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) | [+] 8 Approved Drugs | + | ||||
1 | Buspirone | Drug Info | Approved | Anxiety disorder | [2], [3] | |
2 | Flibanserin | Drug Info | Approved | Mood disorder | [4], [5] | |
3 | OPC-34712 | Drug Info | Approved | Major depressive disorder | [6], [7] | |
4 | TERTATOLOL | Drug Info | Approved | Hypertension | [8], [9] | |
5 | Trazodone | Drug Info | Approved | Depression | [10], [11] | |
6 | Treximet | Drug Info | Approved | Migraine | [12] | |
7 | Urapidil | Drug Info | Approved | Hypertension | [9] | |
8 | Vilazodone | Drug Info | Approved | Major depressive disorder | [13], [14] | |
Clinical Trial Drug(s) | [+] 32 Clinical Trial Drugs | + | ||||
1 | CM-2395 | Drug Info | Phase 3 | Schizophrenia | [15] | |
2 | Eltoprazine | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [16] | |
3 | SEP-363856 | Drug Info | Phase 3 | Schizophrenia | [17] | |
4 | Xaliproden | Drug Info | Phase 3 | Juvenile idiopathic arthritis | [18] | |
5 | LECOZOTAN HYDROCHLORIDE | Drug Info | Phase 2/3 | Cognitive impairment | [19] | |
6 | Sarizotan | Drug Info | Phase 2/3 | Rett syndrome | [20] | |
7 | Ensaculin hydrochloride | Drug Info | Phase 2 | Parkinson disease | [21] | |
8 | FKW00GA | Drug Info | Phase 2 | Social phobia | [16] | |
9 | Mazapertine succinate | Drug Info | Phase 2 | Psychotic disorder | [22] | |
10 | MIN-117 | Drug Info | Phase 2 | Major depressive disorder | [23] | |
11 | MN-305 | Drug Info | Phase 2 | Mood disorder | [24] | |
12 | Neu-P11 | Drug Info | Phase 2 | Insomnia | [25] | |
13 | OPC-14523 | Drug Info | Phase 2 | Mood disorder | [26] | |
14 | ORG-13011 | Drug Info | Phase 2 | Psychotic disorder | [27] | |
15 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [28] | |
16 | S-15535 | Drug Info | Phase 2 | Anxiety disorder | [29], [30] | |
17 | S-16924 | Drug Info | Phase 2 | Anxiety disorder | [31], [32], [33] | |
18 | SDZ-MAR-327 | Drug Info | Phase 2 | Psychotic disorder | [34], [35] | |
19 | SUN N4057 | Drug Info | Phase 2 | Coronary artery disease | [36] | |
20 | TGBA01AD | Drug Info | Phase 2 | Mood disorder | [24] | |
21 | TGFK08AA | Drug Info | Phase 2 | Generalized anxiety disorder | [37] | |
22 | TGFK09SD | Drug Info | Phase 2 | Hypoactive sexual desire dysfunction | [38] | |
23 | TGWOOAA | Drug Info | Phase 2 | Social phobia | [39] | |
24 | Zalospirone | Drug Info | Phase 2 | Anxiety disorder | [40], [41] | |
25 | 1192U90 | Drug Info | Phase 1 | Psychotic disorder | [42] | |
26 | AV-965 | Drug Info | Phase 1 | Alzheimer disease | [43] | |
27 | DSP-1053 | Drug Info | Phase 1 | Major depressive disorder | [44] | |
28 | GSK-958108 | Drug Info | Phase 1 | Premature ejaculation | [45] | |
29 | NLX-101 | Drug Info | Phase 1 | Rett syndrome | [46] | |
30 | SKL-PSY | Drug Info | Phase 1 | Bipolar disorder | [47] | |
31 | SSR-181507 | Drug Info | Phase 1 | Schizophrenia | [34] | |
32 | Umespirone | Drug Info | Phase 1 | Anxiety disorder | [48] | |
Patented Agent(s) | [+] 5 Patented Agents | + | ||||
1 | PMID30124346-Compound-13TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [49] | |
2 | PMID30124346-Compound-34TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [49] | |
3 | PMID30124346-Compound-60TABLE5 | Drug Info | Patented | Parkinson disease | [49], [50], [51] | |
4 | PMID30124346-Compound-LDT66 | Drug Info | Patented | Benign prostatic hyperplasia | [49] | |
5 | PMID30124346-Compound-LDT8 | Drug Info | Patented | Benign prostatic hyperplasia | [49] | |
Discontinued Drug(s) | [+] 36 Discontinued Drugs | + | ||||
1 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | Withdrawn from market | Addictive disorder | [52], [53] | |
2 | Bifeprunox | Drug Info | Discontinued in Phase 3 | Schizophrenia | [34] | |
3 | BMS-181100 | Drug Info | Discontinued in Phase 3 | Psychotic disorder | [54], [55] | |
4 | Flesinoxan | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [56], [57] | |
5 | Adatanserin | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
6 | ALNESPIRONE | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [58] | |
7 | AP-521 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [59] | |
8 | DU 125530 | Drug Info | Discontinued in Phase 2 | Mood disorder | [60] | |
9 | GSK163090 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [61] | |
10 | LESOPITRON DIHYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Mood disorder | [62] | |
11 | PRX-00023 | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
12 | REC-15/3079 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [63], [64] | |
13 | Robalzotan | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [65], [66] | |
14 | BINOSPIRONE MESYLATE | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [67] | |
15 | DU-29894 | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [68] | |
16 | E2101 | Drug Info | Discontinued in Phase 1 | Spasm | [69] | |
17 | Ebalzotan | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [70] | |
18 | Eptapirone | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [71] | |
19 | GR-127607 | Drug Info | Discontinued in Phase 1 | Migraine | [72] | |
20 | Nerisopam | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [73] | |
21 | SLV-313 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [34] | |
22 | SUN-8399 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [74] | |
23 | U-93385 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [75] | |
24 | A-74283 | Drug Info | Terminated | Hypertension | [77] | |
25 | Anpirtoline | Drug Info | Terminated | Pain | [78] | |
26 | BTS-79018 | Drug Info | Terminated | Schizophrenia | [34] | |
27 | CGS-18102A | Drug Info | Terminated | Anxiety disorder | [79] | |
28 | Du-123015 | Drug Info | Terminated | Anxiety disorder | [80] | |
29 | Gepirone | Drug Info | Terminated | Depression | [24] | |
30 | HT-90B | Drug Info | Terminated | Anxiety disorder | [81] | |
31 | Ipsapirone | Drug Info | Terminated | Anxiety disorder | [82], [83] | |
32 | LY-293284 | Drug Info | Terminated | Anxiety disorder | [84], [85] | |
33 | RWJ-25730 | Drug Info | Terminated | Psychotic disorder | [86] | |
34 | S-14506 | Drug Info | Terminated | Anxiety disorder | [87], [88] | |
35 | SLV-307 | Drug Info | Terminated | Parkinson disease | [89] | |
36 | WAY-100635 | Drug Info | Terminated | Eating disorder | [90], [91] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | CM-2236 | Drug Info | Preclinical | Post-traumatic stress disorder | [76] | |
2 | PD-158771 | Drug Info | Preclinical | Schizophrenia | [34] | |
Mode of Action | [+] 7 Modes of Action | + | ||||
Agonist | [+] 50 Agonist drugs | + | ||||
1 | Buspirone | Drug Info | [1] | |||
2 | Urapidil | Drug Info | [97] | |||
3 | CM-2395 | Drug Info | [98] | |||
4 | Eltoprazine | Drug Info | [99] | |||
5 | SEP-363856 | Drug Info | [20] | |||
6 | MN-305 | Drug Info | [24] | |||
7 | Neu-P11 | Drug Info | [105] | |||
8 | SUN N4057 | Drug Info | [113] | |||
9 | Zalospirone | Drug Info | [41] | |||
10 | 1192U90 | Drug Info | [34] | |||
11 | Aryl piperazine derivative 14 | Drug Info | [49] | |||
12 | Aryl piperazine derivative 15 | Drug Info | [49] | |||
13 | Aryl piperazine derivative 16 | Drug Info | [49] | |||
14 | PMID30124346-Compound-13TABLE4 | Drug Info | [49] | |||
15 | Flesinoxan | Drug Info | [129] | |||
16 | Adatanserin | Drug Info | [24], [132] | |||
17 | ALNESPIRONE | Drug Info | [133], [9] | |||
18 | AP-521 | Drug Info | [134], [9] | |||
19 | LESOPITRON DIHYDROCHLORIDE | Drug Info | [136] | |||
20 | Ebalzotan | Drug Info | [144] | |||
21 | Eptapirone | Drug Info | [145] | |||
22 | GR-127607 | Drug Info | [146] | |||
23 | Nerisopam | Drug Info | [147] | |||
24 | SUN-8399 | Drug Info | [149] | |||
25 | U-93385 | Drug Info | [150], [9] | |||
26 | CM-2236 | Drug Info | [151] | |||
27 | A-74283 | Drug Info | [152] | |||
28 | Gepirone | Drug Info | [24] | |||
29 | Ipsapirone | Drug Info | [159] | |||
30 | LY-293284 | Drug Info | [160] | |||
31 | 1-naphthylpiperazine | Drug Info | [184], [173] | |||
32 | 5-CT | Drug Info | [199] | |||
33 | 7-methoxy-1-naphthylpiperazine | Drug Info | [184] | |||
34 | BRL-15572 | Drug Info | [203] | |||
35 | CP 93129 | Drug Info | [199] | |||
36 | EDMT | Drug Info | [206] | |||
37 | FG-5893 | Drug Info | [210] | |||
38 | L-772,405 | Drug Info | [212] | |||
39 | LP-12 | Drug Info | [213] | |||
40 | LP-211 | Drug Info | [214] | |||
41 | LP-44 | Drug Info | [213] | |||
42 | LY 165,163 | Drug Info | [210] | |||
43 | nafadotride | Drug Info | [210] | |||
44 | piribedil | Drug Info | [221] | |||
45 | S-14671 | Drug Info | [111] | |||
46 | SB 216641 | Drug Info | [203] | |||
47 | spiroxatrine | Drug Info | [210] | |||
48 | U92016A | Drug Info | [231] | |||
49 | [3H]8-OH-DPAT | Drug Info | [236] | |||
50 | [3H]NLX-112 | Drug Info | [237] | |||
Modulator | [+] 34 Modulator drugs | + | ||||
1 | Flibanserin | Drug Info | [5] | |||
2 | OPC-34712 | Drug Info | [92], [93] | |||
3 | Trazodone | Drug Info | [95] | |||
4 | Vilazodone | Drug Info | [14] | |||
5 | Sarizotan | Drug Info | [102] | |||
6 | Ensaculin hydrochloride | Drug Info | [21], [103] | |||
7 | FKB01MD | Drug Info | [16] | |||
8 | Mazapertine succinate | Drug Info | [102] | |||
9 | OPC-14523 | Drug Info | [106] | |||
10 | S-16924 | Drug Info | [32], [33] | |||
11 | SDZ-MAR-327 | Drug Info | [112] | |||
12 | TGBA01AD | Drug Info | [114] | |||
13 | TGFK08AA | Drug Info | [115] | |||
14 | TGFK09SD | Drug Info | [116] | |||
15 | NLX-101 | Drug Info | [121] | |||
16 | SKL-PSY | Drug Info | [122] | |||
17 | SSR-181507 | Drug Info | [123] | |||
18 | Bifeprunox | Drug Info | [126] | |||
19 | BMS-181100 | Drug Info | [127], [128] | |||
20 | PRX-00023 | Drug Info | [138] | |||
21 | DU-29894 | Drug Info | [142] | |||
22 | E2101 | Drug Info | [143] | |||
23 | SLV-313 | Drug Info | [148] | |||
24 | Anpirtoline | Drug Info | [78] | |||
25 | CGS-18102A | Drug Info | [155] | |||
26 | Du-123015 | Drug Info | [157] | |||
27 | HT-90B | Drug Info | [158] | |||
28 | RWJ-25730 | Drug Info | [162] | |||
29 | S-14506 | Drug Info | [163] | |||
30 | CGS-19480A | Drug Info | [204], [9] | |||
31 | EMD 56551 | Drug Info | [207] | |||
32 | NPT-500 | Drug Info | [122] | |||
33 | SEL-73 | Drug Info | [122] | |||
34 | SR-59026 | Drug Info | [230] | |||
Inhibitor | [+] 142 Inhibitor drugs | + | ||||
1 | TERTATOLOL | Drug Info | [94] | |||
2 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | [125] | |||
3 | Sunepitron | Drug Info | [130] | |||
4 | TIOSPIRONE | Drug Info | [131] | |||
5 | MAZAPERTINE | Drug Info | [137] | |||
6 | A-80426 | Drug Info | [153] | |||
7 | BMY-7378 | Drug Info | [154] | |||
8 | CP-293019 | Drug Info | [156] | |||
9 | WB-4101 | Drug Info | [168] | |||
10 | (3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | [169] | |||
11 | (R)-(-)-10-methyl-11-hydroxyaporphine | Drug Info | [170] | |||
12 | (R)-11-Amino-2-methoxyaporphine | Drug Info | [171] | |||
13 | (R)-2,11-Diaminoaporphine | Drug Info | [171] | |||
14 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [173] | |||
15 | 1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane | Drug Info | [174] | |||
16 | 1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane | Drug Info | [174] | |||
17 | 1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane | Drug Info | [174] | |||
18 | 1,6-bis(4-m-tolylpiperazin-1-yl)hexane | Drug Info | [174] | |||
19 | 1,6-bis(4-phenylpiperazin-1-yl)hexane | Drug Info | [174] | |||
20 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [175] | |||
21 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [169] | |||
22 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [169] | |||
23 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [176] | |||
24 | 1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine | Drug Info | [177] | |||
25 | 1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine | Drug Info | [178] | |||
26 | 1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | [177] | |||
27 | 1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | [177] | |||
28 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [177] | |||
29 | 1-(2-(benzyloxy)phenyl)piperazine | Drug Info | [177] | |||
30 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [177] | |||
31 | 1-(2-Butoxy-phenyl)-piperazine | Drug Info | [179] | |||
32 | 1-(2-Chloro-phenyl)-piperazine | Drug Info | [180] | |||
33 | 1-(2-Ethoxy-phenyl)-piperazine | Drug Info | [179] | |||
34 | 1-(2-Fluoro-phenyl)-piperazine | Drug Info | [179] | |||
35 | 1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | [179] | |||
36 | 1-(2-Methoxy-phenyl)-4-propyl-piperazine | Drug Info | [181] | |||
37 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [180] | |||
38 | 1-(2-methoxyphenyl)-4-pentylpiperazine | Drug Info | [182] | |||
39 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [177] | |||
40 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [183] | |||
41 | 1-(3-Fluoro-phenyl)-piperazine | Drug Info | [179] | |||
42 | 1-(3-Nitro-phenyl)-piperazine | Drug Info | [179] | |||
43 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [169] | |||
44 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [184] | |||
45 | 1-(benzyloxy)-2-(2-phenylethyl)benzene | Drug Info | [185] | |||
46 | 1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene | Drug Info | [185] | |||
47 | 1-Benzyl-4-chroman-2-ylmethyl-piperazine | Drug Info | [186] | |||
48 | 1-Butyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [181] | |||
49 | 1-Ethyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [181] | |||
50 | 1-Methyl-1,3-dihydro-indol-2-one | Drug Info | [187] | |||
51 | 1-Naphthalen-2-yl-piperazine | Drug Info | [173] | |||
52 | 1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [188] | |||
53 | 1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene | Drug Info | [185] | |||
54 | 2-(2'-methyl-biphenyl-3-yl)-ethylamine | Drug Info | [189] | |||
55 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [176] | |||
56 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
57 | 2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
58 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
59 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
60 | 2-(3-Bromophenylthio)-N,N-dimethylethanamine | Drug Info | [190] | |||
61 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
62 | 2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [186] | |||
63 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
64 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
65 | 2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine | Drug Info | [191] | |||
66 | 2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | [192] | |||
67 | 2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine | Drug Info | [190] | |||
68 | 2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol | Drug Info | [94] | |||
69 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
70 | 2-Piperazin-1-yl-benzonitrile | Drug Info | [179] | |||
71 | 2-Piperazin-1-yl-phenol | Drug Info | [169] | |||
72 | 2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [185] | |||
73 | 3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole | Drug Info | [193] | |||
74 | 3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | [188] | |||
75 | 3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | [192] | |||
76 | 3-(2-Benzylamino-ethoxy)-phenol | Drug Info | [194] | |||
77 | 3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine | Drug Info | [188] | |||
78 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [186] | |||
79 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one | Drug Info | [186] | |||
80 | 3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | [178] | |||
81 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [169] | |||
82 | 3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [195] | |||
83 | 3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [195] | |||
84 | 3-Naphthalen-1-yl-1-propyl-pyrrolidine | Drug Info | [188] | |||
85 | 3-Naphthalen-1-yl-pyrrolidine | Drug Info | [188] | |||
86 | 3-Phenyl-1-propyl-pyrrolidine | Drug Info | [188] | |||
87 | 3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [185] | |||
88 | 4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol | Drug Info | [196] | |||
89 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [177] | |||
90 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [177] | |||
91 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
92 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
93 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [177] | |||
94 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
95 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [177] | |||
96 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [177] | |||
97 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [177] | |||
98 | 4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
99 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
100 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
101 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [177] | |||
102 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [177] | |||
103 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [177] | |||
104 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [197] | |||
105 | 4-Benzyl-1-chroman-2-ylmethyl-piperidine | Drug Info | [186] | |||
106 | 4-Benzyl-1-chroman-3-ylmethyl-piperidine | Drug Info | [186] | |||
107 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
108 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
109 | 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
110 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
111 | 8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine | Drug Info | [94] | |||
112 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [173] | |||
113 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [173] | |||
114 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
115 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [173] | |||
116 | 9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine | Drug Info | [94] | |||
117 | A-987306 | Drug Info | [201] | |||
118 | AGROCLAVINE | Drug Info | [202] | |||
119 | Brolamfetamine | Drug Info | [176] | |||
120 | CHLOROPHENYLPIPERAZINE | Drug Info | [179] | |||
121 | ESCHOLTZINE | Drug Info | [208] | |||
122 | Etisulergine | Drug Info | [209] | |||
123 | JNJ-10392980 | Drug Info | [211] | |||
124 | MCL-516 | Drug Info | [171] | |||
125 | N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine | Drug Info | [196] | |||
126 | N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine | Drug Info | [196] | |||
127 | N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide | Drug Info | [214] | |||
128 | N-methyllaurotetanine | Drug Info | [208] | |||
129 | N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide | Drug Info | [216] | |||
130 | PB-28 | Drug Info | [219] | |||
131 | PG-01037 | Drug Info | [220] | |||
132 | PHENYLPIPERAZINE | Drug Info | [173] | |||
133 | QUIPAZINE | Drug Info | [222] | |||
134 | SB-271046 | Drug Info | [227] | |||
135 | SB-656104 | Drug Info | [228] | |||
136 | SEROTONIN | Drug Info | [222] | |||
137 | SNAP-8719 | Drug Info | [229] | |||
138 | TFMPP | Drug Info | [169] | |||
139 | UH-232 | Drug Info | [232] | |||
140 | UH-301 | Drug Info | [233] | |||
141 | WAY-466 | Drug Info | [234] | |||
142 | [3H]spiperone | Drug Info | [168] | |||
Antagonist | [+] 41 Antagonist drugs | + | ||||
1 | Treximet | Drug Info | [96] | |||
2 | Xaliproden | Drug Info | [100] | |||
3 | LECOZOTAN HYDROCHLORIDE | Drug Info | [9], [101] | |||
4 | FKW00GA | Drug Info | [16] | |||
5 | MIN-117 | Drug Info | [104] | |||
6 | ORG-13011 | Drug Info | [9], [107] | |||
7 | RP5063 | Drug Info | [108], [109] | |||
8 | S-15535 | Drug Info | [9], [110], [111] | |||
9 | TGWOOAA | Drug Info | [117] | |||
10 | AV-965 | Drug Info | [118] | |||
11 | DSP-1053 | Drug Info | [119] | |||
12 | GSK-958108 | Drug Info | [120] | |||
13 | Umespirone | Drug Info | [124] | |||
14 | PMID30124346-Compound-LDT8 | Drug Info | [49] | |||
15 | DU 125530 | Drug Info | [135] | |||
16 | GSK163090 | Drug Info | [96] | |||
17 | REC-15/3079 | Drug Info | [139] | |||
18 | Robalzotan | Drug Info | [140] | |||
19 | BINOSPIRONE MESYLATE | Drug Info | [141], [9] | |||
20 | PD-158771 | Drug Info | [34] | |||
21 | NAN-190 | Drug Info | [161] | |||
22 | SDZ 216-525 | Drug Info | [161] | |||
23 | SLV-307 | Drug Info | [164] | |||
24 | WAY-100635 | Drug Info | [135], [165], [166], [167] | |||
25 | (R)-flurocarazolol | Drug Info | [172] | |||
26 | (S)-flurocarazolol | Drug Info | [172] | |||
27 | 9-OH-risperidone | Drug Info | [200] | |||
28 | cyamemazine | Drug Info | [205] | |||
29 | GR 125,743 | Drug Info | [199] | |||
30 | LY433221 | Drug Info | [215] | |||
31 | MPDT | Drug Info | [206] | |||
32 | P-MPPI | Drug Info | [217], [161] | |||
33 | p-[18F]MPPF | Drug Info | [218] | |||
34 | repinotan | Drug Info | [223] | |||
35 | SB 272183 | Drug Info | [225] | |||
36 | SB 649915 | Drug Info | [226] | |||
37 | SB 714786 | Drug Info | [226] | |||
38 | WAY 100135 | Drug Info | [161] | |||
39 | [11C]WAY100635 | Drug Info | [235] | |||
40 | [3H]p-MPPF | Drug Info | [238] | |||
41 | [3H]robalzotan | Drug Info | [239] | |||
Ligand | [+] 4 Ligand drugs | + | ||||
1 | Aryl piperazine derivative 1 | Drug Info | [49] | |||
2 | Aryl piperazine derivative 6 | Drug Info | [49] | |||
3 | PMID30124346-Compound-34TABLE4 | Drug Info | [49] | |||
4 | PMID30124346-Compound-60TABLE5 | Drug Info | [49] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | BTS-79018 | Drug Info | [34] | |||
Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
1 | RS-30199 | Drug Info | [224] |
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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