General Information of Drug Therapeutic Target (DTT) (ID: TT9JNIC)

DTT Name Histamine H3 receptor (H3R)
Synonyms Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
Gene Name HRH3
DTT Type
Successful target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
HRH3_HUMAN
TTD ID
T64765
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Histamine receptors (R-HSA-390650 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pitolisant DM8RFNJ Excessive daytime sleepiness MG42 Approved [2]
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17 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
SUVN-G3031 DM3BO8G Cognitive impairment 6D71 Phase 3 [3]
ABT-288 DM7X54F Alzheimer disease 8A20 Phase 2 [4]
ABT-652 DMLEO2Z Diabetic neuropathy 8C0Z Phase 2 [5]
AZD-5213 DMOZ04X Alzheimer disease 8A20 Phase 2 [6]
Bavisant DM6CVZ5 Attention deficit hyperactivity disorder 6A05.Z Phase 2 [7]
GSK239512 DMBJMZC Alzheimer disease 8A20 Phase 2 [8]
JNJ-17216498 DM1GRCU Narcolepsy 7A20 Phase 2 [9]
JNJ-39220675 DM0WY3H Alcohol dependence 6C40.2 Phase 2 [10]
S-38093 DMD8XOY Alzheimer disease 8A20 Phase 2 [11]
SAR-110894 DMCLEXM Alzheimer disease 8A20 Phase 2 [6]
ABT-239 DMR7OGL Cognitive impairment 6D71 Phase 1 [12]
APD-916 DMRGF9Q Sleep-wake disorder 7A00-7B2Z Phase 1 [13]
HPP404 DMUEZ7V Allergic rhinitis CA08.0 Phase 1 [14]
Irdabisant DMR3E4L Cognitive impairment 6D71 Phase 1 [15]
MK-3134 DM5EFPS Dementia 6D80-6D86 Phase 1 [16]
MK-7288 DMJ2Q6H Excessive daytime sleepiness MG42 Phase 1 [17]
MK-0249 DMAPV6J Insulin-resistant disorder 5A44 Clinical trial [18]
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⏷ Show the Full List of 17 Clinical Trial Drug(s)
41 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
4-benzylidene-1-(cyclobutylo)piperidine derivative 1 DMZDUNT N. A. N. A. Patented [19]
Acrylamide compound 1 DMO4YAB N. A. N. A. Patented [19]
Acrylamide compound 2 DM7EOG4 N. A. N. A. Patented [19]
Acrylamide compound 3 DM7JARB N. A. N. A. Patented [19]
Acrylamide compound 4 DMZL6D8 N. A. N. A. Patented [19]
Benzo[d]oxazol-2(3H)-one derivative 1 DMKXD2V N. A. N. A. Patented [19]
Benzo[d]oxazol-2(3H)-one derivative 2 DM47KWB N. A. N. A. Patented [19]
Benzo[d]oxazol-2(3H)-one derivative 3 DM3Z5UQ N. A. N. A. Patented [19]
Biphenyl derivative 4 DMIPVYW Histamine H3-associated disorder NE61 Patented [19]
Phenoxypiperidine derivative 1 DM0PBJT N. A. N. A. Patented [19]
Phenoxypiperidine derivative 2 DMC5G8P N. A. N. A. Patented [19]
Phenylsulfonyl derivative 1 DM9NOP3 Central nervous system disease 8A04-8D87 Patented [19]
Phenylsulfonyl derivative 2 DM63128 Central nervous system disease 8A04-8D87 Patented [19]
Phenylsulfonyl derivative 3 DME6FLN Central nervous system disease 8A04-8D87 Patented [19]
Phenylsulfonyl derivative 4 DM1HYW4 Central nervous system disease 8A04-8D87 Patented [19]
Piperazine carbamate/urea derivative 1 DMCIXD4 N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 2 DMCG6BE N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 3 DM2R468 N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 4 DM75J4T N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 5 DMJ80IZ N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 6 DMZEPU3 N. A. N. A. Patented [19]
Piperazine carbamate/urea derivative 7 DM067UC N. A. N. A. Patented [19]
Piperidine derivative 1 DMHN5KW N. A. N. A. Patented [19]
PMID29334795-Compound-21 DMTOA1Q Corticobasal degeneration 8A00.1Y Patented [19]
PMID29334795-Compound-22 DM8N10A Alzheimer disease 8A20 Patented [19]
PMID29334795-Compound-23 DM3VL64 Schizophrenia 6A20 Patented [19]
PMID29334795-Compound-24 DMTUQV0 N. A. N. A. Patented [19]
PMID29334795-Compound-25 DMGEWVP N. A. N. A. Patented [19]
PMID29334795-Compound-28 DM1SWYU Histamine H3-associated disorder NE61 Patented [19]
PMID29334795-Compound-55 DMM30LJ N. A. N. A. Patented [19]
PMID29334795-Compound-56 DMS9Q3U N. A. N. A. Patented [19]
PMID29334795-Compound-57 DMGO1PA N. A. N. A. Patented [19]
PMID29334795-Compound-58 DMB8GHJ N. A. N. A. Patented [19]
PMID29334795-Compound-61 DM9H3LI N. A. N. A. Patented [19]
PMID29334795-Compound-62 DMKAFPC N. A. N. A. Patented [19]
PMID29334795-Compound-66 DMQOF53 N. A. N. A. Patented [19]
PMID29334795-Compound-67 DMC95N7 N. A. N. A. Patented [19]
Pyridazin-3(2H)-one derivative 1 DMKJ3PC N. A. N. A. Patented [19]
Steroidal carboxamide derivative 1 DMHLA5V N. A. N. A. Patented [19]
Triazolo-benzodiazepine derivative 1 DM79KEX N. A. N. A. Patented [19]
Triazolo-benzodiazepine derivative 2 DMQSCHA N. A. N. A. Patented [19]
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⏷ Show the Full List of 41 Patented Agent(s)
10 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
BP-2.94 DMI3T64 Pain MG30-MG3Z Discontinued in Phase 2 [20]
Cipralisant DMTAKNF Attention deficit hyperactivity disorder 6A05.Z Discontinued in Phase 2 [21]
GSK835726 DMRNJPY Allergic rhinitis CA08.0 Discontinued in Phase 2 [8]
GSK1004723 DMEC6RD Allergic rhinitis CA08.0 Discontinued in Phase 1 [8]
SAR-152954 DM7OR48 Sleep-wake disorder 7A00-7B2Z Discontinued in Phase 1 [22]
GR-175737 DMOY8UA N. A. N. A. Terminated [23]
GT-2016 DM42XHS Alzheimer disease 8A20 Terminated [23]
GT-2203 DMJ4PNR Anxiety disorder 6B00-6B0Z Terminated [24]
Thioperamide DM8S593 Cognitive impairment 6D71 Terminated [25]
UCL-1390 DMD3CA5 Eating disorder 6B82 Terminated [26]
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⏷ Show the Full List of 10 Discontinued Drug(s)
146 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1H-indol-2-yl)(piperazin-1-yl)methanone DMW15DS Discovery agent N.A. Investigative [27]
(1R,2R)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine DM5ROS1 Discovery agent N.A. Investigative [28]
(1R,2S)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine DMZ3DMX Discovery agent N.A. Investigative [28]
(1S,2S)-2-(1H-Imidazol-4-yl)-cyclopentylamine DMZCS2K Discovery agent N.A. Investigative [28]
(R)-1-(2-methoxyphenethyl)-2-methylpyrrolidine DMMY0NF Discovery agent N.A. Investigative [29]
(R)-1-(3-methoxyphenethyl)-2-methylpyrrolidine DM76SZK Discovery agent N.A. Investigative [29]
(R)-1-(4-methoxyphenethyl)-2-methylpyrrolidine DMR3DSG Discovery agent N.A. Investigative [29]
(R)-1-(4-nitrophenethyl)-2-methylpyrrolidine DMNROUV Discovery agent N.A. Investigative [29]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol DMFDW4C Discovery agent N.A. Investigative [29]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine DM0L6ES Discovery agent N.A. Investigative [29]
(R)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine DMT8HP1 Discovery agent N.A. Investigative [29]
(R)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine DMA1FUH Discovery agent N.A. Investigative [29]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate DMCSHI3 Discovery agent N.A. Investigative [30]
(R)-3-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine DMUFP7W Discovery agent N.A. Investigative [29]
(R)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine DM5CL8B Discovery agent N.A. Investigative [29]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline DM3LQFK Discovery agent N.A. Investigative [31]
(R)-alpha-methylhistamine DMKAW4P Discovery agent N.A. Investigative [25]
(S)-1-(2-methoxyphenethyl)-2-methylpyrrolidine DMF9YLR Discovery agent N.A. Investigative [29]
(S)-1-(3-methoxyphenethyl)-2-methylpyrrolidine DM8UWT9 Discovery agent N.A. Investigative [29]
(S)-1-(4-methoxyphenethyl)-2-methylpyrrolidine DMDBHY1 Discovery agent N.A. Investigative [29]
(S)-1-(4-nitrophenethyl)-2-methylpyrrolidine DMG7XL5 Discovery agent N.A. Investigative [29]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol DMQGCKX Discovery agent N.A. Investigative [29]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine DMVKL84 Discovery agent N.A. Investigative [29]
(S)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine DMQGCM3 Discovery agent N.A. Investigative [29]
(S)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine DMJFI75 Discovery agent N.A. Investigative [29]
(S)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate DM435QN Discovery agent N.A. Investigative [30]
(S)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine DMLZBJT Discovery agent N.A. Investigative [29]
(S)-alpha-methylhistamine DMTUZIN Discovery agent N.A. Investigative [32]
1-(2-(naphthalen-2-yl)ethyl)pyrrolidine DMYFKID Discovery agent N.A. Investigative [29]
1-(2-m-tolyl-ethyl)-pyrrolidine DMKITY6 Discovery agent N.A. Investigative [29]
1-(2-methoxyphenethyl)pyrrolidine DMDQVSU Discovery agent N.A. Investigative [29]
1-(2-p-tolyl-ethyl)-pyrrolidine DMDLKPI Discovery agent N.A. Investigative [29]
1-(3-(2-(3-methoxyphenoxy)ethoxy)propyl)azepane DMEDSLZ Discovery agent N.A. Investigative [33]
1-(3-(3-phenylpropoxy)propyl)piperidine DM3EYOL Discovery agent N.A. Investigative [34]
1-(3-(4-(2-fluoroethyl)phenoxy)propyl)piperidine DMHEIKQ Discovery agent N.A. Investigative [35]
1-(3-(4-(fluoromethyl)phenoxy)propyl)piperidine DMVXCPE Discovery agent N.A. Investigative [35]
1-(3-methoxyphenethyl)pyrrolidine DMGU7MO Discovery agent N.A. Investigative [29]
1-(4-(benzyloxy)phenethyl)pyrrolidine DMT3H0K Discovery agent N.A. Investigative [29]
1-(4-methoxyphenethyl)pyrrolidine DMAW78K Discovery agent N.A. Investigative [29]
1-(4-nitrophenethyl)pyrrolidine DMKR8BI Discovery agent N.A. Investigative [29]
1-[2-(2,4,6-trimethyl-phenyl)-ethyl]-pyrrolidine DMEHP8M Discovery agent N.A. Investigative [29]
2-((1H-imidazol-4-yl)methyl)pyridine DM1TK45 Discovery agent N.A. Investigative [36]
2-((2-ethoxyphenoxy)methyl)-4-isopropylmorpholine DM91PA5 Discovery agent N.A. Investigative [37]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridine DMZ83G9 Discovery agent N.A. Investigative [38]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridine DMEKSAZ Discovery agent N.A. Investigative [38]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole DMZVBPG Discovery agent N.A. Investigative [36]
2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole DMCHZ8J Discovery agent N.A. Investigative [29]
2-(2-(pyrrolidin-1-yl)ethyl)phenol DMQ0WKA Discovery agent N.A. Investigative [29]
2-(2-(pyrrolidin-1-yl)ethyl)pyridine DMGQC2F Discovery agent N.A. Investigative [29]
2-(3-Methyl-3H-imidazol-4-yl)-ethylamine DME09J2 Discovery agent N.A. Investigative [23]
2-(4-Cyclopentyl-piperazin-1-yl)-quinoline DM6VQEO Discovery agent N.A. Investigative [39]
2-(4-Cyclopropyl-piperazin-1-yl)-quinoline DMPU90E Discovery agent N.A. Investigative [39]
2-(4-Isopropyl-piperazin-1-yl)-quinoline DMSH4WP Discovery agent N.A. Investigative [39]
2-(4-Methyl-piperazin-1-yl)-quinoline DMB8OY6 Discovery agent N.A. Investigative [39]
2-(4-Propyl-piperazin-1-yl)-quinoline DMWPM9L Discovery agent N.A. Investigative [39]
2-(ethoxycarbonyl)-1H-indole-5-carboxylic acid DMS7WQD Discovery agent N.A. Investigative [40]
2-[2-(1H-Imidazol-4-yl)-cyclopropyl]-ethylamine DMKEZ5G Discovery agent N.A. Investigative [41]
2-[4-(1-Ethyl-propyl)-piperazin-1-yl]-quinoline DMUH526 Discovery agent N.A. Investigative [39]
3-((1H-imidazol-4-yl)methyl)pyridine DMJ6O43 Discovery agent N.A. Investigative [36]
4-((1H-imidazol-4-yl)methyl)-1-heptylpiperidine DMX2QD5 Discovery agent N.A. Investigative [42]
4-((1H-Imidazol-4-yl)methyl)-1-phenylpiperidine DMRYWSN Discovery agent N.A. Investigative [43]
4-((2R,3S)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole DMJN2OW Discovery agent N.A. Investigative [28]
4-((2S,3R)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole DM8WCJK Discovery agent N.A. Investigative [28]
4-(2-(3,4-Dimethylphenylamino)ethyl)-1H-imidazole DMKZ6JW Discovery agent N.A. Investigative [44]
4-(2-(3-tert-Butylphenylamino)ethyl)-1H-imidazole DMP1LY4 Discovery agent N.A. Investigative [44]
4-(2-(4-Cyclohexylphenylamino)ethyl)-1H-imidazole DMM8CU2 Discovery agent N.A. Investigative [44]
4-(2-(4-Methoxyphenylamino)ethyl)-1H-imidazole DMFCS8G Discovery agent N.A. Investigative [44]
4-(2-(4-Methylphenylamino)ethyl)-1H-imidazole DMYM72T Discovery agent N.A. Investigative [44]
4-(2-(4-tert-Butylphenylamino)ethyl)-1H-imidazole DMK8ROX Discovery agent N.A. Investigative [44]
4-(2-(Cyclohexylamino)ethyl)-1H-imidazole DM1MP96 Discovery agent N.A. Investigative [44]
4-(2-(Phenylamino)ethyl)-1H-imidazole DMX1HKU Discovery agent N.A. Investigative [44]
4-(2-(pyrrolidin-1-yl)ethyl)pyridine DMHWD2C Discovery agent N.A. Investigative [29]
4-(3-Phenoxy-propyl)-1H-imidazole DM5F13I Discovery agent N.A. Investigative [45]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [46]
4-(6-Cyclohexyl-hex-3-ynyl)-1H-imidazole DMPD9GE Discovery agent N.A. Investigative [23]
4-(6-Cyclopentyl-hex-3-ynyl)-1H-imidazole DM4EC0J Discovery agent N.A. Investigative [23]
4-(7,7-Dimethyl-oct-3-ynyl)-1H-imidazole DMIY5QU Discovery agent N.A. Investigative [23]
4-(7-Methyl-oct-3-ynyl)-1H-imidazole DMJ86OS Discovery agent N.A. Investigative [23]
4-(8-Phenyl-oct-3-ynyl)-1H-imidazole DM27OGL Discovery agent N.A. Investigative [23]
4-Benzyl-1-[3-phenylpropoxy)propyl]piperidine DMIX6RG Discovery agent N.A. Investigative [34]
4-Butyl-1-[3-(phenylpropoxy)propyl]piperidine DM6ADJM Discovery agent N.A. Investigative [34]
4-Hept-3-ynyl-1H-imidazole DM5MHO6 Discovery agent N.A. Investigative [23]
4-Hex-3-ynyl-1H-imidazole DMYNTJ0 Discovery agent N.A. Investigative [23]
4-isopropyl-2-(phenoxymethyl)morpholine DM7F38J Discovery agent N.A. Investigative [37]
4-Propyl-1-[3-(phenylpropoxy)propyl]piperidine DMDBC1K Discovery agent N.A. Investigative [34]
4-[3-(4-Butyl-phenoxy)-propyl]-1H-imidazole DMFKRMG Discovery agent N.A. Investigative [47]
4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole DMXBEYQ Discovery agent N.A. Investigative [47]
4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole DM4GU29 Discovery agent N.A. Investigative [45]
5-(2-(pyrrolidin-1-yl)ethyl)isothiazole DMXAF7Y Discovery agent N.A. Investigative [29]
5-ethyl-2-(2-(pyrrolidin-1-yl)ethyl)pyridine DMX64E3 Discovery agent N.A. Investigative [29]
5-methoxy-2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole DMX1LY3 Discovery agent N.A. Investigative [29]
5-phenyl-2-(4-(piperidin-1-yl)butyl)oxazole DMQHU0J Discovery agent N.A. Investigative [48]
A-304121 DMPI0YX Discovery agent N.A. Investigative [49]
A-317920 DM124K5 Attention deficit hyperactivity disorder 6A05.Z Investigative [25]
A-331440 DMPU3QR Obesity 5B81 Investigative [25]
Aerophobin-1 DME0I6U Discovery agent N.A. Investigative [50]
APLYSAMINE DM6NM8V Discovery agent N.A. Investigative [51]
ATH-90879 DMSNBMQ Obesity 5B81 Investigative [24]
burimamide DMZ2VYG Discovery agent N.A. Investigative [52]
C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine DMY2NU8 Discovery agent N.A. Investigative [41]
CARCININE DMQUKBG Discovery agent N.A. Investigative [51]
Ciproxifan DM9N8WM Dementia 6D80-6D86 Investigative [25]
Clobenpropit DM537OH Discovery agent N.A. Investigative [25]
CONESSINE DM4VYP0 Discovery agent N.A. Investigative [53]
Des-bromoaplysamine-1 DMIKUBY Discovery agent N.A. Investigative [54]
EVT-501 DM4Q2HZ Sleep-wake disorder 7A00-7B2Z Investigative [24]
FUB 349 DMUAYWX Discovery agent N.A. Investigative [55]
FUB-130 DMCLSE0 Neurological disorder 6B60 Investigative [24]
GSK-334429 DM5EO3F Cognitive impairment 6D71 Investigative [24]
GSK189254A DMKXPOL Cognitive impairment 6D71 Investigative [25]
GT2394 DMH3PDG Discovery agent N.A. Investigative [32]
imbutamine DMPKWUO Discovery agent N.A. Investigative [56]
Imetit DMMJ6NS Discovery agent N.A. Investigative [25]
Immepip DMDM3Y1 Discovery agent N.A. Investigative [25]
Immethridine DM7YQ26 Discovery agent N.A. Investigative [25]
impentamine DMPJXZN Discovery agent N.A. Investigative [56]
impromidine DMTDRPM Discovery agent N.A. Investigative [52]
IODOPROXYFAN DMDA6VL Discovery agent N.A. Investigative [45]
JB 98064 DMPRTVX Discovery agent N.A. Investigative [32]
JNJ-28583867 DM5LEOR Discovery agent N.A. Investigative [57]
JNJ-5207852 DM5L23N Narcolepsy 7A20 Investigative [25]
Methimepip DMVQSEH Discovery agent N.A. Investigative [25]
N-benzyl-4-cyclopentylpiperazine-1-carboxamide DMUFR62 Discovery agent N.A. Investigative [58]
N-methyl-2-(pyridin-2-yl)ethanamine DM8LNMY Discovery agent N.A. Investigative [40]
N-methylhistamine DMCFH5W Discovery agent N.A. Investigative [52]
N-[3H]alpha-methylhistamine DMWDCV1 Discovery agent N.A. Investigative [59]
N-[3H]methylhistamine DM0CI4L Discovery agent N.A. Investigative [52]
PF-3900422 DM7E391 Central nervous system disease 8A04-8D87 Investigative [24]
Proxyfan DM72AT8 Discovery agent N.A. Investigative [25]
SCH79687 DM5ZEPD Central nervous system disease 8A04-8D87 Investigative [25]
ST-1025 DM14PLC Discovery agent N.A. Investigative [48]
ST-1093 DMKZJWV Discovery agent N.A. Investigative [48]
SUVN-G1031 DMVDHBT Metabolic disorder 5C50-5D2Z Investigative [24]
UCB-2892 DMQ20A4 Cognitive impairment 6D71 Investigative [24]
UCL-2138 DM15CJZ Discovery agent N.A. Investigative [35]
UCL1972 DM0P5Z9 Discovery agent N.A. Investigative [25]
Verongamine DMD1C6S Discovery agent N.A. Investigative [50]
VUF 4904 DMFPNRD Discovery agent N.A. Investigative [60]
VUF 5207 DMMNVGJ Discovery agent N.A. Investigative [60]
VUF 5681 DMVFJR4 Discovery agent N.A. Investigative [25]
VUF 8328 DMI6GD0 Discovery agent N.A. Investigative [60]
VUF-10214 DMADEOQ Discovery agent N.A. Investigative [61]
VUF-5297 DM3G6OK Discovery agent N.A. Investigative [41]
VUF5391 DMF1O0Z Discovery agent N.A. Investigative [25]
[123I]iodoproxyfan DM5SRT1 Discovery agent N.A. Investigative [55]
[125I]iodophenpropit DMN4ABU Discovery agent N.A. Investigative [62]
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⏷ Show the Full List of 146 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Schizophrenia 6A20 Pre-frontal cortex 2.63E-01 0.06 0.23
Schizophrenia 6A20 Superior temporal cortex 6.11E-01 -0.08 -0.69
Alzheimer's disease 8A00.0 Entorhinal cortex 3.62E-02 -0.09 -0.22
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References

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2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
6 SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
7 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.
8 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
9 Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
10 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.
11 Histamine H3 Receptors and Sleep-Wake Regulation. JPET January 2011 vol. 336 no. 1 17-23.
12 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.
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