Target Information
| Target General Information | Top | |||||
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| Target ID |
T83813
(Former ID: TTDS00105)
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| Target Name |
5-HT 2C receptor (HTR2C)
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| 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
Click to Show/Hide
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| Gene Name |
HTR2C
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 5 Target-related Diseases | + | ||||
| 1 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 2 | Migraine [ICD-11: 8A80] | |||||
| 3 | Obesity [ICD-11: 5B80-5B81] | |||||
| 4 | Pain [ICD-11: MG30-MG3Z] | |||||
| 5 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
| Function |
Functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T83COK | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Lorcaserin | Drug Info | Approved | Obesity | [2], [3] | |
| 2 | Metergolin | Drug Info | Approved | Hyperprolactinaemia | [4] | |
| 3 | Methysergide | Drug Info | Approved | Migraine | [5], [6] | |
| 4 | Mirtazapine | Drug Info | Approved | Depression | [7], [8] | |
| 5 | Nefazodone | Drug Info | Approved | Major depressive disorder | [4] | |
| 6 | Tramadol | Drug Info | Approved | Pain | [9], [10] | |
| Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
| 1 | Eltoprazine | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [11] | |
| 2 | M100907 | Drug Info | Phase 3 | Sleep-wake disorder | [12] | |
| 3 | SR46349B | Drug Info | Phase 3 | Schizophrenia | [13] | |
| 4 | ATHX-105 | Drug Info | Phase 2 | Obesity | [14] | |
| 5 | Nuplazid | Drug Info | Phase 2 | Alzheimer disease | [15] | |
| 6 | PRX00933 | Drug Info | Phase 2 | Diabetic complication | [16] | |
| 7 | Puerarin | Drug Info | Phase 2 | Alcohol dependence | [17] | |
| 8 | Vabicaserin | Drug Info | Phase 2 | Psychotic disorder | [18] | |
| 9 | Tedatioxetine | Drug Info | Phase 1 | Major depressive disorder | [19] | |
| Discontinued Drug(s) | [+] 8 Discontinued Drugs | + | ||||
| 1 | Deramciclane | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [20], [21] | |
| 2 | Ritanserin | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [22], [23] | |
| 3 | MCPP | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
| 4 | R-1065 | Drug Info | Discontinued in Phase 1 | Obesity | [25] | |
| 5 | SB-247853 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [26] | |
| 6 | ICI-169369 | Drug Info | Terminated | Anxiety disorder | [27], [28] | |
| 7 | Org-37684 | Drug Info | Terminated | Anxiety disorder | [29], [30] | |
| 8 | SDZ-SER-082 | Drug Info | Terminated | Neurological disorder | [31], [32] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 56 Agonist drugs | + | ||||
| 1 | Lorcaserin | Drug Info | [33], [34] | |||
| 2 | ATHX-105 | Drug Info | [46] | |||
| 3 | Nuplazid | Drug Info | [47] | |||
| 4 | PRX00933 | Drug Info | [16] | |||
| 5 | Aryl piperazine derivative 10 | Drug Info | [52] | |||
| 6 | Aryl piperazine derivative 8 | Drug Info | [52] | |||
| 7 | Aryl piperazine derivative 9 | Drug Info | [52] | |||
| 8 | Benzazepine derivative 1 | Drug Info | [52] | |||
| 9 | Benzazepine derivative 2 | Drug Info | [52] | |||
| 10 | Benzazepine derivative 3 | Drug Info | [52] | |||
| 11 | Benzazepine derivative 4 | Drug Info | [52] | |||
| 12 | Benzazepine derivative 5 | Drug Info | [52] | |||
| 13 | Benzazepine derivative 6 | Drug Info | [52] | |||
| 14 | Chromene derivative 1 | Drug Info | [52] | |||
| 15 | Heteroaryl-azepine derivative 1 | Drug Info | [52] | |||
| 16 | Heteroaryl-azepine derivative 10 | Drug Info | [52] | |||
| 17 | Heteroaryl-azepine derivative 11 | Drug Info | [52] | |||
| 18 | Heteroaryl-azepine derivative 12 | Drug Info | [52] | |||
| 19 | Heteroaryl-azepine derivative 13 | Drug Info | [52] | |||
| 20 | Heteroaryl-azepine derivative 14 | Drug Info | [52] | |||
| 21 | Heteroaryl-azepine derivative 15 | Drug Info | [52] | |||
| 22 | Heteroaryl-azepine derivative 2 | Drug Info | [52] | |||
| 23 | Heteroaryl-azepine derivative 3 | Drug Info | [52] | |||
| 24 | Heteroaryl-azepine derivative 4 | Drug Info | [52] | |||
| 25 | Heteroaryl-azepine derivative 5 | Drug Info | [52] | |||
| 26 | Heteroaryl-azepine derivative 6 | Drug Info | [52] | |||
| 27 | Heteroaryl-azepine derivative 7 | Drug Info | [52] | |||
| 28 | Heteroaryl-azepine derivative 8 | Drug Info | [52] | |||
| 29 | Heteroaryl-azepine derivative 9 | Drug Info | [52] | |||
| 30 | PMID26609882-Compound-83 | Drug Info | [52] | |||
| 31 | Quinoline derivative 2 | Drug Info | [52] | |||
| 32 | Tricyclic pyrrolidine derivative 1 | Drug Info | [52] | |||
| 33 | Tricyclic pyrrolidine derivative 2 | Drug Info | [52] | |||
| 34 | Tricyclic pyrrolidine derivative 3 | Drug Info | [52] | |||
| 35 | Tricyclic pyrrolidine derivative 4 | Drug Info | [52] | |||
| 36 | MCPP | Drug Info | [60], [4] | |||
| 37 | R-1065 | Drug Info | [61] | |||
| 38 | SB-247853 | Drug Info | [62], [4] | |||
| 39 | Org-37684 | Drug Info | [67] | |||
| 40 | 5-CT | Drug Info | [78] | |||
| 41 | AL-37350A | Drug Info | [81] | |||
| 42 | alpha-methyl-5-HT | Drug Info | [82] | |||
| 43 | BRL-15572 | Drug Info | [84] | |||
| 44 | BW723C86 | Drug Info | [86] | |||
| 45 | CP-809101 | Drug Info | [88] | |||
| 46 | CSC-500297 | Drug Info | [88] | |||
| 47 | m-chlorophenylpiperazine | Drug Info | [93] | |||
| 48 | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | [94] | |||
| 49 | Org 12962 | Drug Info | [35] | |||
| 50 | SB 216641 | Drug Info | [84] | |||
| 51 | SB 243213 | Drug Info | [106] | |||
| 52 | TFMPP | Drug Info | [78] | |||
| 53 | TQ-1017 | Drug Info | [4] | |||
| 54 | WAY-163909 | Drug Info | [110] | |||
| 55 | [125I]DOI | Drug Info | [82] | |||
| 56 | [3H]LSD | Drug Info | [88] | |||
| Antagonist | [+] 29 Antagonist drugs | + | ||||
| 1 | Metergolin | Drug Info | [35] | |||
| 2 | Methysergide | Drug Info | [1], [36], [37], [38] | |||
| 3 | Mirtazapine | Drug Info | [39], [40] | |||
| 4 | Nefazodone | Drug Info | [40], [41] | |||
| 5 | Eltoprazine | Drug Info | [43] | |||
| 6 | PMID26609882-Compound-58 | Drug Info | [52] | |||
| 7 | Pyrimidine derivative 23 | Drug Info | [52] | |||
| 8 | Pyrimidine derivative 24 | Drug Info | [52] | |||
| 9 | Pyrimidine derivative 25 | Drug Info | [52] | |||
| 10 | Pyrimidine derivative 26 | Drug Info | [52] | |||
| 11 | Pyrimidine derivative 27 | Drug Info | [52] | |||
| 12 | Pyrimidine derivative 28 | Drug Info | [52] | |||
| 13 | Pyrimidine derivative 29 | Drug Info | [52] | |||
| 14 | Ritanserin | Drug Info | [56], [57], [58], [59] | |||
| 15 | LY53857 | Drug Info | [38], [64], [65], [66] | |||
| 16 | BVT 933 | Drug Info | [85] | |||
| 17 | cyamemazine | Drug Info | [89] | |||
| 18 | EGIS-7625 | Drug Info | [90] | |||
| 19 | FR260010 | Drug Info | [91] | |||
| 20 | LY334362 | Drug Info | [92] | |||
| 21 | MPDT | Drug Info | [97] | |||
| 22 | norfluoxetine | Drug Info | [99] | |||
| 23 | SB 204741 | Drug Info | [35] | |||
| 24 | SB 215505 | Drug Info | [103] | |||
| 25 | SB 221284 | Drug Info | [35] | |||
| 26 | SB 228357 | Drug Info | [104] | |||
| 27 | SB 242084 | Drug Info | [105] | |||
| 28 | spiramide | Drug Info | [35] | |||
| 29 | [3H]mesulergine | Drug Info | [82] | |||
| Modulator | [+] 9 Modulator drugs | + | ||||
| 1 | Tramadol | Drug Info | [42] | |||
| 2 | SR46349B | Drug Info | [45] | |||
| 3 | Puerarin | Drug Info | [48] | |||
| 4 | Vabicaserin | Drug Info | [49], [50] | |||
| 5 | Tedatioxetine | Drug Info | [51] | |||
| 6 | Deramciclane | Drug Info | [53], [54], [55] | |||
| 7 | ICI-169369 | Drug Info | [63] | |||
| 8 | SDZ-SER-082 | Drug Info | [69] | |||
| 9 | MK-212 | Drug Info | [95], [96] | |||
| Inhibitor | [+] 77 Inhibitor drugs | + | ||||
| 1 | M100907 | Drug Info | [44] | |||
| 2 | Ro-60-0175 | Drug Info | [68] | |||
| 3 | (+/-)-nantenine | Drug Info | [70] | |||
| 4 | (2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine | Drug Info | [68] | |||
| 5 | (2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | [68] | |||
| 6 | (2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | [68] | |||
| 7 | (2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine | Drug Info | [68] | |||
| 8 | (E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine | Drug Info | [71] | |||
| 9 | (R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 10 | (R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 11 | (R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 12 | (R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 13 | (R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 14 | (S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [72] | |||
| 15 | 1-((R)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [73] | |||
| 16 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [73] | |||
| 17 | 1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol | Drug Info | [73] | |||
| 18 | 1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol | Drug Info | [73] | |||
| 19 | 1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol | Drug Info | [73] | |||
| 20 | 1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol | Drug Info | [73] | |||
| 21 | 1-(2-aminoethyl)-1H-indazol-6-ol | Drug Info | [73] | |||
| 22 | 1-(2-Dimethylamino-ethyl)-1H-indol-4-ol | Drug Info | [74] | |||
| 23 | 1-(piperazin-1-yl)isoquinoline | Drug Info | [75] | |||
| 24 | 1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol | Drug Info | [74] | |||
| 25 | 2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | [73] | |||
| 26 | 2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline | Drug Info | [75] | |||
| 27 | 3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | [73] | |||
| 28 | 3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol | Drug Info | [74] | |||
| 29 | 3-(2-Dimethylamino-ethyl)-1H-indol-6-ol | Drug Info | [74] | |||
| 30 | 3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol | Drug Info | [74] | |||
| 31 | 3-(2-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | [74] | |||
| 32 | 3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol | Drug Info | [74] | |||
| 33 | 3-(3-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | [74] | |||
| 34 | 3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol | Drug Info | [74] | |||
| 35 | 3-Dimethylaminomethyl-1H-indol-4-ol | Drug Info | [74] | |||
| 36 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [76] | |||
| 37 | 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine | Drug Info | [75] | |||
| 38 | 4-(piperazin-1-yl)furo[3,2-c]pyridine | Drug Info | [75] | |||
| 39 | 4-(piperazin-1-yl)thieno[2,3-d]pyrimidine | Drug Info | [75] | |||
| 40 | 4-(piperazin-1-yl)thieno[3,2-c]pyridine | Drug Info | [75] | |||
| 41 | 4-(piperazin-1-yl)thieno[3,2-d]pyrimidine | Drug Info | [75] | |||
| 42 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
| 43 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
| 44 | 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
| 45 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
| 46 | 5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | [72] | |||
| 47 | 5-MEO-DMT | Drug Info | [73] | |||
| 48 | 6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine | Drug Info | [79] | |||
| 49 | 6-(piperazin-1-yl)-9-propyl-9H-purine | Drug Info | [75] | |||
| 50 | 6-bromo-2'-de-N-methylaplysinopsin | Drug Info | [80] | |||
| 51 | 6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine | Drug Info | [75] | |||
| 52 | 6-bromoaplysinopsin | Drug Info | [80] | |||
| 53 | 6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | [72] | |||
| 54 | 6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine | Drug Info | [75] | |||
| 55 | 7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine | Drug Info | [79] | |||
| 56 | 7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine | Drug Info | [79] | |||
| 57 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
| 58 | Aplysinopsin | Drug Info | [72] | |||
| 59 | BARETTIN | Drug Info | [83] | |||
| 60 | CHLOROPHENYLPIPERAZINE | Drug Info | [87] | |||
| 61 | Cyclo[(6-bromotryptophan)arginine] | Drug Info | [83] | |||
| 62 | N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide | Drug Info | [98] | |||
| 63 | N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | [72] | |||
| 64 | N-3'-ethylaplysinopsin | Drug Info | [80] | |||
| 65 | OCTOCLOTHEPIN | Drug Info | [100] | |||
| 66 | PG-01037 | Drug Info | [101] | |||
| 67 | RS-102,221 | Drug Info | [102] | |||
| 68 | SB-271046 | Drug Info | [107] | |||
| 69 | SEROTONIN | Drug Info | [83] | |||
| 70 | VER-2692 | Drug Info | [108] | |||
| 71 | VER-3323 | Drug Info | [109] | |||
| 72 | VER-5384 | Drug Info | [109] | |||
| 73 | VER-5593 | Drug Info | [109] | |||
| 74 | WAY-208466 | Drug Info | [111] | |||
| 75 | WAY-466 | Drug Info | [112] | |||
| 76 | YM-348 | Drug Info | [79] | |||
| 77 | [2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | [74] | |||
| 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: Lorcaserin | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the 5HT2C receptor (INI isoform) bound to lorcaserin | PDB:8DPF | ||||
| Method | Electron microscopy | Resolution | 2.84 Å | Mutation | Yes | [113] |
| PDB Sequence |
SIVIIIIMTI
68 GGNILVIMAV78 SMEKKLHNAT88 NYFLMSLAIA98 DMLVGLLVMP108 LSLLAILYDY 118 VWLCPVWISL133 DVLFSTASIM143 HLCAISLDRY153 VAIRNPIEHS163 RFNSRTKAIM 173 KIAIVWAISI183 GVSVPIPVIG193 LRDEEKVFVN203 TCVLNDPNFV215 LIGSFVAFFI 225 PLTIMVITYC235 LTIYVLRRQA245 LMMQAINNER307 KASKVLGIVF317 FVFLIMWCPF 327 FITNILSVLC337 ECNQKLMEKL349 LNVFVWIGYV359 CSGINPLVYT369 LFNKIYRRAF 379 SNYL
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Ergotamine | Ligand Info | |||||
| Structure Description | Crystal structure of 5-HT2C in complex with ergotamine | PDB:6BQG | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | Yes | [114] |
| PDB Sequence |
GGRFKFPDGV
52 QNWPALSIVI62 IIIMTIGGNI72 LVIMAVSMEK82 KLHNATNYFL92 MSLAIADMLV 102 GLLVMPLSLL112 AILYDYVWPL122 PRYLCPVWIS132 LDVLFSTASI142 MHLCAISLDR 152 YVAIRNPIEH162 NSRTKAIMKI175 AIVWAISIGV185 SVPIPVIGLR195 DEEKVFVNNT 205 TCVLNDPNFV215 LIGSFVAFFI225 PLTIMVITYC235 LTIYVLRRQA245 ADLEDNWETL 1010 NDNLKVIEKA1020 DNAAQVKDAL1030 TKMRAAALDA1040 QKAMKDFRHG1064 FDILVGQIDD 1074 ALKLANEGKV1084 KEAQAAAEQL1094 KTTRNAYIQK1104 YLQAINNERK308 ASKVLGIVFF 318 VFLIMWCPFF328 ITNILSVLCE338 KSCNQKLMEK348 LLNVFVWIGY358 VNSGINPLVY 368 TLFNKIYRRA378 FSNYLRCN
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TRP130
4.114
ASP134
2.679
VAL135
3.622
SER138
3.352
THR139
2.807
ILE142
4.811
VAL185
4.531
CYS207
4.230
VAL208
3.654
LEU209
2.721
ASN210
4.708
PHE214
4.163
VAL215
3.995
GLY218
3.579
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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 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 Pathway Affiliation
Biological Network Descriptors
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| 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 | ||
| Gap junction | hsa04540 | Affiliated Target |
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| Class: Cellular Processes => Cellular community - eukaryotes | Pathway Hierarchy | ||
| Serotonergic synapse | hsa04726 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Inflammatory mediator regulation of TRP channels | hsa04750 | Affiliated Target |
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| Class: Organismal Systems => Sensory system | Pathway Hierarchy | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 7.50E-06 |
|---|---|---|---|---|---|
| Closeness centrality | 1.96E-01 | Radiality | 1.34E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 3.55E+01 | Topological coefficient | 5.23E-01 | 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 | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Gap junction | |||||
| 4 | Serotonergic synapse | |||||
| 5 | Inflammatory mediator regulation of TRP channels | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | 5HT2 type receptor mediated signaling pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Serotonin receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| WikiPathways | [+] 6 WikiPathways | + | ||||
| 1 | Serotonin Receptor 2 and ELK-SRF/GATA4 signaling | |||||
| 2 | Monoamine GPCRs | |||||
| 3 | GPCRs, Class A Rhodopsin-like | |||||
| 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 | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
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