53 | Noberastine | Drug Info | [160] | |||
| 54 | Vapitadine | Drug Info | [164] | |||
| 55 | Astemizole | Drug Info | [166], [99] | |||
| 56 | Terfenadine | Drug Info | [167], [141] | |||
| 57 | GSK835726 | Drug Info | [169] | |||
| 58 | HSR-609 | Drug Info | [170], [16] | |||
| 59 | ReN-1869 | Drug Info | [172] | |||
| 60 | SUN-1334H | Drug Info | [173] | |||
| 61 | GSK1004723 | Drug Info | [169] | |||
| 62 | (+)-cis-H2-PAT | Drug Info | [177] | |||
| 63 | (+)-trans-H2-PAT | Drug Info | [177] | |||
| 64 | (+/-)-cis-H2-PAT | Drug Info | [177] | |||
| 65 | (-)-trans-H2-PAT | Drug Info | [177] | |||
| 66 | (S)-cetirizine | Drug Info | [178] | |||
| 67 | 9-OH-risperidone | Drug Info | [185] | |||
| 68 | arpromidine | Drug Info | [181] | |||
| 69 | BU-E 47 | Drug Info | [181] | |||
| 70 | Hydroxyclemastine | Drug Info | [1], [115] | |||
| 71 | impromidine | Drug Info | [189] | |||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | Dexchlorpheniramine Maleate | Drug Info | [124] | |||
| 2 | Ethopropazine | Drug Info | [124] | |||
| 3 | E-4716 | Drug Info | [76] | |||
| 4 | LY-2624803 | Drug Info | [159] | |||
| 5 | OBE-101 | Drug Info | [161] | |||
| 6 | UCB-35440 | Drug Info | [163] | |||
| 7 | Norastemizole | Drug Info | [168] | |||
| 8 | Mequitamium iodide | Drug Info | [171] | |||
| 9 | AZD-1744 | Drug Info | [174] | |||
| 10 | KA-398 | Drug Info | [175] | |||
| 11 | Selenotifen | Drug Info | [176] | |||
| Inhibitor | [+] 26 Inhibitor drugs | + | ||||
| 1 | Doxepin | Drug Info | [129], [130] | |||
| 2 | RUPATADINE | Drug Info | [157] | |||
| 3 | Citalopram derivative 1 | Drug Info | [165] | |||
| 4 | 1-(4-p-Tolyl-butyl)-piperidine | Drug Info | [179] | |||
| 5 | 1-[(Furan-2(5H)-one)-4-methyl]-desloratadine | Drug Info | [180] | |||
| 6 | 2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine | Drug Info | [182] | |||
| 7 | 3,3-diphenylpropan-1-amine | Drug Info | [182] | |||
| 8 | 4,4-Diphenylbutan-1-amine | Drug Info | [182] | |||
| 9 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [183] | |||
| 10 | 9-(2-aminoethyl)-9,10-dihydroanthracene | Drug Info | [182] | |||
| 11 | 9-(2-aminopropyl)-9,10-dihydroanthracene | Drug Info | [182] | |||
| 12 | 9-(Aminomethyl)-9,10-dihydroanthracene | Drug Info | [182] | |||
| 13 | 9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine | Drug Info | [186] | |||
| 14 | DIMEBOLIN | Drug Info | [187] | |||
| 15 | Diphenyl(piperidin-4-yl)methanol | Drug Info | [179] | |||
| 16 | KF-A6 | Drug Info | [190] | |||
| 17 | MDL-28163 | Drug Info | [157] | |||
| 18 | N,N-dimethyl-2,2-diphenylethanamine | Drug Info | [182] | |||
| 19 | N,N-Dimethyl-3,3-diphenylpropan-1-amine | Drug Info | [182] | |||
| 20 | N,N-dimethyl-4,4-diphenylbutan-1-amine | Drug Info | [182] | |||
| 21 | N-methyl-3,3-diphenylpropan-1-amine | Drug Info | [182] | |||
| 22 | N-methyl-4,4-diphenylbutan-1-amine | Drug Info | [182] | |||
| 23 | OCTOCLOTHEPIN | Drug Info | [191] | |||
| 24 | R-226161 | Drug Info | [192] | |||
| 25 | R-dimethindene | Drug Info | [193] | |||
| 26 | VUF-10148 | Drug Info | [194] | |||
| Agonist | [+] 15 Agonist drugs | + | ||||
| 1 | Ergotidine | Drug Info | [43] | |||
| 2 | 2-(2-thiazolyl)ethanamine | Drug Info | [181] | |||
| 3 | 2-(3-bromophenyl)histamine | Drug Info | [181] | |||
| 4 | 2-(3-chlorophenyl)histamine | Drug Info | [181] | |||
| 5 | 2-(3-iodophenyl)histamine | Drug Info | [181] | |||
| 6 | 2-pyridylethylamine | Drug Info | [178] | |||
| 7 | 8R-Lisuride | Drug Info | [184] | |||
| 8 | dimethylhistaprodifen | Drug Info | [181] | |||
| 9 | histaprodifen | Drug Info | [188] | |||
| 10 | methylhistaprodifen | Drug Info | [181] | |||
| 11 | oxo-arpromidine | Drug Info | [189] | |||
| 12 | UR-PG131A | Drug Info | [189] | |||
| 13 | UR-PG146 | Drug Info | [189] | |||
| 14 | UR-PG153 | Drug Info | [189] | |||
| 15 | UR-PG55B | Drug Info | [189] | |||
| Partial agonist | [+] 1 Partial agonist drugs | + | ||||
| 1 | RP5063 | Drug Info | [162] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Ergotidine | Ligand Info | |||||
| Structure Description | Cryo-EM structure of histamine H1 receptor Gq complex | PDB:7DFL | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | No | [195] |
| PDB Sequence |
MPLVVVLSTI
37 CLVTVGLNLL47 VLYAVRSERK57 LHTVGNLYIV67 SLSVADLIVG77 AVVMPMNILY 87 LLMSKWSLGR97 PLCLFWLSMD107 YVASTASIFS117 VFILCIDRYR127 SVQQPLRYLK 137 YRTKTRASAT147 ILGAWFLSFL157 WVIPILGWNH167 FMQQTSVRRE177 DKCETDFYDV 187 TWFKVMTAII197 NFYLPTLLML207 WFYAKIYKAV217 RQHCLHMNRE410 RKAAKQLGFI 420 MAAFILCWIP430 YFIFFMVIAF440 CKNCCNEHLH450 MFTIWLGYIN460 STLNPLIYPL 470 CNENFKKTFK480 RILHI
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| Ligand Name: Doxepin | Ligand Info | |||||
| Structure Description | Structure of the human histamine H1 receptor in complex with doxepin | PDB:3RZE | ||||
| Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | Yes | [196] |
| PDB Sequence |
MPLVVVLSTI
37 CLVTVGLNLL47 VLYAVRSERK57 LHTVGNLYIV67 SLSVADLIVG77 AVVMPMNILY 87 LLMSKWSLGR97 PLCLFWLSMD107 YVASTASIFS117 VFILCIDRYR127 SVQQPLRYLK 137 YRTKTRASAT147 ILGAWFLSFL157 WVIPILGWNH167 RREDKCETDF184 YDVTWFKVMT 194 AIINFYLPTL204 LMLWFYAKIY214 KAVRQHCNIF1004 EMLRIDEGLR1014 LKIYKDTEGY 1024 YTIGIGHLLT1034 KSPSLNAAKS1044 ELDKAIGRNT1054 NGVITKDEAE1064 KLFNQDVDAA 1074 VRGILRNAKL1084 KPVYDSLDAV1094 RRAALINMVF1104 QMGETGVAGF1114 TNSLRMLQQK 1124 RWDEAAVNLA1134 KSRWYNQTPN1144 RAKRVITTFR1154 TGTWDAYLHM407 NRERKAAKQL 417 GFIMAAFILC427 WIPYFIFFMV437 IAFCKNCCNE447 HLHMFTIWLG457 YINSTLNPLI 467 YPLCNENFKK477 TFKRILHI
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Calcium signaling pathway | hsa04020 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Inflammatory mediator regulation of TRP channels | hsa04750 | Affiliated Target |
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| Class: Organismal Systems => Sensory system | Pathway Hierarchy | ||
| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.86E-01 | Radiality | 1.31E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 5.20E+01 | Topological coefficient | 1.00E+00 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Inflammatory mediator regulation of TRP channels | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Histamine H1 receptor mediated signaling pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Histamine receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| WikiPathways | [+] 6 WikiPathways | + | ||||
| 1 | Monoamine GPCRs | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | IL-4 Signaling Pathway | |||||
| 4 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 5 | GPCR ligand binding | |||||
| 6 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
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| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017601. | |||||
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| REF 23 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070797. | |||||
| REF 24 | Drug information of Cinnarizine, 2008. eduDrugs. | |||||
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| REF 26 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 073283. | |||||
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| REF 28 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009495. | |||||
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| REF 32 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089116. | |||||
| REF 33 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040519. | |||||
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| REF 35 | Drug information of Diphenylpyraline, 2008. eduDrugs. | |||||
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