Target Information
Target General Information | Top | |||||
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Target ID |
T32060
(Former ID: TTDS00103)
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Target Name |
5-HT 2A receptor (HTR2A)
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Synonyms |
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Gene Name |
HTR2A
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 7 Target-related Diseases | + | ||||
1 | Acute diabete complication [ICD-11: 5A2Y] | |||||
2 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
3 | Cerebral ischaemia [ICD-11: 8B1Z] | |||||
4 | Mood disorder [ICD-11: 6A60-6E23] | |||||
5 | Parkinsonism [ICD-11: 8A00] | |||||
6 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
7 | Schizophrenia [ICD-11: 6A20] | |||||
Function |
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 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 phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV 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 | T64BED |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 9 Approved Drugs | + | ||||
1 | Aniracetam | Drug Info | Approved | Cerebrovascular ischaemia | [2], [3] | |
2 | Flibanserin | Drug Info | Approved | Mood disorder | [4], [5] | |
3 | Iloperidone | Drug Info | Approved | Schizophrenia | [6], [7] | |
4 | lumateperone tosylate | Drug Info | Approved | Schizophrenia | [8] | |
5 | Lurasidone hydrochloride | Drug Info | Approved | Schizophrenia | [9], [10], [11], [12] | |
6 | Metergolin | Drug Info | Approved | Hyperprolactinaemia | [12] | |
7 | Pimavanserin | Drug Info | Approved | Parkinson disease | [13] | |
8 | Sarpogrelate | Drug Info | Approved | Diabetic complication | [14], [15] | |
9 | ZOTEPINE | Drug Info | Approved | Anxiety disorder | [16], [12] | |
Clinical Trial Drug(s) | [+] 22 Clinical Trial Drugs | + | ||||
1 | Blonanserin | Drug Info | Phase 3 | Schizophrenia | [17], [18] | |
2 | ITI-007 | Drug Info | Phase 3 | Insomnia | [19], [20] | |
3 | M100907 | Drug Info | Phase 3 | Sleep-wake disorder | [21] | |
4 | MIN-101 | Drug Info | Phase 3 | Schizophrenia | [22] | |
5 | SR46349B | Drug Info | Phase 3 | Schizophrenia | [18] | |
6 | TNX-102 | Drug Info | Phase 3 | Fibromyalgia | [23] | |
7 | Zicronapine | Drug Info | Phase 3 | Schizophrenia | [24] | |
8 | BVT.28949 | Drug Info | Phase 2 | Glaucoma/ocular hypertension | [25] | |
9 | FKW00GA | Drug Info | Phase 2 | Social phobia | [26] | |
10 | NELOTANSERIN | Drug Info | Phase 2 | Lewy body dementia | [27] | |
11 | Nuplazid | Drug Info | Phase 2 | Alzheimer disease | [28] | |
12 | Ocaperidone | Drug Info | Phase 2 | Schizoaffective disorder | [29], [18], [30] | |
13 | PRUVANSERIN | Drug Info | Phase 2 | Sleep-wake disorder | [31] | |
14 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [32] | |
15 | SYN120 | Drug Info | Phase 2 | Parkinson disease | [33] | |
16 | 1192U90 | Drug Info | Phase 1 | Psychotic disorder | [34] | |
17 | Abaperidone | Drug Info | Phase 1 | Schizophrenia | [35] | |
18 | ATI-9242 | Drug Info | Phase 1 | Schizophrenia | [26] | |
19 | DSP-1200 | Drug Info | Phase 1 | Depression | [26] | |
20 | SKL-10406 | Drug Info | Phase 1 | Major depressive disorder | [36] | |
21 | Temanogrel | Drug Info | Phase 1 | Cardiovascular disease | [37] | |
22 | YKP-1358 | Drug Info | Phase 1 | Schizoaffective disorder | [18] | |
Patented Agent(s) | [+] 3 Patented Agents | + | ||||
1 | PMID30124346-Compound-13TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [38] | |
2 | PMID30124346-Compound-34TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [38] | |
3 | PMID30124346-Compound-LDT8 | Drug Info | Patented | Benign prostatic hyperplasia | [38] | |
Discontinued Drug(s) | [+] 21 Discontinued Drugs | + | ||||
1 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | Withdrawn from market | Addictive disorder | [39], [40] | |
2 | Deramciclane | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [41], [42] | |
3 | Iferanserin-Ventrus | Drug Info | Discontinued in Phase 3 | Hemorrhoids | [43] | |
4 | MDL-11939 | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [44], [45] | |
5 | Ritanserin | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [46], [47] | |
6 | Adatanserin | Drug Info | Discontinued in Phase 2 | Mood disorder | [48] | |
7 | AMESERGIDE | Drug Info | Discontinued in Phase 2 | Mood disorder | [49], [50] | |
8 | FCE-22716 | Drug Info | Discontinued in Phase 2 | Hypertension | [51] | |
9 | SERAZAPINE HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [52] | |
10 | SERGOLEXOLE MALEATE | Drug Info | Discontinued in Phase 2 | Migraine | [53] | |
11 | SL65.0472 | Drug Info | Discontinued in Phase 2 | Cardiovascular disease | [54] | |
12 | YM-992 | Drug Info | Discontinued in Phase 2 | Depression | [55] | |
13 | AM-831 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [56] | |
14 | DUP-734 | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [57] | |
15 | AMPEROZIDE | Drug Info | Terminated | Alcohol dependence | [58] | |
16 | DV-7028 | Drug Info | Terminated | Cardiovascular disease | [59] | |
17 | Fananserin | Drug Info | Terminated | Schizophrenia | [60], [18] | |
18 | GMC-283 | Drug Info | Terminated | Schizophrenia | [18] | |
19 | ICI-169369 | Drug Info | Terminated | Anxiety disorder | [61], [62] | |
20 | R-102444 | Drug Info | Terminated | Pancreatitis | [63] | |
21 | ZD-3638 | Drug Info | Terminated | Schizophrenia | [18] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | Org-23366 | Drug Info | Preclinical | Schizophrenia | [18] | |
Mode of Action | [+] 7 Modes of Action | + | ||||
Inhibitor | [+] 191 Inhibitor drugs | + | ||||
1 | Aniracetam | Drug Info | [64] | |||
2 | ZOTEPINE | Drug Info | [69] | |||
3 | TRYPTAMINE | Drug Info | [75] | |||
4 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | [88] | |||
5 | MDL-11939 | Drug Info | [93] | |||
6 | TIOSPIRONE | Drug Info | [97] | |||
7 | MAZAPERTINE | Drug Info | [100] | |||
8 | YM-992 | Drug Info | [104] | |||
9 | A-80426 | Drug Info | [107] | |||
10 | MDL-28161 | Drug Info | [93] | |||
11 | Ro-60-0175 | Drug Info | [120] | |||
12 | RP-68303 | Drug Info | [121] | |||
13 | (+/-)-nantenine | Drug Info | [122] | |||
14 | (1-Phenethyl-piperidin-4-yl)-phenyl-methanone | Drug Info | [69] | |||
15 | (2-Indol-1-yl-ethyl)-dimethyl-amine | Drug Info | [123] | |||
16 | (2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine | Drug Info | [120] | |||
17 | (2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | [120] | |||
18 | (2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine | Drug Info | [120] | |||
19 | (2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine | Drug Info | [124] | |||
20 | (E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine | Drug Info | [125] | |||
21 | (E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine | Drug Info | [125] | |||
22 | (R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamine | Drug Info | [88] | |||
23 | (R)-(-)-11-hydroxy-N-n-propylnoraporphine | Drug Info | [126] | |||
24 | (R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [127] | |||
25 | (R)-3-(4-propylmorpholin-2-yl)phenol | Drug Info | [128] | |||
26 | (R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
27 | (R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
28 | (R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
29 | (R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
30 | (R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
31 | (S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine | Drug Info | [88] | |||
32 | (S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine | Drug Info | [129] | |||
33 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [130] | |||
34 | 1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole | Drug Info | [123] | |||
35 | 1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane | Drug Info | [131] | |||
36 | 1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane | Drug Info | [131] | |||
37 | 1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane | Drug Info | [131] | |||
38 | 1,6-bis(4-m-tolylpiperazin-1-yl)hexane | Drug Info | [131] | |||
39 | 1,6-bis(4-phenylpiperazin-1-yl)hexane | Drug Info | [131] | |||
40 | 1-((R)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [124] | |||
41 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [124] | |||
42 | 1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol | Drug Info | [124] | |||
43 | 1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol | Drug Info | [124] | |||
44 | 1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol | Drug Info | [124] | |||
45 | 1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol | Drug Info | [124] | |||
46 | 1-(10-Bromoanthracen-9-yl)-2-aminopropane | Drug Info | [132] | |||
47 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [133] | |||
48 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [133] | |||
49 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [132] | |||
50 | 1-(2,6-dimethoxy-4-methylphenyl)propan-2-amine | Drug Info | [132] | |||
51 | 1-(2-aminoethyl)-1H-indazol-6-ol | Drug Info | [124] | |||
52 | 1-(2-Methoxy-phenyl)-4-propyl-piperazine | Drug Info | [134] | |||
53 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [133] | |||
54 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [135] | |||
55 | 1-(3-(phenylthio)propyl)-4-m-tolylpiperazine | Drug Info | [136] | |||
56 | 1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane | Drug Info | [132] | |||
57 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [133] | |||
58 | 1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [132] | |||
59 | 1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol | Drug Info | [137] | |||
60 | 1-Butyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [134] | |||
61 | 1-Ethyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [134] | |||
62 | 1-methoxy-9-aminomethyl-9,10-dihydroanthracene | Drug Info | [138] | |||
63 | 1-Methyl-1,3-dihydro-indol-2-one | Drug Info | [139] | |||
64 | 1-Naphthalen-2-yl-piperazine | Drug Info | [130] | |||
65 | 1-naphthylpiperazine | Drug Info | [130] | |||
66 | 1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [140] | |||
67 | 11-Butyryloxy-N-n-propylnoraporphine | Drug Info | [126] | |||
68 | 11-Heptanoyloxy-N-n-propylnoraporphine | Drug Info | [126] | |||
69 | 11-Hexanoyloxy-N-n-propylnoraporphine | Drug Info | [126] | |||
70 | 11-Propionyloxy-N-n-propylnoraporphine | Drug Info | [126] | |||
71 | 11-valeryloxynoraporphine | Drug Info | [126] | |||
72 | 2,2-Diphenyl-ethylamine | Drug Info | [141] | |||
73 | 2,5-dimethoxy-4-bromophenethylamine | Drug Info | [142] | |||
74 | 2-(1H-indol-3-yl)-N,N-dimethylethanamine | Drug Info | [143], [132] | |||
75 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [144] | |||
76 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [144] | |||
77 | 2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine | Drug Info | [132] | |||
78 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [144] | |||
79 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [144] | |||
80 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [144] | |||
81 | 2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine | Drug Info | [145] | |||
82 | 2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | [124] | |||
83 | 2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine | Drug Info | [146] | |||
84 | 2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline | Drug Info | [147] | |||
85 | 2-methoxy-9-aminomethyl-9,10-dihydroanthracene | Drug Info | [138] | |||
86 | 2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole | Drug Info | [148] | |||
87 | 2-Phenyl-3-piperidin-4-yl-1H-indole | Drug Info | [148] | |||
88 | 2-Piperazin-1-yl-phenol | Drug Info | [133] | |||
89 | 3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole | Drug Info | [148] | |||
90 | 3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole | Drug Info | [148] | |||
91 | 3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole | Drug Info | [148] | |||
92 | 3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | [124] | |||
93 | 3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol | Drug Info | [137] | |||
94 | 3-(2-Dimethylamino-ethyl)-1H-indol-6-ol | Drug Info | [137] | |||
95 | 3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol | Drug Info | [137] | |||
96 | 3-(2-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | [137] | |||
97 | 3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol | Drug Info | [137] | |||
98 | 3-(3-Dimethylamino-propyl)-1H-indol-4-ol | Drug Info | [137] | |||
99 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [133] | |||
100 | 3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol | Drug Info | [137] | |||
101 | 3-Dimethylaminomethyl-1H-indol-4-ol | Drug Info | [137] | |||
102 | 3-methoxy-9-aminomethyl-9,10-dihydroanthracene | Drug Info | [138] | |||
103 | 3-Naphthalen-1-yl-1-propyl-pyrrolidine | Drug Info | [140] | |||
104 | 3-Naphthalen-1-yl-pyrrolidine | Drug Info | [140] | |||
105 | 4,4-Diphenylbutan-1-amine | Drug Info | [146] | |||
106 | 4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine | Drug Info | [141] | |||
107 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [149] | |||
108 | 4-(4-Fluoro-benzyl)-piperidine hydrochloride | Drug Info | [93] | |||
109 | 4-Benzyl-1-methyl-piperidine hydrochloride | Drug Info | [93] | |||
110 | 4-methoxy-9-aminomethyl-9,10-dihydroanthracene | Drug Info | [138] | |||
111 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [150] | |||
112 | 5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
113 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [150] | |||
114 | 5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | [129] | |||
115 | 5-MEO-DMT | Drug Info | [124] | |||
116 | 5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
117 | 5-Methoxy-4,9-dihydro-3H-beta-carboline | Drug Info | [151] | |||
118 | 5-METHOXYTRYPTAMINE | Drug Info | [75] | |||
119 | 6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine | Drug Info | [152] | |||
120 | 6-bromoaplysinopsin | Drug Info | [153] | |||
121 | 6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole | Drug Info | [123] | |||
122 | 6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide | Drug Info | [129] | |||
123 | 6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
124 | 7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine | Drug Info | [152] | |||
125 | 7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine | Drug Info | [152] | |||
126 | 7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole | Drug Info | [123] | |||
127 | 7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
128 | 8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
129 | 8-Bromo-4,9-dihydro-3H-beta-carboline | Drug Info | [151] | |||
130 | 8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole | Drug Info | [123] | |||
131 | 8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [151] | |||
132 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [130] | |||
133 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [130] | |||
134 | 8-Methoxy-4,9-dihydro-3H-beta-carboline | Drug Info | [151] | |||
135 | 9-(2-aminoethyl)-9,10-dihydroanthracene | Drug Info | [146] | |||
136 | 9-(2-aminopropyl)-9,10-dihydroanthracene | Drug Info | [146] | |||
137 | 9-(Aminomethyl)-9,10-dihydroanthracene | Drug Info | [141] | |||
138 | 9-(N-benzylaminomethyl)-9,10-dihydroanthracene | Drug Info | [154] | |||
139 | A-987306 | Drug Info | [156] | |||
140 | ALTANSERIN | Drug Info | [72] | |||
141 | Aplysinopsin | Drug Info | [129] | |||
142 | BARETTIN | Drug Info | [159] | |||
143 | Brolamfetamine | Drug Info | [161] | |||
144 | C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine | Drug Info | [142] | |||
145 | C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine | Drug Info | [141] | |||
146 | C-(9H-Thioxanthen-9-yl)-methylamine | Drug Info | [141] | |||
147 | C-(9H-Xanthen-9-yl)-methylamine | Drug Info | [141] | |||
148 | CHLOROPHENYLPIPERAZINE | Drug Info | [163] | |||
149 | CINANSERIN | Drug Info | [75] | |||
150 | DOM | Drug Info | [132] | |||
151 | Etisulergine | Drug Info | [167] | |||
152 | FLUANISONE | Drug Info | [168] | |||
153 | ISOCLOZAPINE | Drug Info | [169] | |||
154 | LY433222 | Drug Info | [104] | |||
155 | MESCALINE | Drug Info | [132] | |||
156 | N,N-dimethyl-2,2-diphenylethanamine | Drug Info | [146] | |||
157 | N,N-Dimethyl-3,3-diphenylpropan-1-amine | Drug Info | [146] | |||
158 | N,N-dimethyl-4,4-diphenylbutan-1-amine | Drug Info | [146] | |||
159 | N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide | Drug Info | [177] | |||
160 | N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide | Drug Info | [177] | |||
161 | N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide | Drug Info | [178] | |||
162 | N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide | Drug Info | [178] | |||
163 | N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide | Drug Info | [178] | |||
164 | N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide | Drug Info | [178] | |||
165 | N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide | Drug Info | [177] | |||
166 | N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide | Drug Info | [177] | |||
167 | N-(1-benzylpiperidine-4-yl)-2-naphthamide | Drug Info | [178] | |||
168 | N-(1-phenethylpiperidin-4-yl)-1-naphthamide | Drug Info | [177] | |||
169 | N-(1-phenethylpiperidin-4-yl)-2-naphthamide | Drug Info | [177] | |||
170 | N-3'-ethylaplysinopsin | Drug Info | [153] | |||
171 | N-methyl-3,3-diphenylpropan-1-amine | Drug Info | [146] | |||
172 | N-methyl-4,4-diphenylbutan-1-amine | Drug Info | [146] | |||
173 | PG-01037 | Drug Info | [180] | |||
174 | PHENETHYLAMINE | Drug Info | [141] | |||
175 | PHENYLPIPERAZINE | Drug Info | [130] | |||
176 | PSILOCIN | Drug Info | [132] | |||
177 | QUIPAZINE | Drug Info | [181] | |||
178 | Racemic DOI | Drug Info | [132] | |||
179 | Racemic DOTFM | Drug Info | [132] | |||
180 | SB-271046 | Drug Info | [185] | |||
181 | SEROTONIN | Drug Info | [181] | |||
182 | TRYPTOLINE | Drug Info | [151] | |||
183 | VER-2692 | Drug Info | [186] | |||
184 | VER-3323 | Drug Info | [187] | |||
185 | VER-5384 | Drug Info | [187] | |||
186 | VER-5593 | Drug Info | [187] | |||
187 | WAY-208466 | Drug Info | [188] | |||
188 | YM-348 | Drug Info | [152] | |||
189 | [2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | [137] | |||
190 | [2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amine | Drug Info | [123] | |||
191 | [3H]spiperone | Drug Info | [192] | |||
Modulator | [+] 21 Modulator drugs | + | ||||
1 | Flibanserin | Drug Info | [5] | |||
2 | Lurasidone hydrochloride | Drug Info | [10], [11] | |||
3 | Pimavanserin | Drug Info | [13], [66] | |||
4 | SR46349B | Drug Info | [73] | |||
5 | Zicronapine | Drug Info | [76] | |||
6 | NELOTANSERIN | Drug Info | [78] | |||
7 | Ocaperidone | Drug Info | [30] | |||
8 | PRUVANSERIN | Drug Info | [80] | |||
9 | Abaperidone | Drug Info | [82] | |||
10 | ATI-9242 | Drug Info | [83], [30] | |||
11 | YKP-1358 | Drug Info | [86] | |||
12 | Deramciclane | Drug Info | [89], [90], [91] | |||
13 | Iferanserin-Ventrus | Drug Info | [92] | |||
14 | SL65.0472 | Drug Info | [103] | |||
15 | DUP-734 | Drug Info | [106] | |||
16 | AMPEROZIDE | Drug Info | [108] | |||
17 | ICI-169369 | Drug Info | [113] | |||
18 | R-102444 | Drug Info | [117], [118], [119] | |||
19 | EPLIVANSERIN MESILATE | Drug Info | [166] | |||
20 | SEL-73 | Drug Info | [30] | |||
21 | Very low dose (VLD) cyclobenzaprine | Drug Info | [30] | |||
Antagonist | [+] 70 Antagonist drugs | + | ||||
1 | Iloperidone | Drug Info | [7], [18] | |||
2 | lumateperone tosylate | Drug Info | [8] | |||
3 | Metergolin | Drug Info | [65] | |||
4 | Sarpogrelate | Drug Info | [1], [67], [68] | |||
5 | Blonanserin | Drug Info | [18] | |||
6 | ITI-007 | Drug Info | [70] | |||
7 | M100907 | Drug Info | [71], [72] | |||
8 | MIN-101 | Drug Info | [30] | |||
9 | TNX-102 | Drug Info | [74] | |||
10 | BVT.28949 | Drug Info | [77], [30] | |||
11 | FKW00GA | Drug Info | [26] | |||
12 | SYN120 | Drug Info | [81] | |||
13 | 1192U90 | Drug Info | [18] | |||
14 | DSP-1200 | Drug Info | [26] | |||
15 | 3-phenyl pyrazole derivative 1 | Drug Info | [87] | |||
16 | Benzoyl-piperidine derivative 1 | Drug Info | [87] | |||
17 | Benzoyl-piperidine derivative 2 | Drug Info | [87] | |||
18 | L-piperazino-3-phenyl-indane derivative 1 | Drug Info | [87] | |||
19 | Piperazine derivative 3 | Drug Info | [87] | |||
20 | Piperazine derivative 4 | Drug Info | [87] | |||
21 | PMID26609882-Compound-34 | Drug Info | [87] | |||
22 | PMID26609882-Compound-35 | Drug Info | [87] | |||
23 | PMID26609882-Compound-36 | Drug Info | [87] | |||
24 | PMID30124346-Compound-LDT8 | Drug Info | [38] | |||
25 | Pyrazole derivative 67 | Drug Info | [87] | |||
26 | Pyrazole derivative 68 | Drug Info | [87] | |||
27 | Pyrazole derivative 69 | Drug Info | [87] | |||
28 | Pyrazole derivative 70 | Drug Info | [87] | |||
29 | Pyrazole derivative 71 | Drug Info | [87] | |||
30 | Pyrazole derivative 72 | Drug Info | [87] | |||
31 | Pyrazole derivative 73 | Drug Info | [87] | |||
32 | Pyrazole derivative 74 | Drug Info | [87] | |||
33 | Pyrazole derivative 75 | Drug Info | [87] | |||
34 | Pyrimidine derivative 23 | Drug Info | [87] | |||
35 | Pyrimidine derivative 24 | Drug Info | [87] | |||
36 | Pyrimidine derivative 25 | Drug Info | [87] | |||
37 | Pyrimidine derivative 26 | Drug Info | [87] | |||
38 | Pyrimidine derivative 27 | Drug Info | [87] | |||
39 | Pyrimidine derivative 28 | Drug Info | [87] | |||
40 | Pyrimidine derivative 29 | Drug Info | [87] | |||
41 | Ritanserin | Drug Info | [94], [95], [96] | |||
42 | Adatanserin | Drug Info | [48], [98] | |||
43 | AMESERGIDE | Drug Info | [99], [30] | |||
44 | FCE-22716 | Drug Info | [51], [30] | |||
45 | SERAZAPINE HYDROCHLORIDE | Drug Info | [101], [30] | |||
46 | SERGOLEXOLE MALEATE | Drug Info | [102], [30] | |||
47 | Org-23366 | Drug Info | [18] | |||
48 | Fananserin | Drug Info | [112], [18] | |||
49 | GMC-283 | Drug Info | [18] | |||
50 | LY53857 | Drug Info | [96], [114], [115], [116] | |||
51 | 9-OH-risperidone | Drug Info | [155] | |||
52 | bufotenine | Drug Info | [162] | |||
53 | cyamemazine | Drug Info | [164] | |||
54 | EGIS-7625 | Drug Info | [165] | |||
55 | LY063518 | Drug Info | [171] | |||
56 | LY108742 | Drug Info | [172] | |||
57 | LY215840 | Drug Info | [172] | |||
58 | LY314228 | Drug Info | [171] | |||
59 | LY320954 | Drug Info | [171] | |||
60 | LY86057 | Drug Info | [172] | |||
61 | MPDT | Drug Info | [176] | |||
62 | norfluoxetine | Drug Info | [179] | |||
63 | SB 215505 | Drug Info | [182] | |||
64 | SB 221284 | Drug Info | [65] | |||
65 | SB 228357 | Drug Info | [183] | |||
66 | SB 242084 | Drug Info | [184] | |||
67 | spiramide | Drug Info | [65] | |||
68 | [11C]volinanserin | Drug Info | [189] | |||
69 | [18F]altanserin | Drug Info | [191] | |||
70 | [3H]N-methylspiperone | Drug Info | [158] | |||
Agonist | [+] 25 Agonist drugs | + | ||||
1 | Nuplazid | Drug Info | [79] | |||
2 | Temanogrel | Drug Info | [85], [30] | |||
3 | Aryl piperazine derivative 9 | Drug Info | [87] | |||
4 | Diarylamine and arylheteroarylamine pyrazole derivative 1 | Drug Info | [87] | |||
5 | Diarylamine and arylheteroarylamine pyrazole derivative 2 | Drug Info | [87] | |||
6 | Diarylamine and arylheteroarylamine pyrazole derivative 3 | Drug Info | [87] | |||
7 | AM-831 | Drug Info | [105] | |||
8 | DV-7028 | Drug Info | [109], [110], [111] | |||
9 | 5-CT | Drug Info | [65] | |||
10 | ACP-106 | Drug Info | [30] | |||
11 | AL-37350A | Drug Info | [157] | |||
12 | alpha-methyl-5-HT | Drug Info | [158] | |||
13 | BRL-15572 | Drug Info | [160] | |||
14 | BW723C86 | Drug Info | [65] | |||
15 | LP-12 | Drug Info | [170] | |||
16 | LP-44 | Drug Info | [170] | |||
17 | m-chlorophenylpiperazine | Drug Info | [173] | |||
18 | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | [174] | |||
19 | MMDA | Drug Info | [175] | |||
20 | N-1-isopropyl-5-MeOT | Drug Info | [172] | |||
21 | N-1-isopropyltryptamine | Drug Info | [172] | |||
22 | Org 12962 | Drug Info | [65] | |||
23 | SB 216641 | Drug Info | [160] | |||
24 | TFMPP | Drug Info | [65], [133] | |||
25 | [125I]DOI | Drug Info | [190] | |||
Partial agonist | [+] 1 Partial agonist drugs | + | ||||
1 | RP5063 | Drug Info | [26] | |||
Binder | [+] 2 Binder drugs | + | ||||
1 | SKL-10406 | Drug Info | [84] | |||
2 | ZD-3638 | Drug Info | [18] | |||
Ligand | [+] 4 Ligand drugs | + | ||||
1 | Aryl piperazine derivative 1 | Drug Info | [38] | |||
2 | Aryl piperazine derivative 6 | Drug Info | [38] | |||
3 | PMID30124346-Compound-13TABLE4 | Drug Info | [38] | |||
4 | PMID30124346-Compound-34TABLE4 | Drug Info | [38] |
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"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 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 | [+] 9 WikiPathways | + | ||||
1 | Serotonin Receptor 2 and STAT3 Signaling | |||||
2 | Serotonin Receptor 2 and ELK-SRF/GATA4 signaling | |||||
3 | SIDS Susceptibility Pathways | |||||
4 | Monoamine GPCRs | |||||
5 | GPCRs, Class A Rhodopsin-like | |||||
6 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
7 | GPCR ligand binding | |||||
8 | GPCR downstream signaling | |||||
9 | GPCRs, Other |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
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