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 | |||||
|---|---|---|---|---|---|---|
| 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] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Crystal structure of human histamine receptor H3R in complex with antagonist PF03654746 | PDB:7F61 | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | Yes | [93] |
| PDB Sequence |
RGFSAAWTAV
36 LAALMALLIV46 ATVLGNALVM56 LAFVADSSLR66 TQNNFFLLNL76 AISDFLVGAF 86 CIPLYVPYVL96 TGRWTFGRGL106 CKLWLVVDYL116 LCTSKAFNIV126 LISYDRFLSV 136 TRAVSYRAQQ146 GDTRRAVRKM156 LLVWVLAFLL166 YGPAILSWEY176 LSGGSSIPEG 186 HCYAEFFYNW196 YFLITASTLE206 FFTPFLSVTF216 FNLSIYLNIQ226 RRTRLRLDGA 236 REAAGRFRLS351 RDRKVAKSLA361 VIVSIFGLCW371 APYTLLMIIR381 AACHGHCVPD 391 YWYETSFWLL401 WANSAVNPVL411 YPLCHHSFRR421 AFTKLLCPQK431 L |
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| Ligand Name: N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of human histamine receptor H3R in complex with antagonist PF03654746 | PDB:7F61 | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | Yes | [93] |
| PDB Sequence |
RGFSAAWTAV
36 LAALMALLIV46 ATVLGNALVM56 LAFVADSSLR66 TQNNFFLLNL76 AISDFLVGAF 86 CIPLYVPYVL96 TGRWTFGRGL106 CKLWLVVDYL116 LCTSKAFNIV126 LISYDRFLSV 136 TRAVSYRAQQ146 GDTRRAVRKM156 LLVWVLAFLL166 YGPAILSWEY176 LSGGSSIPEG 186 HCYAEFFYNW196 YFLITASTLE206 FFTPFLSVTF216 FNLSIYLNIQ226 RRTRLRLDGA 236 REAAGRFRLS351 RDRKVAKSLA361 VIVSIFGLCW371 APYTLLMIIR381 AACHGHCVPD 391 YWYETSFWLL401 WANSAVNPVL411 YPLCHHSFRR421 AFTKLLCPQK431 L |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
|
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| 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 | |
|
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) |
||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| 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 | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| 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. | |||||
| REF 10 | ClinicalTrials.gov (NCT01772199) Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple Sclerosis. U.S. National Institutes of Health. | |||||
| REF 11 | ClinicalTrials.gov (NCT00424931) A Safety and Effectiveness Study of a Single Dose of JNJ-17216498 in Patients With Narcolepsy. U.S. National Institutes of Health. | |||||
| REF 12 | ClinicalTrials.gov (NCT00804687) An Efficacy Study of JNJ-39220675 and Pseudoephedrine in Participants With Allergic Rhinitis. U.S. National Institutes of Health. | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032202) | |||||
| REF 14 | ClinicalTrials.gov (NCT01266525) Effect of Different Doses of SAR110894D on Cognition in Patients With Mild to Moderate Alzheimer's Disease on Donepezil. U.S. National Institutes of Health. | |||||
| REF 15 | 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: 1218). | |||||
| REF 16 | The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. | |||||
| REF 17 | ClinicalTrials.gov (NCT01093508) Single-dose Safety Study of APD916 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
| REF 18 | Clinical pipeline report, company report or official report of TransTech Pharma (2011). | |||||
| REF 19 | ClinicalTrials.gov (NCT01903824) Pharmacokinetics and Pharmacodynamics (PK/PD) of CEP-26401 in Healthy Subjects. U.S. National Institutes of Health. | |||||
| REF 20 | ClinicalTrials.gov (NCT00887601) BOLD Functional Magnetic Resonance Imaging (fMRI) and Cerebral Blood Flow Measurements as Biomarkers for Cognition Enhancing Drugs (3134-006). U.S. National Institutes of Health. | |||||
| REF 21 | ClinicalTrials.gov (NCT01092780) Pharmacodynamics and Efficacy of MK7288 (MK-7288-010). U.S. National Institutes of Health. | |||||
| REF 22 | (11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists. J Nucl Med. 2014 Jan;55(1):65-72. | |||||
| REF 23 | Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).Expert Opin Ther Pat. 2018 Mar;28(3):175-196. | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008192) | |||||
| REF 25 | 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: 1244). | |||||
| REF 26 | Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154) | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028155) | |||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033674) | |||||
| REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001957) | |||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008938) | |||||
| REF 32 | 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: 1267). | |||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004362) | |||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005172) | |||||
| REF 35 | A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71. | |||||
| REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225) | |||||
| REF 37 | SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14. | |||||
| REF 38 | Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34. | |||||
| REF 39 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
| REF 40 | Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. | |||||
| REF 41 | JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41. | |||||
| REF 42 | Histamine H3 Receptors and Sleep-Wake Regulation. JPET January 2011 vol. 336 no. 1 17-23. | |||||
| REF 43 | Use of the H3 receptor antagonist radioligand [3H]-A-349821 to reveal in vivo receptor occupancy of cognition enhancing H3 receptor antagonists. Br J Pharmacol. 2009 May;157(1):139-49. | |||||
| REF 44 | A robust and high-capacity [(35)S]GTPgammaS binding assay for determining antagonist and inverse agonist pharmacological parameters of histamine H(3) receptor ligands. Assay Drug Dev Technol. 2008 Jun;6(3):339-49. | |||||
| REF 45 | Identification of biaryl sulfone derivatives as antagonists of the histamine H receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5. | |||||
| REF 46 | CEP-26401 (irdabisant), a potent and selective histamine H receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. | |||||
| REF 47 | Additive effects of a cholinesterase inhibitor and a histamine inverse agonist on scopolamine deficits in humans. Psychopharmacology (Berl). 2011 Dec;218(3):513-24. | |||||
| REF 48 | Early-stage comparative effectiveness: randomized controlled trial with histamine inverse agonist MK-7288 in excessive daytime sleepiness patients. J Clin Pharmacol. 2013 Dec;53(12):1294-302. | |||||
| REF 49 | Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem. 2008 Aug 14;51(15):4780-9. | |||||
| REF 50 | Sleep and waking during acute histamine H3 agonist BP 2.94 or H3 antagonist carboperamide (MR 16155) administration in rats. Neuropsychopharmacology. 1996 Jul;15(1):31-5. | |||||
| REF 51 | G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. J Pharmacol Exp Ther. 2005 Jul;314(1):271-81. | |||||
| REF 52 | Clinical pipeline report, company report or official report of Sanofi. | |||||
| REF 53 | New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine. Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8. | |||||
| REF 54 | 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. (Target id: 264). | |||||
| REF 55 | Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am J Rhinol. 1999 Sep-Oct;13(5):391-9. | |||||
| REF 56 | Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem. 2005 Dec 29;48(26):8289-98. | |||||
| REF 57 | A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist. J Med Chem. 1995 May 12;38(10):1593-9. | |||||
| REF 58 | In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series. Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. | |||||
| REF 59 | Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5. | |||||
| REF 60 | In vitro studies on a class of quinoline containing histamine H3 antagonists. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3295-300. | |||||
| REF 61 | Azomethine prodrugs of (R)-alpha-methylhistamine, a highly potent and selective histamine H3-receptor agonist. Curr Med Chem. 2001 Sep;8(11):1329-40. | |||||
| REF 62 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. | |||||
| REF 63 | Characteristics of recombinantly expressed rat and human histamine H3 receptors. Eur J Pharmacol. 2002 Oct 18;453(1):33-41. | |||||
| REF 64 | Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands. Bioorg Med Chem. 2009 Apr 15;17(8):3037-42. | |||||
| REF 65 | Piperidine variations in search for non-imidazole histamine H(3) receptor ligands. Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. | |||||
| REF 66 | Fluorinated non-imidazole histamine H3 receptor antagonists. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2172-5. | |||||
| REF 67 | Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain. J Med Chem. 2010 Sep 9;53(17):6445-56. | |||||
| REF 68 | 2-Aryloxymethylmorpholine histamine H(3) antagonists. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5796-9. | |||||
| REF 69 | Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6176-80. | |||||
| REF 70 | 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. J Med Chem. 2005 Jan 13;48(1):306-11. | |||||
| REF 71 | 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem. 2009 Jul 9;52(13):3855-68. | |||||
| REF 72 | Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist f... J Med Chem. 2003 May 8;46(10):1980-8. | |||||
| REF 73 | Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold. Bioorg Med Chem Lett. 2006 Jan 15;16(2):395-9. | |||||
| REF 74 | Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. Bioorg Med Chem. 2010 Jul 15;18(14):5441-8. | |||||
| REF 75 | Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active hi... J Med Chem. 2010 May 13;53(9):3840-4. | |||||
| REF 76 | Different antagonist binding properties of human and rat histamine H3 receptors. Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4. | |||||
| REF 77 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
| REF 78 | Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. Bioorg Med Chem Lett. 2000 Oct 16;10(20):2379-82. | |||||
| REF 79 | Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5883-6. | |||||
| REF 80 | Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochem Pharmacol. 2004 Sep 1;68(5):933-45. | |||||
| REF 81 | Verongamine, a novel bromotyrosine-derived histamine H3-antagonist from the marine sponge Verongula gigantea. J Nat Prod. 1994 Jan;57(1):175-7. | |||||
| REF 82 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem. 2008 Sep 11;51(17):5423-30. | |||||
| REF 83 | Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-acti... J Med Chem. 2009 Aug 13;52(15):4640-9. | |||||
| REF 84 | Aplysamine-1 and related analogs as histamine H3 receptor antagonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):897-900. | |||||
| REF 85 | Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol. 2000 Dec;131(7):1247-50. | |||||
| REF 86 | Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. J Med Chem. 2003 Dec 4;46(25):5445-57. | |||||
| REF 87 | Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. | |||||
| REF 88 | Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5303-8. | |||||
| REF 89 | Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol. 2003 Apr 25;467(1-3):57-65. | |||||
| REF 90 | Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. J Pharmacol Exp Ther. 2001 Dec;299(3):908-14. | |||||
| REF 91 | Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J Med Chem. 2008 Apr 24;51(8):2457-67. | |||||
| REF 92 | Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br J Pharmacol. 1994 Oct;113(2):355-62. | |||||
| REF 93 | Structural basis for recognition of antihistamine drug by human histamine receptor. Nat Commun. 2022 Oct 15;13(1):6105. | |||||
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