Target Information
Target General Information | Top | |||||
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Target ID |
T78709
(Former ID: TTDS00098)
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Target Name |
5-HT 1A receptor (HTR1A)
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Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Gene Name |
HTR1A
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 5 Target-related Diseases | + | ||||
1 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
2 | Depression [ICD-11: 6A70-6A7Z] | |||||
3 | Hypertension [ICD-11: BA00-BA04] | |||||
4 | Migraine [ICD-11: 8A80] | |||||
5 | Mood disorder [ICD-11: 6A60-6E23] | |||||
Function |
Functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC RQ Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T31QEZ |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 9 Approved Drugs | + | ||||
1 | Buspirone | Drug Info | Approved | Anxiety disorder | [2], [3] | |
2 | Flibanserin | Drug Info | Approved | Mood disorder | [4], [5] | |
3 | Gepirone | Drug Info | Approved | Major depressive disorder | [6] | |
4 | OPC-34712 | Drug Info | Approved | Major depressive disorder | [7], [8] | |
5 | TERTATOLOL | Drug Info | Approved | Hypertension | [9], [10] | |
6 | Trazodone | Drug Info | Approved | Depression | [11], [12] | |
7 | Treximet | Drug Info | Approved | Migraine | [13] | |
8 | Urapidil | Drug Info | Approved | Hypertension | [10] | |
9 | Vilazodone | Drug Info | Approved | Major depressive disorder | [14], [15] | |
Clinical Trial Drug(s) | [+] 32 Clinical Trial Drugs | + | ||||
1 | CM-2395 | Drug Info | Phase 3 | Schizophrenia | [16] | |
2 | Eltoprazine | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [17] | |
3 | SEP-363856 | Drug Info | Phase 3 | Schizophrenia | [18] | |
4 | Xaliproden | Drug Info | Phase 3 | Juvenile idiopathic arthritis | [19] | |
5 | LECOZOTAN HYDROCHLORIDE | Drug Info | Phase 2/3 | Cognitive impairment | [20] | |
6 | Sarizotan | Drug Info | Phase 2/3 | Rett syndrome | [21] | |
7 | Ensaculin hydrochloride | Drug Info | Phase 2 | Parkinson disease | [22] | |
8 | FKW00GA | Drug Info | Phase 2 | Social phobia | [17] | |
9 | Mazapertine succinate | Drug Info | Phase 2 | Psychotic disorder | [23] | |
10 | MIN-117 | Drug Info | Phase 2 | Major depressive disorder | [24] | |
11 | MN-305 | Drug Info | Phase 2 | Mood disorder | [25] | |
12 | Neu-P11 | Drug Info | Phase 2 | Insomnia | [26] | |
13 | OPC-14523 | Drug Info | Phase 2 | Mood disorder | [27] | |
14 | ORG-13011 | Drug Info | Phase 2 | Psychotic disorder | [28] | |
15 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [29] | |
16 | S-15535 | Drug Info | Phase 2 | Anxiety disorder | [30], [31] | |
17 | S-16924 | Drug Info | Phase 2 | Anxiety disorder | [32], [33], [34] | |
18 | SDZ-MAR-327 | Drug Info | Phase 2 | Psychotic disorder | [35], [36] | |
19 | SUN N4057 | Drug Info | Phase 2 | Coronary artery disease | [37] | |
20 | TGBA01AD | Drug Info | Phase 2 | Mood disorder | [25] | |
21 | TGFK08AA | Drug Info | Phase 2 | Generalized anxiety disorder | [38] | |
22 | TGFK09SD | Drug Info | Phase 2 | Hypoactive sexual desire dysfunction | [39] | |
23 | TGWOOAA | Drug Info | Phase 2 | Social phobia | [40] | |
24 | Zalospirone | Drug Info | Phase 2 | Anxiety disorder | [41], [42] | |
25 | 1192U90 | Drug Info | Phase 1 | Psychotic disorder | [43] | |
26 | AV-965 | Drug Info | Phase 1 | Alzheimer disease | [44] | |
27 | DSP-1053 | Drug Info | Phase 1 | Major depressive disorder | [45] | |
28 | GSK-958108 | Drug Info | Phase 1 | Premature ejaculation | [46] | |
29 | NLX-101 | Drug Info | Phase 1 | Rett syndrome | [47] | |
30 | SKL-PSY | Drug Info | Phase 1 | Bipolar disorder | [48] | |
31 | SSR-181507 | Drug Info | Phase 1 | Schizophrenia | [35] | |
32 | Umespirone | Drug Info | Phase 1 | Anxiety disorder | [49] | |
Patented Agent(s) | [+] 5 Patented Agents | + | ||||
1 | PMID30124346-Compound-13TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [50] | |
2 | PMID30124346-Compound-34TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [50] | |
3 | PMID30124346-Compound-60TABLE5 | Drug Info | Patented | Parkinson disease | [50], [51], [52] | |
4 | PMID30124346-Compound-LDT66 | Drug Info | Patented | Benign prostatic hyperplasia | [50] | |
5 | PMID30124346-Compound-LDT8 | Drug Info | Patented | Benign prostatic hyperplasia | [50] | |
Discontinued Drug(s) | [+] 35 Discontinued Drugs | + | ||||
1 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | Withdrawn from market | Addictive disorder | [53], [54] | |
2 | Bifeprunox | Drug Info | Discontinued in Phase 3 | Schizophrenia | [35] | |
3 | BMS-181100 | Drug Info | Discontinued in Phase 3 | Psychotic disorder | [55], [56] | |
4 | Flesinoxan | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [57], [58] | |
5 | Adatanserin | Drug Info | Discontinued in Phase 2 | Mood disorder | [25] | |
6 | ALNESPIRONE | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [59] | |
7 | AP-521 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [60] | |
8 | DU 125530 | Drug Info | Discontinued in Phase 2 | Mood disorder | [61] | |
9 | GSK163090 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [62] | |
10 | LESOPITRON DIHYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Mood disorder | [63] | |
11 | PRX-00023 | Drug Info | Discontinued in Phase 2 | Mood disorder | [25] | |
12 | REC-15/3079 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [64], [65] | |
13 | Robalzotan | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [66], [67] | |
14 | BINOSPIRONE MESYLATE | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [68] | |
15 | DU-29894 | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [69] | |
16 | E2101 | Drug Info | Discontinued in Phase 1 | Spasm | [70] | |
17 | Ebalzotan | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [71] | |
18 | Eptapirone | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [72] | |
19 | GR-127607 | Drug Info | Discontinued in Phase 1 | Migraine | [73] | |
20 | Nerisopam | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [74] | |
21 | SLV-313 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [35] | |
22 | SUN-8399 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [75] | |
23 | U-93385 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [76] | |
24 | A-74283 | Drug Info | Terminated | Hypertension | [78] | |
25 | Anpirtoline | Drug Info | Terminated | Pain | [79] | |
26 | BTS-79018 | Drug Info | Terminated | Schizophrenia | [35] | |
27 | CGS-18102A | Drug Info | Terminated | Anxiety disorder | [80] | |
28 | Du-123015 | Drug Info | Terminated | Anxiety disorder | [81] | |
29 | HT-90B | Drug Info | Terminated | Anxiety disorder | [82] | |
30 | Ipsapirone | Drug Info | Terminated | Anxiety disorder | [83], [84] | |
31 | LY-293284 | Drug Info | Terminated | Anxiety disorder | [85], [86] | |
32 | RWJ-25730 | Drug Info | Terminated | Psychotic disorder | [87] | |
33 | S-14506 | Drug Info | Terminated | Anxiety disorder | [88], [89] | |
34 | SLV-307 | Drug Info | Terminated | Parkinson disease | [90] | |
35 | WAY-100635 | Drug Info | Terminated | Eating disorder | [91], [92] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | CM-2236 | Drug Info | Preclinical | Post-traumatic stress disorder | [77] | |
2 | PD-158771 | Drug Info | Preclinical | Schizophrenia | [35] | |
Mode of Action | [+] 7 Modes of Action | + | ||||
Agonist | [+] 50 Agonist drugs | + | ||||
1 | Buspirone | Drug Info | [1] | |||
2 | Gepirone | Drug Info | [6] | |||
3 | Urapidil | Drug Info | [98] | |||
4 | CM-2395 | Drug Info | [99] | |||
5 | Eltoprazine | Drug Info | [100] | |||
6 | SEP-363856 | Drug Info | [21] | |||
7 | MN-305 | Drug Info | [25] | |||
8 | Neu-P11 | Drug Info | [106] | |||
9 | SUN N4057 | Drug Info | [114] | |||
10 | Zalospirone | Drug Info | [42] | |||
11 | 1192U90 | Drug Info | [35] | |||
12 | Aryl piperazine derivative 14 | Drug Info | [50] | |||
13 | Aryl piperazine derivative 15 | Drug Info | [50] | |||
14 | Aryl piperazine derivative 16 | Drug Info | [50] | |||
15 | PMID30124346-Compound-13TABLE4 | Drug Info | [50] | |||
16 | Flesinoxan | Drug Info | [130] | |||
17 | Adatanserin | Drug Info | [25], [133] | |||
18 | ALNESPIRONE | Drug Info | [134], [10] | |||
19 | AP-521 | Drug Info | [135], [10] | |||
20 | LESOPITRON DIHYDROCHLORIDE | Drug Info | [137] | |||
21 | Ebalzotan | Drug Info | [145] | |||
22 | Eptapirone | Drug Info | [146] | |||
23 | GR-127607 | Drug Info | [147] | |||
24 | Nerisopam | Drug Info | [148] | |||
25 | SUN-8399 | Drug Info | [150] | |||
26 | U-93385 | Drug Info | [151], [10] | |||
27 | CM-2236 | Drug Info | [152] | |||
28 | A-74283 | Drug Info | [153] | |||
29 | Ipsapirone | Drug Info | [160] | |||
30 | LY-293284 | Drug Info | [161] | |||
31 | 1-naphthylpiperazine | Drug Info | [185], [174] | |||
32 | 5-CT | Drug Info | [200] | |||
33 | 7-methoxy-1-naphthylpiperazine | Drug Info | [185] | |||
34 | BRL-15572 | Drug Info | [204] | |||
35 | CP 93129 | Drug Info | [200] | |||
36 | EDMT | Drug Info | [207] | |||
37 | FG-5893 | Drug Info | [211] | |||
38 | L-772,405 | Drug Info | [213] | |||
39 | LP-12 | Drug Info | [214] | |||
40 | LP-211 | Drug Info | [215] | |||
41 | LP-44 | Drug Info | [214] | |||
42 | LY 165,163 | Drug Info | [211] | |||
43 | nafadotride | Drug Info | [211] | |||
44 | piribedil | Drug Info | [222] | |||
45 | S-14671 | Drug Info | [112] | |||
46 | SB 216641 | Drug Info | [204] | |||
47 | spiroxatrine | Drug Info | [211] | |||
48 | U92016A | Drug Info | [232] | |||
49 | [3H]8-OH-DPAT | Drug Info | [237] | |||
50 | [3H]NLX-112 | Drug Info | [238] | |||
Modulator | [+] 34 Modulator drugs | + | ||||
1 | Flibanserin | Drug Info | [5] | |||
2 | OPC-34712 | Drug Info | [93], [94] | |||
3 | Trazodone | Drug Info | [96] | |||
4 | Vilazodone | Drug Info | [15] | |||
5 | Sarizotan | Drug Info | [103] | |||
6 | Ensaculin hydrochloride | Drug Info | [22], [104] | |||
7 | FKB01MD | Drug Info | [17] | |||
8 | Mazapertine succinate | Drug Info | [103] | |||
9 | OPC-14523 | Drug Info | [107] | |||
10 | S-16924 | Drug Info | [33], [34] | |||
11 | SDZ-MAR-327 | Drug Info | [113] | |||
12 | TGBA01AD | Drug Info | [115] | |||
13 | TGFK08AA | Drug Info | [116] | |||
14 | TGFK09SD | Drug Info | [117] | |||
15 | NLX-101 | Drug Info | [122] | |||
16 | SKL-PSY | Drug Info | [123] | |||
17 | SSR-181507 | Drug Info | [124] | |||
18 | Bifeprunox | Drug Info | [127] | |||
19 | BMS-181100 | Drug Info | [128], [129] | |||
20 | PRX-00023 | Drug Info | [139] | |||
21 | DU-29894 | Drug Info | [143] | |||
22 | E2101 | Drug Info | [144] | |||
23 | SLV-313 | Drug Info | [149] | |||
24 | Anpirtoline | Drug Info | [79] | |||
25 | CGS-18102A | Drug Info | [156] | |||
26 | Du-123015 | Drug Info | [158] | |||
27 | HT-90B | Drug Info | [159] | |||
28 | RWJ-25730 | Drug Info | [163] | |||
29 | S-14506 | Drug Info | [164] | |||
30 | CGS-19480A | Drug Info | [205], [10] | |||
31 | EMD 56551 | Drug Info | [208] | |||
32 | NPT-500 | Drug Info | [123] | |||
33 | SEL-73 | Drug Info | [123] | |||
34 | SR-59026 | Drug Info | [231] | |||
Inhibitor | [+] 142 Inhibitor drugs | + | ||||
1 | TERTATOLOL | Drug Info | [95] | |||
2 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | [126] | |||
3 | Sunepitron | Drug Info | [131] | |||
4 | TIOSPIRONE | Drug Info | [132] | |||
5 | MAZAPERTINE | Drug Info | [138] | |||
6 | A-80426 | Drug Info | [154] | |||
7 | BMY-7378 | Drug Info | [155] | |||
8 | CP-293019 | Drug Info | [157] | |||
9 | WB-4101 | Drug Info | [169] | |||
10 | (3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | [170] | |||
11 | (R)-(-)-10-methyl-11-hydroxyaporphine | Drug Info | [171] | |||
12 | (R)-11-Amino-2-methoxyaporphine | Drug Info | [172] | |||
13 | (R)-2,11-Diaminoaporphine | Drug Info | [172] | |||
14 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [174] | |||
15 | 1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane | Drug Info | [175] | |||
16 | 1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane | Drug Info | [175] | |||
17 | 1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane | Drug Info | [175] | |||
18 | 1,6-bis(4-m-tolylpiperazin-1-yl)hexane | Drug Info | [175] | |||
19 | 1,6-bis(4-phenylpiperazin-1-yl)hexane | Drug Info | [175] | |||
20 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [176] | |||
21 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [170] | |||
22 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [170] | |||
23 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [177] | |||
24 | 1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine | Drug Info | [178] | |||
25 | 1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine | Drug Info | [179] | |||
26 | 1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | [178] | |||
27 | 1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | [178] | |||
28 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [178] | |||
29 | 1-(2-(benzyloxy)phenyl)piperazine | Drug Info | [178] | |||
30 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [178] | |||
31 | 1-(2-Butoxy-phenyl)-piperazine | Drug Info | [180] | |||
32 | 1-(2-Chloro-phenyl)-piperazine | Drug Info | [181] | |||
33 | 1-(2-Ethoxy-phenyl)-piperazine | Drug Info | [180] | |||
34 | 1-(2-Fluoro-phenyl)-piperazine | Drug Info | [180] | |||
35 | 1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | [180] | |||
36 | 1-(2-Methoxy-phenyl)-4-propyl-piperazine | Drug Info | [182] | |||
37 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [181] | |||
38 | 1-(2-methoxyphenyl)-4-pentylpiperazine | Drug Info | [183] | |||
39 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [178] | |||
40 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [184] | |||
41 | 1-(3-Fluoro-phenyl)-piperazine | Drug Info | [180] | |||
42 | 1-(3-Nitro-phenyl)-piperazine | Drug Info | [180] | |||
43 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [170] | |||
44 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [185] | |||
45 | 1-(benzyloxy)-2-(2-phenylethyl)benzene | Drug Info | [186] | |||
46 | 1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene | Drug Info | [186] | |||
47 | 1-Benzyl-4-chroman-2-ylmethyl-piperazine | Drug Info | [187] | |||
48 | 1-Butyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [182] | |||
49 | 1-Ethyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [182] | |||
50 | 1-Methyl-1,3-dihydro-indol-2-one | Drug Info | [188] | |||
51 | 1-Naphthalen-2-yl-piperazine | Drug Info | [174] | |||
52 | 1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [189] | |||
53 | 1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene | Drug Info | [186] | |||
54 | 2-(2'-methyl-biphenyl-3-yl)-ethylamine | Drug Info | [190] | |||
55 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [177] | |||
56 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [179] | |||
57 | 2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [179] | |||
58 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [177] | |||
59 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [179] | |||
60 | 2-(3-Bromophenylthio)-N,N-dimethylethanamine | Drug Info | [191] | |||
61 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [177] | |||
62 | 2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [187] | |||
63 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [177] | |||
64 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [177] | |||
65 | 2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine | Drug Info | [192] | |||
66 | 2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | [193] | |||
67 | 2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine | Drug Info | [191] | |||
68 | 2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol | Drug Info | [95] | |||
69 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [179] | |||
70 | 2-Piperazin-1-yl-benzonitrile | Drug Info | [180] | |||
71 | 2-Piperazin-1-yl-phenol | Drug Info | [170] | |||
72 | 2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [186] | |||
73 | 3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole | Drug Info | [194] | |||
74 | 3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | [189] | |||
75 | 3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | [193] | |||
76 | 3-(2-Benzylamino-ethoxy)-phenol | Drug Info | [195] | |||
77 | 3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine | Drug Info | [189] | |||
78 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [187] | |||
79 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one | Drug Info | [187] | |||
80 | 3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | [179] | |||
81 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [170] | |||
82 | 3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [196] | |||
83 | 3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [196] | |||
84 | 3-Naphthalen-1-yl-1-propyl-pyrrolidine | Drug Info | [189] | |||
85 | 3-Naphthalen-1-yl-pyrrolidine | Drug Info | [189] | |||
86 | 3-Phenyl-1-propyl-pyrrolidine | Drug Info | [189] | |||
87 | 3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [186] | |||
88 | 4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol | Drug Info | [197] | |||
89 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [178] | |||
90 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [178] | |||
91 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
92 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
93 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [178] | |||
94 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
95 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [178] | |||
96 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [178] | |||
97 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [178] | |||
98 | 4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | [179] | |||
99 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
100 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
101 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [178] | |||
102 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [178] | |||
103 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [178] | |||
104 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [198] | |||
105 | 4-Benzyl-1-chroman-2-ylmethyl-piperidine | Drug Info | [187] | |||
106 | 4-Benzyl-1-chroman-3-ylmethyl-piperidine | Drug Info | [187] | |||
107 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [199] | |||
108 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [199] | |||
109 | 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [199] | |||
110 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [199] | |||
111 | 8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine | Drug Info | [95] | |||
112 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [174] | |||
113 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [174] | |||
114 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [199] | |||
115 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [174] | |||
116 | 9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine | Drug Info | [95] | |||
117 | A-987306 | Drug Info | [202] | |||
118 | AGROCLAVINE | Drug Info | [203] | |||
119 | Brolamfetamine | Drug Info | [177] | |||
120 | CHLOROPHENYLPIPERAZINE | Drug Info | [180] | |||
121 | ESCHOLTZINE | Drug Info | [209] | |||
122 | Etisulergine | Drug Info | [210] | |||
123 | JNJ-10392980 | Drug Info | [212] | |||
124 | MCL-516 | Drug Info | [172] | |||
125 | N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine | Drug Info | [197] | |||
126 | N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine | Drug Info | [197] | |||
127 | N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide | Drug Info | [215] | |||
128 | N-methyllaurotetanine | Drug Info | [209] | |||
129 | N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide | Drug Info | [217] | |||
130 | PB-28 | Drug Info | [220] | |||
131 | PG-01037 | Drug Info | [221] | |||
132 | PHENYLPIPERAZINE | Drug Info | [174] | |||
133 | QUIPAZINE | Drug Info | [223] | |||
134 | SB-271046 | Drug Info | [228] | |||
135 | SB-656104 | Drug Info | [229] | |||
136 | SEROTONIN | Drug Info | [223] | |||
137 | SNAP-8719 | Drug Info | [230] | |||
138 | TFMPP | Drug Info | [170] | |||
139 | UH-232 | Drug Info | [233] | |||
140 | UH-301 | Drug Info | [234] | |||
141 | WAY-466 | Drug Info | [235] | |||
142 | [3H]spiperone | Drug Info | [169] | |||
Antagonist | [+] 41 Antagonist drugs | + | ||||
1 | Treximet | Drug Info | [97] | |||
2 | Xaliproden | Drug Info | [101] | |||
3 | LECOZOTAN HYDROCHLORIDE | Drug Info | [10], [102] | |||
4 | FKW00GA | Drug Info | [17] | |||
5 | MIN-117 | Drug Info | [105] | |||
6 | ORG-13011 | Drug Info | [10], [108] | |||
7 | RP5063 | Drug Info | [109], [110] | |||
8 | S-15535 | Drug Info | [10], [111], [112] | |||
9 | TGWOOAA | Drug Info | [118] | |||
10 | AV-965 | Drug Info | [119] | |||
11 | DSP-1053 | Drug Info | [120] | |||
12 | GSK-958108 | Drug Info | [121] | |||
13 | Umespirone | Drug Info | [125] | |||
14 | PMID30124346-Compound-LDT8 | Drug Info | [50] | |||
15 | DU 125530 | Drug Info | [136] | |||
16 | GSK163090 | Drug Info | [97] | |||
17 | REC-15/3079 | Drug Info | [140] | |||
18 | Robalzotan | Drug Info | [141] | |||
19 | BINOSPIRONE MESYLATE | Drug Info | [142], [10] | |||
20 | PD-158771 | Drug Info | [35] | |||
21 | NAN-190 | Drug Info | [162] | |||
22 | SDZ 216-525 | Drug Info | [162] | |||
23 | SLV-307 | Drug Info | [165] | |||
24 | WAY-100635 | Drug Info | [136], [166], [167], [168] | |||
25 | (R)-flurocarazolol | Drug Info | [173] | |||
26 | (S)-flurocarazolol | Drug Info | [173] | |||
27 | 9-OH-risperidone | Drug Info | [201] | |||
28 | cyamemazine | Drug Info | [206] | |||
29 | GR 125,743 | Drug Info | [200] | |||
30 | LY433221 | Drug Info | [216] | |||
31 | MPDT | Drug Info | [207] | |||
32 | P-MPPI | Drug Info | [218], [162] | |||
33 | p-[18F]MPPF | Drug Info | [219] | |||
34 | repinotan | Drug Info | [224] | |||
35 | SB 272183 | Drug Info | [226] | |||
36 | SB 649915 | Drug Info | [227] | |||
37 | SB 714786 | Drug Info | [227] | |||
38 | WAY 100135 | Drug Info | [162] | |||
39 | [11C]WAY100635 | Drug Info | [236] | |||
40 | [3H]p-MPPF | Drug Info | [239] | |||
41 | [3H]robalzotan | Drug Info | [240] | |||
Ligand | [+] 4 Ligand drugs | + | ||||
1 | Aryl piperazine derivative 1 | Drug Info | [50] | |||
2 | Aryl piperazine derivative 6 | Drug Info | [50] | |||
3 | PMID30124346-Compound-34TABLE4 | Drug Info | [50] | |||
4 | PMID30124346-Compound-60TABLE5 | Drug Info | [50] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | BTS-79018 | Drug Info | [35] | |||
Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
1 | RS-30199 | Drug Info | [225] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
---|---|
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
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
cAMP signaling pathway | hsa04024 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Serotonergic synapse | hsa04726 | Affiliated Target |
|
Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
Taste transduction | hsa04742 | Affiliated Target |
|
Class: Organismal Systems => Sensory system | Pathway Hierarchy |
Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 6.17E-05 |
---|---|---|---|---|---|
Closeness centrality | 1.92E-01 | Radiality | 1.33E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 1.70E+01 | Topological coefficient | 5.00E-01 | Eccentricity | 13 |
Download | Click to Download the Full PPI Network of This Target | ||||
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 Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating Transcription Factors |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | cAMP signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Serotonergic synapse | |||||
Panther Pathway | [+] 2 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | 5HT1 type receptor mediated signaling pathway | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Serotonin receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | Serotonin HTR1 Group and FOS Pathway | |||||
2 | SIDS Susceptibility Pathways | |||||
3 | Monoamine GPCRs | |||||
4 | GPCRs, Class A Rhodopsin-like | |||||
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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