Target Information
Target General Information | Top | |||||
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Target ID |
T64765
(Former ID: TTDC00079)
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Target Name |
Histamine H3 receptor (H3R)
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Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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Gene Name |
HRH3
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Somnolence [ICD-11: MG42] | |||||
Function |
Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). Agonist stimulation of isoform 3 neither modified adenylate cyclase activity nor induced intracellular calcium mobilization. The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR RAFTKLLCPQKLKIQPHSSLEHCWK Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T88AHJ |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Pitolisant | Drug Info | Approved | Excessive daytime sleepiness | [2] | |
Clinical Trial Drug(s) | [+] 17 Clinical Trial Drugs | + | ||||
1 | SUVN-G3031 | Drug Info | Phase 3 | Cognitive impairment | [3], [4] | |
2 | ABT-288 | Drug Info | Phase 2 | Alzheimer disease | [5], [6] | |
3 | ABT-652 | Drug Info | Phase 2 | Musculoskeletal pain | [7] | |
4 | AZD-5213 | Drug Info | Phase 2 | Alzheimer disease | [8] | |
5 | Bavisant | Drug Info | Phase 2 | Attention deficit hyperactivity disorder | [9] | |
6 | GSK239512 | Drug Info | Phase 2 | Dementia | [10] | |
7 | JNJ-17216498 | Drug Info | Phase 2 | Narcolepsy | [11] | |
8 | JNJ-39220675 | Drug Info | Phase 2 | Alcohol dependence | [12] | |
9 | S-38093 | Drug Info | Phase 2 | Alzheimer disease | [13] | |
10 | SAR-110894 | Drug Info | Phase 2 | Alzheimer disease | [14] | |
11 | ABT-239 | Drug Info | Phase 1 | Cognitive impairment | [15], [16] | |
12 | APD-916 | Drug Info | Phase 1 | Sleep-wake disorder | [17] | |
13 | HPP404 | Drug Info | Phase 1 | Allergic rhinitis | [18] | |
14 | Irdabisant | Drug Info | Phase 1 | Cognitive impairment | [19] | |
15 | MK-3134 | Drug Info | Phase 1 | Dementia | [20] | |
16 | MK-7288 | Drug Info | Phase 1 | Excessive daytime sleepiness | [21] | |
17 | MK-0249 | Drug Info | Clinical trial | Insulin-resistant disorder | [22] | |
Patented Agent(s) | [+] 9 Patented Agents | + | ||||
1 | Biphenyl derivative 4 | Drug Info | Patented | Histamine H3-associated disorder | [23] | |
2 | Phenylsulfonyl derivative 1 | Drug Info | Patented | Central nervous system disease | [23] | |
3 | Phenylsulfonyl derivative 2 | Drug Info | Patented | Central nervous system disease | [23] | |
4 | Phenylsulfonyl derivative 3 | Drug Info | Patented | Central nervous system disease | [23] | |
5 | Phenylsulfonyl derivative 4 | Drug Info | Patented | Central nervous system disease | [23] | |
6 | PMID29334795-Compound-21 | Drug Info | Patented | Progressive supranuclear palsy | [23] | |
7 | PMID29334795-Compound-22 | Drug Info | Patented | Neuropathic pain | [23] | |
8 | PMID29334795-Compound-23 | Drug Info | Patented | Schizophrenia | [23] | |
9 | PMID29334795-Compound-28 | Drug Info | Patented | Histamine H3-associated disorder | [23] | |
Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
1 | BP-2.94 | Drug Info | Discontinued in Phase 2 | Pain | [24] | |
2 | Cipralisant | Drug Info | Discontinued in Phase 2 | Attention deficit hyperactivity disorder | [25], [26] | |
3 | GSK835726 | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [27] | |
4 | GSK1004723 | Drug Info | Discontinued in Phase 1 | Allergic rhinitis | [28] | |
5 | SAR-152954 | Drug Info | Discontinued in Phase 1 | Sleep-wake disorder | [29] | |
6 | GT-2016 | Drug Info | Terminated | Alzheimer disease | [30] | |
7 | GT-2203 | Drug Info | Terminated | Anxiety disorder | [31] | |
8 | Thioperamide | Drug Info | Terminated | Cognitive impairment | [32], [33] | |
9 | UCL-1390 | Drug Info | Terminated | Pain | [34] | |
Mode of Action | [+] 8 Modes of Action | + | ||||
Agonist | [+] 19 Agonist drugs | + | ||||
1 | Pitolisant | Drug Info | [2] | |||
2 | MK-3134 | Drug Info | [47] | |||
3 | MK-7288 | Drug Info | [48] | |||
4 | MK-0249 | Drug Info | [49] | |||
5 | GT-2203 | Drug Info | [54] | |||
6 | (R)-alpha-methylhistamine | Drug Info | [16], [61], [62] | |||
7 | (S)-alpha-methylhistamine | Drug Info | [63] | |||
8 | imbutamine | Drug Info | [86] | |||
9 | Imetit | Drug Info | [16] | |||
10 | Immepip | Drug Info | [16] | |||
11 | Immethridine | Drug Info | [16] | |||
12 | impentamine | Drug Info | [86] | |||
13 | impromidine | Drug Info | [62] | |||
14 | Methimepip | Drug Info | [16] | |||
15 | N-methylhistamine | Drug Info | [62] | |||
16 | N-[3H]alpha-methylhistamine | Drug Info | [89] | |||
17 | N-[3H]methylhistamine | Drug Info | [62] | |||
18 | VUF 5207 | Drug Info | [90] | |||
19 | VUF 8328 | Drug Info | [90] | |||
Antagonist | [+] 43 Antagonist drugs | + | ||||
1 | SUVN-G3031 | Drug Info | [3], [4] | |||
2 | AZD-5213 | Drug Info | [37] | |||
3 | Bavisant | Drug Info | [38] | |||
4 | GSK239512 | Drug Info | [39] | |||
5 | JNJ-17216498 | Drug Info | [40] | |||
6 | JNJ-39220675 | Drug Info | [41] | |||
7 | S-38093 | Drug Info | [42] | |||
8 | SAR-110894 | Drug Info | [37] | |||
9 | ABT-239 | Drug Info | [16], [43], [44] | |||
10 | APD-916 | Drug Info | [45] | |||
11 | HPP404 | Drug Info | [18] | |||
12 | Irdabisant | Drug Info | [46] | |||
13 | GSK835726 | Drug Info | [39] | |||
14 | GSK1004723 | Drug Info | [39] | |||
15 | SAR-152954 | Drug Info | [52] | |||
16 | Thioperamide | Drug Info | [16], [55] | |||
17 | UCL-1390 | Drug Info | [26] | |||
18 | A-304121 | Drug Info | [80] | |||
19 | A-317920 | Drug Info | [16] | |||
20 | A-331440 | Drug Info | [16] | |||
21 | ATH-90879 | Drug Info | [54] | |||
22 | burimamide | Drug Info | [62] | |||
23 | Ciproxifan | Drug Info | [16] | |||
24 | Clobenpropit | Drug Info | [16], [55] | |||
25 | EVT-501 | Drug Info | [54] | |||
26 | FUB 349 | Drug Info | [85], [76] | |||
27 | FUB-130 | Drug Info | [54] | |||
28 | GSK-334429 | Drug Info | [54] | |||
29 | GSK189254A | Drug Info | [16] | |||
30 | GT2394 | Drug Info | [63] | |||
31 | JB 98064 | Drug Info | [63] | |||
32 | JNJ-5207852 | Drug Info | [16] | |||
33 | PF-3900422 | Drug Info | [54] | |||
34 | Proxyfan | Drug Info | [16] | |||
35 | SCH79687 | Drug Info | [16] | |||
36 | SUVN-G1031 | Drug Info | [54] | |||
37 | UCB-2892 | Drug Info | [54] | |||
38 | UCL1972 | Drug Info | [16] | |||
39 | VUF 4904 | Drug Info | [90] | |||
40 | VUF 5681 | Drug Info | [16] | |||
41 | VUF5391 | Drug Info | [16] | |||
42 | [123I]iodoproxyfan | Drug Info | [85] | |||
43 | [125I]iodophenpropit | Drug Info | [92] | |||
Modulator | [+] 3 Modulator drugs | + | ||||
1 | ABT-288 | Drug Info | [35] | |||
2 | ABT-652 | Drug Info | [36] | |||
3 | BP-2.94 | Drug Info | [50] | |||
Inhibitor | [+] 118 Inhibitor drugs | + | ||||
1 | Benzo[d]oxazol-2(3H)-one derivative 1 | Drug Info | [23] | |||
2 | Benzo[d]oxazol-2(3H)-one derivative 2 | Drug Info | [23] | |||
3 | Benzo[d]oxazol-2(3H)-one derivative 3 | Drug Info | [23] | |||
4 | Phenylsulfonyl derivative 1 | Drug Info | [23] | |||
5 | Phenylsulfonyl derivative 2 | Drug Info | [23] | |||
6 | Phenylsulfonyl derivative 3 | Drug Info | [23] | |||
7 | Phenylsulfonyl derivative 4 | Drug Info | [23] | |||
8 | PMID29334795-Compound-62 | Drug Info | [23] | |||
9 | PMID29334795-Compound-66 | Drug Info | [23] | |||
10 | PMID29334795-Compound-67 | Drug Info | [23] | |||
11 | GR-175737 | Drug Info | [53] | |||
12 | GT-2016 | Drug Info | [53] | |||
13 | (1H-indol-2-yl)(piperazin-1-yl)methanone | Drug Info | [56] | |||
14 | (1R,2R)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine | Drug Info | [57] | |||
15 | (1R,2S)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine | Drug Info | [57] | |||
16 | (1S,2S)-2-(1H-Imidazol-4-yl)-cyclopentylamine | Drug Info | [57] | |||
17 | (R)-1-(2-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
18 | (R)-1-(3-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
19 | (R)-1-(4-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
20 | (R)-1-(4-nitrophenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
21 | (R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol | Drug Info | [58] | |||
22 | (R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
23 | (R)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
24 | (R)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
25 | (R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate | Drug Info | [59] | |||
26 | (R)-3-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
27 | (R)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
28 | (R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline | Drug Info | [60] | |||
29 | (S)-1-(2-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
30 | (S)-1-(3-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
31 | (S)-1-(4-methoxyphenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
32 | (S)-1-(4-nitrophenethyl)-2-methylpyrrolidine | Drug Info | [58] | |||
33 | (S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol | Drug Info | [58] | |||
34 | (S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
35 | (S)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
36 | (S)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
37 | (S)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate | Drug Info | [59] | |||
38 | (S)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
39 | 1-(2-(naphthalen-2-yl)ethyl)pyrrolidine | Drug Info | [58] | |||
40 | 1-(2-m-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
41 | 1-(2-methoxyphenethyl)pyrrolidine | Drug Info | [58] | |||
42 | 1-(2-p-tolyl-ethyl)-pyrrolidine | Drug Info | [58] | |||
43 | 1-(3-(2-(3-methoxyphenoxy)ethoxy)propyl)azepane | Drug Info | [64] | |||
44 | 1-(3-(3-phenylpropoxy)propyl)piperidine | Drug Info | [65] | |||
45 | 1-(3-(4-(2-fluoroethyl)phenoxy)propyl)piperidine | Drug Info | [66] | |||
46 | 1-(3-(4-(fluoromethyl)phenoxy)propyl)piperidine | Drug Info | [66] | |||
47 | 1-(3-methoxyphenethyl)pyrrolidine | Drug Info | [58] | |||
48 | 1-(4-(benzyloxy)phenethyl)pyrrolidine | Drug Info | [58] | |||
49 | 1-(4-methoxyphenethyl)pyrrolidine | Drug Info | [58] | |||
50 | 1-(4-nitrophenethyl)pyrrolidine | Drug Info | [58] | |||
51 | 1-[2-(2,4,6-trimethyl-phenyl)-ethyl]-pyrrolidine | Drug Info | [58] | |||
52 | 2-((1H-imidazol-4-yl)methyl)pyridine | Drug Info | [67] | |||
53 | 2-((2-ethoxyphenoxy)methyl)-4-isopropylmorpholine | Drug Info | [68] | |||
54 | 2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridine | Drug Info | [69] | |||
55 | 2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridine | Drug Info | [69] | |||
56 | 2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole | Drug Info | [67] | |||
57 | 2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole | Drug Info | [58] | |||
58 | 2-(2-(pyrrolidin-1-yl)ethyl)phenol | Drug Info | [58] | |||
59 | 2-(2-(pyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
60 | 2-(3-Methyl-3H-imidazol-4-yl)-ethylamine | Drug Info | [53] | |||
61 | 2-(4-Cyclopentyl-piperazin-1-yl)-quinoline | Drug Info | [70] | |||
62 | 2-(4-Cyclopropyl-piperazin-1-yl)-quinoline | Drug Info | [70] | |||
63 | 2-(4-Isopropyl-piperazin-1-yl)-quinoline | Drug Info | [70] | |||
64 | 2-(4-Methyl-piperazin-1-yl)-quinoline | Drug Info | [70] | |||
65 | 2-(4-Propyl-piperazin-1-yl)-quinoline | Drug Info | [70] | |||
66 | 2-(ethoxycarbonyl)-1H-indole-5-carboxylic acid | Drug Info | [71] | |||
67 | 2-[2-(1H-Imidazol-4-yl)-cyclopropyl]-ethylamine | Drug Info | [72] | |||
68 | 2-[4-(1-Ethyl-propyl)-piperazin-1-yl]-quinoline | Drug Info | [70] | |||
69 | 3-((1H-imidazol-4-yl)methyl)pyridine | Drug Info | [67] | |||
70 | 4-((1H-imidazol-4-yl)methyl)-1-heptylpiperidine | Drug Info | [73] | |||
71 | 4-((1H-Imidazol-4-yl)methyl)-1-phenylpiperidine | Drug Info | [74] | |||
72 | 4-((2R,3S)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole | Drug Info | [57] | |||
73 | 4-((2S,3R)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole | Drug Info | [57] | |||
74 | 4-(2-(3,4-Dimethylphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
75 | 4-(2-(3-tert-Butylphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
76 | 4-(2-(4-Cyclohexylphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
77 | 4-(2-(4-Methoxyphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
78 | 4-(2-(4-Methylphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
79 | 4-(2-(4-tert-Butylphenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
80 | 4-(2-(Cyclohexylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
81 | 4-(2-(Phenylamino)ethyl)-1H-imidazole | Drug Info | [75] | |||
82 | 4-(2-(pyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
83 | 4-(3-Phenoxy-propyl)-1H-imidazole | Drug Info | [76] | |||
84 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [77] | |||
85 | 4-(6-Cyclohexyl-hex-3-ynyl)-1H-imidazole | Drug Info | [53] | |||
86 | 4-(6-Cyclopentyl-hex-3-ynyl)-1H-imidazole | Drug Info | [53] | |||
87 | 4-(7,7-Dimethyl-oct-3-ynyl)-1H-imidazole | Drug Info | [53] | |||
88 | 4-(7-Methyl-oct-3-ynyl)-1H-imidazole | Drug Info | [53] | |||
89 | 4-(8-Phenyl-oct-3-ynyl)-1H-imidazole | Drug Info | [53] | |||
90 | 4-Benzyl-1-[3-phenylpropoxy)propyl]piperidine | Drug Info | [65] | |||
91 | 4-Butyl-1-[3-(phenylpropoxy)propyl]piperidine | Drug Info | [65] | |||
92 | 4-Hept-3-ynyl-1H-imidazole | Drug Info | [53] | |||
93 | 4-Hex-3-ynyl-1H-imidazole | Drug Info | [53] | |||
94 | 4-isopropyl-2-(phenoxymethyl)morpholine | Drug Info | [68] | |||
95 | 4-Propyl-1-[3-(phenylpropoxy)propyl]piperidine | Drug Info | [65] | |||
96 | 4-[3-(4-Butyl-phenoxy)-propyl]-1H-imidazole | Drug Info | [78] | |||
97 | 4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole | Drug Info | [78] | |||
98 | 4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole | Drug Info | [76] | |||
99 | 5-(2-(pyrrolidin-1-yl)ethyl)isothiazole | Drug Info | [58] | |||
100 | 5-ethyl-2-(2-(pyrrolidin-1-yl)ethyl)pyridine | Drug Info | [58] | |||
101 | 5-methoxy-2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole | Drug Info | [58] | |||
102 | 5-phenyl-2-(4-(piperidin-1-yl)butyl)oxazole | Drug Info | [79] | |||
103 | Aerophobin-1 | Drug Info | [81] | |||
104 | APLYSAMINE | Drug Info | [82] | |||
105 | C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine | Drug Info | [72] | |||
106 | CARCININE | Drug Info | [82] | |||
107 | CONESSINE | Drug Info | [83] | |||
108 | Des-bromoaplysamine-1 | Drug Info | [84] | |||
109 | IODOPROXYFAN | Drug Info | [76] | |||
110 | JNJ-28583867 | Drug Info | [87] | |||
111 | N-benzyl-4-cyclopentylpiperazine-1-carboxamide | Drug Info | [88] | |||
112 | N-methyl-2-(pyridin-2-yl)ethanamine | Drug Info | [71] | |||
113 | ST-1025 | Drug Info | [79] | |||
114 | ST-1093 | Drug Info | [79] | |||
115 | UCL-2138 | Drug Info | [66] | |||
116 | Verongamine | Drug Info | [81] | |||
117 | VUF-10214 | Drug Info | [91] | |||
118 | VUF-5297 | Drug Info | [72] | |||
Ligand | [+] 9 Ligand drugs | + | ||||
1 | Piperazine carbamate/urea derivative 1 | Drug Info | [23] | |||
2 | Piperazine carbamate/urea derivative 2 | Drug Info | [23] | |||
3 | Piperazine carbamate/urea derivative 3 | Drug Info | [23] | |||
4 | Piperazine carbamate/urea derivative 4 | Drug Info | [23] | |||
5 | Piperazine carbamate/urea derivative 5 | Drug Info | [23] | |||
6 | Piperazine carbamate/urea derivative 6 | Drug Info | [23] | |||
7 | Piperazine carbamate/urea derivative 7 | Drug Info | [23] | |||
8 | Triazolo-benzodiazepine derivative 1 | Drug Info | [23] | |||
9 | Triazolo-benzodiazepine derivative 2 | Drug Info | [23] | |||
Agonis; Inverse agonist | [+] 1 Agonis; Inverse agonist drugs | + | ||||
1 | PMID29334795-Compound-22 | Drug Info | [23] | |||
Inverse agonist | [+] 4 Inverse agonist drugs | + | ||||
1 | PMID29334795-Compound-23 | Drug Info | [23] | |||
2 | PMID29334795-Compound-24 | Drug Info | [23] | |||
3 | PMID29334795-Compound-25 | Drug Info | [23] | |||
4 | Pyridazin-3(2H)-one derivative 1 | Drug Info | [23] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | Cipralisant | Drug Info | [51] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Histamine receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 4 WikiPathways | + | ||||
1 | Monoamine Transport | |||||
2 | GPCRs, Class A Rhodopsin-like | |||||
3 | GPCR ligand binding | |||||
4 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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REF 1 | Effects of pitolisant, a histamine H3 inverse agonist, in drug-resistant idiopathic and symptomatic hypersomnia: a chart review. Sleep Med. 2014 Jun;15(6):681-7. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 4 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6927). | |||||
REF 6 | ClinicalTrials.gov (NCT01018875) Efficacy and Safety Study of ABT-288 in Subjects With Mild-to-Moderate Alzheimer's Disease. U.S. National Institutes of Health. | |||||
REF 7 | ClinicalTrials.gov (NCT01207115) A Study of ABT-652 in Adults With Osteoarthritis Pain of the Knee. U.S. National Institutes of Health. | |||||
REF 8 | ClinicalTrials.gov (NCT01548287) A Study of the Safety and Tolerability of AZD5213 Effect on Sleep for Patients With Alzheimer's/Cognitive Impairment. U.S. National Institutes of Health. | |||||
REF 9 | ClinicalTrials.gov (NCT00566449) A Safety and Effectiveness Study of JNJ-31001074 in Adults With Attention-Deficit/Hyperactivity Disorder.. U.S. National Institutes of Health. | |||||
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