General Information of the Protein
Protein ID
PT01194
Protein Name
Histamine H3 receptor
Secondarily
Protein Name
G-protein coupled receptor 97
Gene Name
HRH3
Secondarily
Gene Name
GPCR97
Sequence
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. 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.
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Uniprot ID
Primary ID:
Q9Y5N1

Secondarily ID:
Q4QRI7
Q9GZX2
Q9H4K8
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HGNC ID
HGNC:5184
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000901 , 661W
Compound ID Compound Name Compound Formula
CP0411059
(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine
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C18H22N2
 1
1
Ki = 3981.07 nM
   TI
   LI
   LO
   TS
CP0391120
(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine
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C14H21NO
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0391121
(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine
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C13H19NO
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0098027
2-(3H-imidazol-4-yl)ethylsulfanylmethanimidamide
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C6H10N4S
 1
1 EC50 = 1.9 nM
CP0136874
(2R)-N,3-dimethyl-2-(methylamino)-N-[(1R,2S,5S,6S,9R,12S,13R,16S)-6,7,13-trimethyl-7-azapentacyclo[10.8.0.0^{2,9}.0^{5,9}.0^{13,18}]icos-18-en-16-yl]butanamide
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C29H49N3O
 1
1 EC50 = 3.3 nM
CP0047517
(1S,2S)-2-(1H-Imidazol-4-yl)-cyclopropylamine
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C6H9N3
 1
1 EC50 = 42 nM
CP0036920
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
 4
1 EC50 = 77 nM
2 Ki = 12.8 nM
3 Ki = 16 nM
4 Ki = 33.88 nM
CP0114981
(1R,2R)-2-(1H-Imidazol-4-yl)-cyclopropylamine
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C6H9N3
 1
1 EC50 = 724 nM
CP0056575
1-(3-(4-(piperidin-1-ylmethyl)phenoxy)propyl)piperidine
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C20H32N2O
 8
1 IC50 = 0.53 nM
2 Kd = 0.1445 nM
3 Ki = 0.2754 nM
4 Ki = 0.5754 nM
5 Ki = 0.6 nM
6 Ki = 0.97 nM
7 Ki = 1 nM
8 Ki = 9.24 nM
CP0159421
5-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylpyrazine-2-carboxamide
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C20H24N4O2
 2
1 IC50 = 0.631 nM
2 Ki = 0.1995 nM
CP0087367
5-fluoro-2-methyl-N-[2-methyl-4-[(3S)-3-[(2R)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]benzamide
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C24H30FN3O
 1
1 IC50 = 0.66 nM
CP0214957
5-fluoro-2-methyl-N-[2-methyl-4-[(3R)-3-[(2R)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]benzamide
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C24H30FN3O
 1
1 IC50 = 0.71 nM
CP0040569
1-[[4-(3-piperidin-1-ylpropoxy)phenyl]methyl]piperidin-4-ol
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C20H32N2O2
 2
1 IC50 = 0.72 nM
2 Ki = 0.7413 nM
CP0248952
1-(3,5-dichlorophenyl)-3-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C22H26Cl2N4O
 1
1 IC50 = 0.95 nM
CP0082544
[1-[[4-(3-piperidin-1-ylpropoxy)phenyl]methyl]piperidin-4-yl]methanol
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C21H34N2O2
 1
1 IC50 = 1.3 nM
CP0284993
(4-propan-2-yl-1,4-diazepan-1-yl)-[1-[6-(trifluoromethyl)pyridin-3-yl]piperidin-4-yl]methanone
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C20H29F3N4O
 2
1 IC50 = 2.512 nM
2 Ki = 0.3162 nM
CP0314508
US8748435, 40
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C27H37N5
 1
1 IC50 = 930 nM
CP0110803
4-(4-(1-isopropylpiperidin-4-yloxy)benzyl)morpholine
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C19H30N2O2
 3
1 Kd = 0.4786 nM
2 Ki = 2.1 nM
3 Ki = 2.138 nM
CP0134516
A-349,821
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C26H34N2O3
 4
1 Kd = 2.138 nM
2 Ki = 0.4898 nM
3 Ki = 1.585 nM
4 Ki = 2 nM
CP0044460
N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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C15H24N4S
 6
1 Kd = 43.65 nM
2 Ki = 25 nM
3 Ki = 28.84 nM
4 Ki = 50.12 nM
5 Ki = 51.1 nM
6 Ki = 63.1 nM
CP0102038
2-(1-cyclobutylpiperidin-4-yl)-6-(1-cyclobutylpiperidin-4-yl)oxy-3,4-dihydroisoquinolin-1-one
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C27H39N3O2
 2
1 Ki = 0.03 nM
2 Ki = 0.8 nM
CP0102037
6-(1-propan-2-ylpiperidin-4-yl)oxy-2-(1-propan-2-ylpyrrolidin-3-yl)-3,4-dihydroisoquinolin-1-one
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C24H37N3O2
 2
1 Ki = 0.1 nM
2 Ki = 2.1 nM
CP0193419
6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotinamide
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C21H25N3O2
 2
1 Ki = 0.12 nM
2 Ki = 0.1259 nM
CP0198937
(R)-2-(1-(6-ethoxypyridazin-3-yl)-5-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C26H30N6O
 2
1 Ki = 0.19 nM
2 Ki = 0.2 nM
CP0202877
2-Propyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C24H29N3O2
 1
1 Ki = 0.2188 nM
CP0232075
2-Phenyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C27H27N3O2
 1
1 Ki = 0.2188 nM
CP0091000
(R)-2-(2,7-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C24H27N5
 1
1 Ki = 0.24 nM
CP0305864
2-Isopropyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C24H29N3O2
 1
1 Ki = 0.25 nM
CP0056747
4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(hexahydro-1H-azepin-1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1(2H)-phthalazinone
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C39H49ClN4O2
 1
1 Ki = 0.2512 nM
CP0044094
(R)-2-(5-methyl-1-(pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H27N5
 1
1 Ki = 0.26 nM
CP0090976
(R)-2-(4-methyl-2-(pyrrolidin-1-yl)pyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H31N5
 2
1 Ki = 0.29 nM
2 Ki = 0.3 nM
CP0044006
(R)-2-methyl-3-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1,8-naphthyridine
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C25H26N4
 2
1 Ki = 0.3 nM
2 Ki = 0.34 nM
CP0203699
1-[[4-[4-(piperidin-1-ylmethyl)phenyl]phenyl]methyl]piperidine
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C24H32N2
 1
1 Ki = 0.3 nM
CP0119048
1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine
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C17H26ClNO
 2
1 Ki = 0.3 nM
2 Ki = 2.7 nM
CP0090649
2,7-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 Ki = 0.3125 nM
CP0206059
6-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O3
 1
1 Ki = 0.3125 nM
CP0206060
2,5-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 Ki = 0.3125 nM
CP0297753
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-7-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 1
1 Ki = 0.3125 nM
CP0194592
(R)-4-(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrile
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C22H22N2O
 4
1 Ki = 0.4 nM
2 Ki = 0.45 nM
3 Ki = 1.35 nM
4 Ki = 2.4 nM
CP0290003
5-Chloro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24ClN3O2
 1
1 Ki = 0.4062 nM
CP0305863
5-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O3
 1
1 Ki = 0.4062 nM
CP0126642
(R)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H26N4
 2
1 Ki = 0.45 nM
2 Ki = 0.5 nM
CP0305862
8-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 Ki = 0.4688 nM
CP0218857
6-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 Ki = 0.5 nM
CP0291530
2-Ethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 Ki = 0.5 nM
CP0164197
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-5-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 3
1 Ki = 0.5312 nM
2 Ki = 1.7 nM
3 Ki = 6.8 nM
CP0073728
7-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 Ki = 0.625 nM
CP0142753
2,8-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 Ki = 0.625 nM
CP0206057
5-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 Ki = 0.6875 nM
CP0313614
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-8-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 1
1 Ki = 0.6875 nM
CP0047136
(2R)-1-(1H-imidazol-5-yl)propan-2-amine
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C6H11N3
 2
1 Ki = 0.7 nM
2 Ki = 0.88 nM
CP0767847
(R)-2-(2-(2-(3-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)ethoxy)ethoxy)ethan-1-amine
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C26H37N5O2
 1
1 Ki = 0.7 nM
CP0310817
7-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O3
 1
1 Ki = 0.7188 nM
CP0045343
4-(1-propan-2-ylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamide
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C22H35N3O2
 2
1 Ki = 0.9 nM
2 Ki = 5.7 nM
CP0282219
2-methyl-6-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyridazin-3-one
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C19H25N3O2
 1
1 Ki = 1 nM
CP0181076
4-(1-cyclopentylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamide
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C24H37N3O2
 2
1 Ki = 1 nM
2 Ki = 8.6 nM
CP0305594
N-[1-(2-methylpropyl)pyrrolidin-3-yl]-4-(1-propan-2-ylpiperidin-4-yl)oxybenzamide
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C23H37N3O2
 2
1 Ki = 1 nM
2 Ki = 1.2 nM
CP0231381
3-(4-{[3-(1-Pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C21H23N3O2
 1
1 Ki = 1.094 nM
CP0305865
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H25N3O2
 1
1 Ki = 1.094 nM
CP0296479
8-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone trifluoroacetate
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C23H27N3O3
 1
1 Ki = 1.156 nM
CP0137854
1-(4-Chloro-phenyl)-4-(4-cyclopentyl-piperazin-1-yl)-butane-1,4-dione; hydrochloride
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C19H25ClN2O2
 1
1 Ki = 1.2 nM
CP0304085
1-[2-[4-[4-(2-piperidin-1-ylethyl)phenyl]phenyl]ethyl]piperidine
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C26H36N2
 1
1 Ki = 1.2 nM
CP0231995
2,6-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 Ki = 1.25 nM
CP0095277
4-(3-(4-(piperidin-1-yl)but-1-ynyl)benzyl)morpholine
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C20H28N2O
 1
1 Ki = 1.3 nM
CP0262053
((2R,4S)-4-(4-chloro-3-methylphenoxy)pyrrolidin-2-yl)(4-cyclobutyl-1,4-diazepan-1-yl)methanone
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C21H30ClN3O2
 1
1 Ki = 1.3 nM
CP0106703
1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(4-fluorophenoxy)pyrrolidin-1-yl)ethanone
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C22H30FN3O3
 1
1 Ki = 1.5 nM
CP0834373
tert-butyl (R)-(2-(2-(2-(3-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)ethoxy)ethoxy)ethyl)carbamate
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C31H45N5O4
 1
1 Ki = 1.5 nM
CP0096441
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(4-fluorophenoxy)pyrrolidin-2-yl)methanone
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C20H28FN3O2
 1
1 Ki = 1.6 nM
CP0115802
1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(3-fluorophenoxy)pyrrolidin-1-yl)ethanone
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C22H30FN3O3
 1
1 Ki = 1.6 nM
CP0085944
2-[[4-(3-piperidin-1-ylpropoxy)phenyl]methyl]-3,4-dihydro-1H-isoquinoline
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C24H32N2O
 1
1 Ki = 1.698 nM
CP0298758
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(4-fluorophenoxy)-1-methylpyrrolidin-2-yl)methanone
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C21H30FN3O2
 1
1 Ki = 1.8 nM
CP0707832
3-(2-((1E,3E)-5-((E)-3,3-Dimethyl-5-sulfo-1-(3-sulfopropyl)indolin-2-ylidene)penta-1,3-dien-1-yl)-3-methyl-3-(6-((2-(2-(2-(3-methyl-4-(6-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)ethoxy)ethoxy)ethyl)amino)-6-oxohexyl)-5-sulfo-3H-indol-1-ium-1-yl)propane-1-sulfonate
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C62H81N7O15S4
 1
1 Ki = 1.9 nM
CP0228017
((2R,4S)-4-(4-chlorophenoxy)pyrrolidin-2-yl)(4-cyclobutyl-1,4-diazepan-1-yl)methanone
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C20H28ClN3O2
 1
1 Ki = 2 nM
CP0246942
(4,4-Difluoropiperidin-1-yl)[1-isopropyl-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl]methanone
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C25H35F2N3O2
 1
1 Ki = 2 nM
CP0304086
1-[[4-[4-(2-piperidin-1-ylethyl)phenyl]phenyl]methyl]piperidine
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C25H34N2
 1
1 Ki = 2 nM
CP0046463
3-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-1H-pyridazin-6-one
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C18H23N3O2
 1
1 Ki = 2 nM
CP0078631
4-[(1R,2R)-2-(5,5-Dimethyl-hex-1-ynyl)-cyclopropyl]-1H-imidazole
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C14H20N2
 1
1 Ki = 2.138 nM
CP0095968
4-((3S,5R)-5-(4-cyclobutyl-1,4-diazepane-1-carbonyl)pyrrolidin-3-yloxy)benzonitrile
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C21H28N4O2
 1
1 Ki = 2.4 nM
CP0242533
2-(1,3-bis(3-(piperidin-1-yl)propyl)imidazolidin-2-ylidene)malononitrile
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C22H36N6
 1
1 Ki = 2.4 nM
CP0325312
((2R,4S)-4-(3-chlorophenoxy)pyrrolidin-2-yl)(4-cyclobutyl-1,4-diazepan-1-yl)methanone
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C20H28ClN3O2
 1
1 Ki = 2.5 nM
CP0115796
1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(thiophen-3-yloxy)pyrrolidin-1-yl)ethanone
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C20H29N3O3S
 1
1 Ki = 2.7 nM
CP0306436
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(4-(methylthio)phenoxy)pyrrolidin-2-yl)methanone
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C21H31N3O2S
 1
1 Ki = 2.8 nM
CP0255637
1-[4-(4-Piperidin-1-ylmethyl-benzyloxy)-benzyl]-piperazine; compound with oxalic acid
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C25H34N2O
 1
1 Ki = 2.818 nM
CP0271597
6-[4-(1-cyclopentylpiperidin-4-yl)oxyphenyl]-2-methylpyridazin-3-one
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C21H27N3O2
 1
1 Ki = 3 nM
CP0292222
6-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methylpyridazin-3-one
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C20H25N3O2
 1
1 Ki = 3 nM
CP0059288
(1R,6S)-5-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
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C19H25N3O2
 1
1 Ki = 3.1 nM
CP0158344
4-((3S,5R)-5-(4-cyclopentyl-1,4-diazepane-1-carbonyl)pyrrolidin-3-yloxy)benzonitrile
   Show/Hide
C22H30N4O2
 1
1 Ki = 3.2 nM
CP0158336
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(3-fluorophenoxy)pyrrolidin-2-yl)methanone
   Show/Hide
C20H28FN3O2
 1
1 Ki = 3.4 nM
CP0081592
(1S,2R)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropane
   Show/Hide
C15H18ClN3
 1
1 Ki = 3.6 nM
CP0310819
2-(1,4'-bipiperidin-1'-yl)-6-(2-methoxypyridin-4-yl)thiazolo[4,5-b]pyridine
   Show/Hide
C22H27N5OS
 1
1 Ki = 4 nM
CP0158337
(4-cyclopentyl-1,4-diazepan-1-yl)((2R,4S)-4-(4-fluorophenoxy)pyrrolidin-2-yl)methanone
   Show/Hide
C21H30FN3O2
 1
1 Ki = 4.1 nM
CP0325311
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(4-(trifluoromethyl)phenoxy)pyrrolidin-2-yl)methanone
   Show/Hide
C21H28F3N3O2
 1
1 Ki = 4.1 nM
CP0088353
(1S,6R)-5-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
   Show/Hide
C19H25N3O2
 1
1 Ki = 4.5 nM
CP0192538
(1S,2R)-trans-2-[2-(cyclohexylmethylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropane
   Show/Hide
C15H25N3
 1
1 Ki = 5.3 nM
CP0123274
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-phenoxypyrrolidin-2-yl)methanone
   Show/Hide
C20H29N3O2
 1
1 Ki = 5.3 nM
CP0306438
(4-cyclobutyl-1,4-diazepan-1-yl)((2R,4S)-4-(thiophen-3-yloxy)pyrrolidin-2-yl)methanone
   Show/Hide
C18H27N3O2S
 1
1 Ki = 5.3 nM
CP0066136
1-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-2-morpholin-4-ylethanone
   Show/Hide
C20H30N2O3
 1
1 Ki = 5.4 nM
CP0773911
(R)-2-((2-(2-(2-(3-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)ethoxy)ethoxy)ethyl)amino)-2-oxoethane-1-sulfonic acid
   Show/Hide
C28H39N5O6S
 1
1 Ki = 5.6 nM
CP0424855
2-(1-(2-(piperidin-1-yl)ethyl)-3-(3-(piperidin-1-yl)propyl)imidazolidin-2-ylidene)malononitrile
   Show/Hide
C21H34N6
 1
1 Ki = 6.6 nM
CP0144396
3-(8-(3,4-dichlorophenyl)-6-methyl-5,6,7,8-tetrahydro-2,6-naphthyridin-3-yloxy)-N,N-diethylpropan-1-amine
   Show/Hide
C22H29Cl2N3O
 1
1 Ki = 7 nM
CP0202866
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridin-6-yl)pyridin-2-ol
   Show/Hide
C21H25N5OS
 1
1 Ki = 8 nM
CP0347010
(1R,2S)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropane
   Show/Hide
C15H18ClN3
 1
1 Ki = 8.4 nM
CP0165547
2-(1,4'-bipiperidin-1'-yl)-6-chlorothiazolo[4,5-c]pyridine
   Show/Hide
C16H21ClN4S
 1
1 Ki = 10 nM
CP0282261
N-[5-[2-(4-piperidin-1-ylpiperidin-1-yl)-[1,3]thiazolo[4,5-b]pyridin-6-yl]pyridin-2-yl]acetamide
   Show/Hide
C23H28N6OS
 1
1 Ki = 10 nM
CP0085130
1-[6-[(3-cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]pyridin-3-yl]pyrrolidin-2-one
   Show/Hide
C23H27N3O2
 1
1 Ki = 10 nM
CP0176249
1-[4-[3-(4-pyridin-4-ylpiperazin-1-yl)propoxy]phenyl]ethanone
   Show/Hide
C20H25N3O2
 1
1 Ki = 10.2 nM
CP0176032
N-methyl-N-[[1-methyl-5-(3-piperidin-1-ylpropoxy)indol-2-yl]methyl]prop-2-yn-1-amine
   Show/Hide
C22H31N3O
 1
1 Ki = 10.8 nM
CP0036621
4,5-diphenyl-2-(3-(piperidin-1-yl)propoxy)thiazole
   Show/Hide
C23H26N2OS
 1
1 Ki = 11.2 nM
CP0215922
1-(7-(3-(piperidin-1-yl)propoxy)-1,2,4,5-tetrahydrobenzo[d]azepin-3-yl)ethanone
   Show/Hide
C20H30N2O2
 1
1 Ki = 11.6 nM
CP0273794
2-[4-(3-Piperidin-1-yl-propoxy)-phenyl]-indolizine
   Show/Hide
C22H26N2O
 1
1 Ki = 13 nM
CP0095048
2-(1,4'-bipiperidin-1'-yl)-6-(2-fluoropyridin-4-yl)thiazolo[4,5-b]pyridine
   Show/Hide
C21H24FN5S
 1
1 Ki = 13 nM
CP0181646
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)nicotinonitrile
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C22H24N6S
 1
1 Ki = 16 nM
CP0341379
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)pyridin-2-amine
   Show/Hide
C21H26N6S
 1
1 Ki = 16 nM
CP0261905
2-(1-(4-(piperidin-1-yl)butyl)-3-(2-(piperidin-1-yl)ethyl)imidazolidin-2-ylidene)malononitrile
   Show/Hide
C22H36N6
 1
1 Ki = 16 nM
CP0296482
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridin-6-yl)pyrazin-2-amine
   Show/Hide
C20H25N7S
 1
1 Ki = 17 nM
CP0180649
5-(3-benzhydryloxypropyl)-1H-imidazole
   Show/Hide
C19H20N2O
 2
1 Ki = 17 nM
2 Ki = 24 nM
CP0203201
2-(1,4'-bipiperidin-1'-yl)-6-(2-fluoropyridin-3-yl)thiazolo[4,5-c]pyridine
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C21H24FN5S
 1
1 Ki = 20 nM
CP0042242
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridin-6-yl)nicotinonitrile
   Show/Hide
C22H24N6S
 1
1 Ki = 22 nM
CP0037479
(4-cyclopropylpiperazin-1-yl)(4-(3,4-dichlorophenoxy)-3-((methylamino)methyl)phenyl)methanone
   Show/Hide
C22H25Cl2N3O2
 1
1 Ki = 23 nM
CP0095046
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)-2-fluorobenzonitrile
   Show/Hide
C23H24FN5S
 1
1 Ki = 23 nM
CP0157294
2-(1,3-bis(2-(piperidin-1-yl)ethyl)imidazolidin-2-ylidene)malononitrile
   Show/Hide
C20H32N6
 1
1 Ki = 24 nM
CP0041914
4-(3-(piperidin-1-yl)propoxy)benzonitrile
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C15H20N2O
 2
1 Ki = 25 nM
2 Ki = 25.12 nM
CP0181647
2-(1,4'-bipiperidin-1'-yl)-6-(pyrimidin-5-yl)thiazolo[4,5-b]pyridine
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C20H24N6S
 1
1 Ki = 25 nM
CP0181648
2-(1,4'-bipiperidin-1'-yl)-6-(pyrimidin-5-yl)thiazolo[4,5-c]pyridine
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C20H24N6S
 1
1 Ki = 25 nM
CP0231999
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridin-6-yl)pyridin-2-amine
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C21H26N6S
 1
1 Ki = 25 nM
CP0746436
4-((2-(2-(2-(3-methyl-4-(6-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)ethoxy)ethoxy)ethyl)carbamoyl)cyclobutane-1,2,3-tricarboxylic acid
   Show/Hide
C34H43N5O9
 1
1 Ki = 25.4 nM
CP0232079
N-[5-[2-(4-piperidin-1-ylpiperidin-1-yl)-[1,3]thiazolo[4,5-c]pyridin-6-yl]pyridin-2-yl]acetamide
   Show/Hide
C23H28N6OS
 1
1 Ki = 27 nM
CP0095045
4-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)benzonitrile
   Show/Hide
C23H25N5S
 1
1 Ki = 28 nM
CP0432836
Aplysamine-1
   Show/Hide
C15H24Br2N2O
 1
1 Ki = 30 nM
CP0095053
2-(1,4'-bipiperidin-1'-yl)-6-(6-fluoropyridin-3-yl)thiazolo[4,5-c]pyridine
   Show/Hide
C21H24FN5S
 1
1 Ki = 35 nM
CP0165548
2-(1,4'-bipiperidin-1'-yl)-6-(6-methoxypyridin-3-yl)thiazolo[4,5-b]pyridine
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C22H27N5OS
 1
1 Ki = 35 nM
CP0552696
1-[4-(4-tert-butylphenoxy)butyl]-4-pyridin-4-ylpiperazine
   Show/Hide
C23H33N3O
 1
1 Ki = 37.8 nM
CP0095052
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)pyridin-2-ol
   Show/Hide
C21H25N5OS
 1
1 Ki = 42 nM
CP0282258
2-(1,4'-bipiperidin-1'-yl)-6-(2-fluoropyridin-3-yl)thiazolo[4,5-b]pyridine
   Show/Hide
C21H24FN5S
 1
1 Ki = 42 nM
CP0073734
2-(1,4'-bipiperidin-1'-yl)-6-(2-fluoropyridin-4-yl)thiazolo[4,5-c]pyridine
   Show/Hide
C21H24FN5S
 1
1 Ki = 44 nM
CP0062562
4-((3R,5S)-5-(4-cyclobutyl-1,4-diazepane-1-carbonyl)pyrrolidin-3-yloxy)benzonitrile
   Show/Hide
C21H28N4O2
 1
1 Ki = 45 nM
CP0099745
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole
   Show/Hide
C16H18N2O2
 2
1 Ki = 46 nM
2 Ki = 63 nM
CP0167796
1-(5-(1,4'-bipiperidin-1'-yl)-1,3,4-thiadiazol-2-yl)-3-cyclopentylurea
   Show/Hide
C18H30N6OS
 1
1 Ki = 49 nM
CP0115794
1-((2S,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(4-(methylthio)phenoxy)pyrrolidin-1-yl)ethanone
   Show/Hide
C23H33N3O3S
 1
1 Ki = 50 nM
CP0230695
2-(1,4'-bipiperidin-1'-yl)-6-(6-fluoropyridin-3-yl)thiazolo[4,5-b]pyridine
   Show/Hide
C21H24FN5S
 1
1 Ki = 63 nM
CP0253732
2-(1,4'-bipiperidin-1'-yl)-6-(2-methoxypyridin-4-yl)thiazolo[4,5-c]pyridine
   Show/Hide
C22H27N5OS
 1
1 Ki = 64 nM
CP0042243
5-(2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridin-6-yl)pyrazin-2-amine
   Show/Hide
C20H25N7S
 1
1 Ki = 66 nM
CP0137827
7-(3-piperidin-1-ylpropoxy)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline
   Show/Hide
C19H27N3O
 1
1 Ki = 76.2 nM
CP0673695
N-{[5-(3-(1-Benzylpiperidin-4-yl)propoxy)-1-methyl-1Hindol-2-yl]methyl}-N-methylprop-2-yn-1-amine
   Show/Hide
C29H37N3O
 1
1 Ki = 84.2 nM
CP0021188
N-methyl-2-(4-phenylmethoxypiperidin-1-yl)ethanamine
   Show/Hide
C15H24N2O
 1
1 Ki = 87 nM
CP0042241
2-(1,4'-bipiperidin-1'-yl)-6-(6-methoxypyridin-3-yl)thiazolo[4,5-c]pyridine
   Show/Hide
C22H27N5OS
 1
1 Ki = 93 nM
CP0290723
2-(1,4'-bipiperidin-1'-yl)-6-(6-methylpyridin-3-yl)thiazolo[4,5-c]pyridine
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C22H27N5S
 1
1 Ki = 104 nM
CP0345088
1-[7-(4-chlorophenoxy)heptyl]piperidine
   Show/Hide
C18H28ClNO
 1
1 Ki = 128 nM
CP0044000
2-(1,4'-bipiperidin-1'-yl)-6-(6-methylpyridin-3-yl)thiazolo[4,5-b]pyridine
   Show/Hide
C22H27N5S
 1
1 Ki = 133 nM
CP0154610
[(2S,5S)-5-(1H-imidazol-5-yl)oxolan-2-yl]methanamine
   Show/Hide
C8H13N3O
 1
1 Ki = 218.78 nM
CP0130853
Imifuramine
   Show/Hide
C8H13N3O
 1
1 Ki = 229.09 nM
CP0348117
5-[(2R,5R)-5-(phenylmethoxymethyl)oxolan-2-yl]-1H-imidazole
   Show/Hide
C15H18N2O2
 1
1 Ki = 245.47 nM
CP0528102
1-[4-[3-(4-pyridin-2-ylpiperazin-1-yl)propoxy]phenyl]ethanone
   Show/Hide
C20H25N3O2
 1
1 Ki = 315 nM
CP0172969
5-[(2R,5S)-5-(phenylmethoxymethyl)oxolan-2-yl]-1H-imidazole
   Show/Hide
C15H18N2O2
 1
1 Ki = 331.13 nM
CP0795071
2-(4-(4-(4-(tert-pentyl)phenoxy)butyl)piperazin-1-yl)pyrazine
   Show/Hide
C23H34N4O
 1
1 Ki = 683 nM
CP0862785
2-(4-(4-(4-(tert-butyl)phenoxy)butyl)piperazin-1-yl)pyrimidine
   Show/Hide
C22H32N4O
 1
1 Ki = 883 nM
CP0352542
1-[4-[4-(4-pyridin-3-ylpiperazin-1-yl)butoxy]phenyl]ethanone
   Show/Hide
C21H27N3O2
 1
1 Ki = 908 nM
CP0154225
[(2R,5R)-5-(1H-imidazol-5-yl)-2,5-dihydrofuran-2-yl]methanamine
   Show/Hide
C8H11N3O
 1
1 Ki = 1023.29 nM
CP0304548
1-[[4-(piperidin-1-ylmethyl)phenyl]methyl]piperidine
   Show/Hide
C18H28N2
 1
1 Ki = 1230 nM
CP0352541
1-[4-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butoxy]phenyl]ethanone
   Show/Hide
C20H26N4O2
 1
1 Ki = 1230 nM
CP0097151
[(2R,5S)-5-(1H-imidazol-5-yl)oxolan-2-yl]methanamine
   Show/Hide
C8H13N3O
 1
1 Ki = 1698.24 nM
CP0002071
N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-N-prop-2-enylprop-2-en-1-amine
   Show/Hide
C17H22N2O
 1
1 Ki = 1698.24 nM
CP0516955
1-[4-[3-(4-pyrazin-2-ylpiperazin-1-yl)propoxy]phenyl]propan-1-one
   Show/Hide
C20H26N4O2
 1
1 Ki = 1720 nM
CP0182141
[(2S,5R)-5-(1H-imidazol-5-yl)oxolan-2-yl]methanamine
   Show/Hide
C8H13N3O
 1
1 Ki = 2041.74 nM
CP0307262
N-butyl-N-[3-[4-(5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy]propyl]butan-1-amine
   Show/Hide
C25H35N3O
 1
1 Ki = 2100 nM
CP0100890
1-cyano-3-[[(2R,5R)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidine
   Show/Hide
C11H16N6O
 1
1 Ki = 2187.76 nM
CP0041262
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole
   Show/Hide
C14H16ClN3O
 2
1 Ki = 2238.72 nM
2 Ki = 5125 nM
CP0718475
2-(4-(4-(4-(tert-pentyl)phenoxy)butyl)piperazin-1-yl)pyrimidine
   Show/Hide
C23H34N4O
 1
1 Ki = 2264 nM
CP0532197
1-[4-[3-(4-pyrimidin-2-ylpiperazin-1-yl)propoxy]phenyl]ethanone
   Show/Hide
C19H24N4O2
 1
1 Ki = 2316 nM
CP0100889
[(2S,5S)-5-(1H-imidazol-5-yl)-2,5-dihydrofuran-2-yl]methanamine
   Show/Hide
C8H11N3O
 1
1 Ki = 2511.89 nM
CP0842770
1-(4-(4-(tert-butyl)phenoxy)butyl)-4-(pyridin-2-yl)piperazine
   Show/Hide
C23H33N3O
 1
1 Ki = 2957 nM
CP0470593
1-[4-[3-(4-pyrimidin-2-ylpiperazin-1-yl)propoxy]phenyl]propan-1-one
   Show/Hide
C20H26N4O2
 1
1 Ki = 3390 nM
CP0842769
1-(4-(4-(tert-butyl)phenoxy)butyl)-4-(pyridin-3-yl)piperazine
   Show/Hide
C23H33N3O
 1
1 Ki = 3420 nM
CP0396770
1-[4-[4-(4-pyridin-2-ylpiperazin-1-yl)butoxy]phenyl]ethanone
   Show/Hide
C21H27N3O2
 1
1 Ki = 3697 nM
CP0718476
2-(4-(3-(4-(tert-butyl)phenoxy)propyl)piperazin-1-yl)pyrimidine
   Show/Hide
C21H30N4O
 1
1 Ki = 3827 nM
CP0833058
2-(4-(4-(4-(tert-butyl)phenoxy)butyl)piperazin-1-yl)pyrazine
   Show/Hide
C22H32N4O
 1
1 Ki = 5477 nM
CP0122622
5-[(2S,5R)-5-(phenylmethoxymethyl)oxolan-2-yl]-1H-imidazole
   Show/Hide
C15H18N2O2
 1
1 Ki = 6918.31 nM
CP0279022
1-cyano-3-[[(2S,5R)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidine
   Show/Hide
C11H16N6O
 1
1 Ki = 7079.46 nM
CP0035258
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
   Show/Hide
C17H18F3NO
 1
1 Ki = 7300 nM
CP0099909
1-cyano-3-[[(2R,5S)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidine
   Show/Hide
C11H16N6O
 1
1 Ki = 8128.31 nM
CP0309840
5-[(2S,5S)-5-(phenylmethoxymethyl)oxolan-2-yl]-1H-imidazole
   Show/Hide
C15H18N2O2
 1
1 Ki = 10471.29 nM
CP0055652
[(2S,5R)-5-(1H-imidazol-5-yl)-2,5-dihydrofuran-2-yl]methanamine
   Show/Hide
C8H11N3O
 1
1 Ki = 11481.54 nM
CP0066043
(5-Chloro-1H-benzoimidazol-2-yl)-(4-methyl-piperazin-1-yl)-methanone
   Show/Hide
C13H15ClN4O
 2
1 Ki = 14053 nM
2 Ki = 20000 nM
CP0195654
1-cyano-3-[[(2S,5S)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidine
   Show/Hide
C11H16N6O
 1
1 Ki = 18620.87 nM
CP0038430
[(2R,5S)-5-(1H-imidazol-5-yl)-2,5-dihydrofuran-2-yl]methanamine
   Show/Hide
C8H11N3O
 1
1 Ki = 19952.62 nM
CP0949327
1-(4-(4-(tert-pentyl)phenoxy)butyl)-4-(pyridin-3-yl)piperazine
   Show/Hide
C24H35N3O
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Histamine H3 receptor (H3R) )
Target Type Successful Target
Disease 15 Target-related Diseases  15
1 Excessive daytime sleepiness [ICD-11: MG42]
2 Cognitive impairment [ICD-11: 6D71]
3 Alzheimer disease [ICD-11: 8A20]
4 Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
5 Dementia [ICD-11: 6D80-6D86]
6 Alcohol dependence [ICD-11: 6C40.2]
7 Insulin-resistant disorder [ICD-11: 5A44]
8 Schizophrenia [ICD-11: 6A20]
9 Allergic rhinitis [ICD-11: CA08.0]
10 Anxiety disorder [ICD-11: 6B00-6B0Z]
11 Pain [ICD-11: MG30-MG3Z]
12 Obesity [ICD-11: 5B81]
13 Neurological disorder [ICD-11: 6B60]
14 Narcolepsy [ICD-11: 7A20]
15 Central nervous system disease [ICD-11: 8A04-8D87]
Approved Drug(s) 1 Approved Drug  1
1 Pitolisant Approved
Excessive daytime sleepiness
Clinical Trial Drug(s) 9 Clinical Trial Drugs  9
1 SUVN-G3031 Phase 3
Cognitive impairment
2 ABT-288 Phase 2
Alzheimer disease
3 Bavisant Phase 2
Attention deficit hyperactivity disorder
4 GSK239512 Phase 2
Dementia
5 JNJ-39220675 Phase 2
Alcohol dependence
6 ABT-239 Phase 1
Cognitive impairment
7 Irdabisant Phase 1
Cognitive impairment
8 MK-3134 Phase 1
Dementia
9 MK-0249 Clinical trial
Insulin-resistant disorder
Discontinued Drug(s) 6 Discontinued Drugs  6
1 Cipralisant Discontinued in Phase 2
Attention deficit hyperactivity disorder
2 GSK1004723 Discontinued in Phase 1
Allergic rhinitis
3 GT-2016 Terminated
Alzheimer disease
4 GT-2203 Terminated
Anxiety disorder
5 Thioperamide Terminated
Cognitive impairment
6 UCL-1390 Terminated
Pain
Investigative Drug(s) 8 Investigative Drugs  8
1 A-317920 Investigative
Attention deficit hyperactivity disorder
2 A-331440 Investigative
Obesity
3 Ciproxifan Investigative
Obesity
4 FUB-130 Investigative
Neurological disorder
5 GSK-334429 Investigative
Cognitive impairment
6 GSK189254A Investigative
Cognitive impairment
7 JNJ-5207852 Investigative
Narcolepsy
8 SCH79687 Investigative
Central nervous system disease
Patented Agent(s) 1 Patented Agent  1
1 PMID29334795-Compound-23 Patented
Schizophrenia
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00577 Histamine receptor H3 Macaca mulatta, Rhesus macaque
PT03573 Histamine H3 receptor Cavia porcellus, Guinea pig