General Information of the Protein
Protein ID
PT00577
Protein Name
Histamine receptor H3
Gene Name
HRH3
Sequence
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGNTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAGGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAAGAEAGETALGGGGGGGSAASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEQCWK
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Organism
Macaca mulatta, Rhesus macaque
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Uniprot ID
Q865E1
Subcellular Location
Cell membrane
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0540768
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]cyclohexanecarboxamide
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C23H35N3O
 1
1
Ki = 0.39 nM
   TI
   LI
   LO
   TS
CP0070912
3,5-dimethyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]-1,2-oxazole-4-carboxamide
   Show/Hide
C22H30N4O2
 1
1
Ki = 0.4 nM
   TI
   LI
   LO
   TS
CP0492985
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]cyclopentanecarboxamide
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C22H33N3O
 1
1
Ki = 0.5 nM
   TI
   LI
   LO
   TS
CP0476801
2,2,3,3-tetramethyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]cyclopropane-1-carboxamide
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C24H37N3O
 1
1
Ki = 0.55 nM
   TI
   LI
   LO
   TS
CP0500998
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]bicyclo[2.2.1]heptane-2-carboxamide
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C24H35N3O
 1
1
Ki = 0.55 nM
   TI
   LI
   LO
   TS
CP0476800
2-cyclopentyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]acetamide
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C23H35N3O
 1
1
Ki = 0.85 nM
   TI
   LI
   LO
   TS
CP0107784
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]oxane-4-carboxamide
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C22H33N3O2
 1
1
Ki = 0.97 nM
   TI
   LI
   LO
   TS
CP0462174
3-methyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]-1,2-oxazole-5-carboxamide
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C21H28N4O2
 1
1
Ki = 1.1 nM
   TI
   LI
   LO
   TS
CP0484202
6-methyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]pyridine-2-carboxamide
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C23H30N4O
 1
1
Ki = 1.4 nM
   TI
   LI
   LO
   TS
CP0436027
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]furan-3-carboxamide
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C21H27N3O2
 1
1
Ki = 1.8 nM
   TI
   LI
   LO
   TS
CP0406979
1-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]-3-(thiophen-2-ylmethyl)urea
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C21H28N4OS
 1
1
Ki = 1.9 nM
   TI
   LI
   LO
   TS
CP0087368
5-fluoro-2-methyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]benzamide
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C24H30FN3O
 1
1
Ki = 2.5 nM
   TI
   LI
   LO
   TS
CP0509429
3,4-difluoro-N-[2-methyl-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-yl]benzenesulfonamide
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C21H26F2N4O2S
 1
1
Ki = 2.5 nM
   TI
   LI
   LO
   TS
CP0525020
N-[2-methyl-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-yl]benzamide
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C22H28N4O
 1
1
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0475033
2-cyclopentyl-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]acetamide
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C22H33N3O
 1
1
Ki = 3.1 nM
   TI
   LI
   LO
   TS
CP0380162
1-(2,4-difluorophenyl)-3-[4-(3-piperidin-1-ylpropoxy)phenyl]urea
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C21H25F2N3O2
 1
1
Ki = 3.4 nM
   TI
   LI
   LO
   TS
CP0406982
1-(3,5-dichlorophenyl)-3-[4-(3-piperidin-1-ylpropoxy)phenyl]urea
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C21H25Cl2N3O2
 1
1
Ki = 3.4 nM
   TI
   LI
   LO
   TS
CP0553880
N-[2-methyl-4-[(3R)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]oxane-4-carboxamide
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C22H33N3O2
 1
1
Ki = 3.9 nM
   TI
   LI
   LO
   TS
CP0484201
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]furan-2-carboxamide
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C21H27N3O2
 1
1
Ki = 3.9 nM
   TI
   LI
   LO
   TS
CP0489114
1-cyclohexyl-3-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C22H34N4O
 1
1
Ki = 4.1 nM
   TI
   LI
   LO
   TS
CP0540854
N-[2-methyl-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-yl]naphthalene-1-carboxamide
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C26H30N4O
 1
1
Ki = 4.2 nM
   TI
   LI
   LO
   TS
CP0380999
1-cyclohexyl-3-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C23H36N4O
 1
1
Ki = 4.6 nM
   TI
   LI
   LO
   TS
CP0537690
2-methyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]-1,3-oxazole-4-carboxamide
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C21H28N4O2
 1
1
Ki = 4.6 nM
   TI
   LI
   LO
   TS
CP0484124
5-methyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]-1H-pyrazole-3-carboxamide
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C21H29N5O
 1
1
Ki = 4.7 nM
   TI
   LI
   LO
   TS
CP0517271
N-[2-methyl-6-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-yl]-2-phenylacetamide
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C23H30N4O
 1
1
Ki = 4.9 nM
   TI
   LI
   LO
   TS
CP0567287
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperidine-1-carboxamide
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C21H32N4O
 1
1
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0948376
N-(2-methyl-4-(2-methyl-1,3'-bipyrrolidin-1'-yl)phenyl)tetrahydro-2H-pyran-4-carboxamide
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C22H33N3O2
 1
1
Ki = 6.8 nM
   TI
   LI
   LO
   TS
CP0374981
1-[(3,5-dichlorophenyl)methyl]-3-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C23H28Cl2N4O
 1
1
Ki = 7.1 nM
   TI
   LI
   LO
   TS
CP0553879
N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]oxolane-2-carboxamide
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C21H31N3O2
 1
1
Ki = 7.33 nM
   TI
   LI
   LO
   TS
CP0438205
N-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]oxolane-2-carboxamide
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C21H31N3O2
 1
1
Ki = 7.34 nM
   TI
   LI
   LO
   TS
CP0375427
1-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]-3-(thiophen-2-ylmethyl)urea
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C22H30N4OS
 1
1
Ki = 8.4 nM
   TI
   LI
   LO
   TS
CP0848190
2-cyclopentyl-N-(2-methyl-4-(2-methyl-1,3'-bipyrrolidin-1'-yl)phenyl)acetamide
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C23H35N3O
 1
1
Ki = 8.4 nM
   TI
   LI
   LO
   TS
CP0432603
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]oxolane-2-carboxamide
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C20H29N3O2
 1
1
Ki = 8.7 nM
   TI
   LI
   LO
   TS
CP0856213
N-(2-methyl-4-(2-methyl-1,3'-bipyrrolidin-1'-yl)phenyl)cyclohexanecarboxamide
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C23H35N3O
 1
1
Ki = 9 nM
   TI
   LI
   LO
   TS
CP0501000
N-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]cyclopropanecarboxamide
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C20H29N3O
 1
1
Ki = 9.6 nM
   TI
   LI
   LO
   TS
CP0422519
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]cyclopropanecarboxamide
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C19H27N3O
 1
1
Ki = 9.7 nM
   TI
   LI
   LO
   TS
CP0489113
4-methyl-N-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperazine-1-carboxamide
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C22H35N5O
 1
1
Ki = 10.5 nM
   TI
   LI
   LO
   TS
CP0500862
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]-4-phenylpiperazine-1-carboxamide
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C26H35N5O
 1
1
Ki = 10.6 nM
   TI
   LI
   LO
   TS
CP0395415
2-cyclopentyl-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]acetamide
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C23H35N3O
 1
1
Ki = 10.7 nM
   TI
   LI
   LO
   TS
CP0525051
1,5-dimethyl-N-[2-methyl-4-[(3S)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]phenyl]pyrazole-3-carboxamide
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C22H31N5O
 1
1
Ki = 10.8 nM
   TI
   LI
   LO
   TS
CP0456099
1-cyclohexyl-3-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C23H36N4O
 1
1
Ki = 11.2 nM
   TI
   LI
   LO
   TS
CP0403914
4-methyl-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperazine-1-carboxamide
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C22H35N5O
 1
1
Ki = 12.7 nM
   TI
   LI
   LO
   TS
CP0440508
1-acetyl-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]pyrrolidine-2-carboxamide
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C22H32N4O2
 1
1
Ki = 14.1 nM
   TI
   LI
   LO
   TS
CP0541595
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)phenyl]cyclopropanecarboxamide
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C20H26F3N3O
 1
1
Ki = 14.7 nM
   TI
   LI
   LO
   TS
CP0406981
1-[4-[2-(diethylamino)ethoxy]phenyl]-3-[4-(2-methylpropoxy)phenyl]thiourea
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C23H33N3O2S
 1
1
Ki = 15.7 nM
   TI
   LI
   LO
   TS
CP0395398
N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]bicyclo[2.2.1]heptane-2-carboxamide
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C23H33N3O
 1
1
Ki = 15.7 nM
   TI
   LI
   LO
   TS
CP0514211
N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]oxane-4-carboxamide
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C22H33N3O2
 1
1
Ki = 17 nM
   TI
   LI
   LO
   TS
CP0541615
N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]oxolane-2-carboxamide
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C21H31N3O2
 1
1
Ki = 17 nM
   TI
   LI
   LO
   TS
CP0379883
N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]cyclopropanecarboxamide
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C20H29N3O
 1
1
Ki = 17.7 nM
   TI
   LI
   LO
   TS
CP0380117
1-(3,5-dichloro-4-methylphenyl)-3-[4-(3-piperidin-1-ylpropoxy)phenyl]urea
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C22H27Cl2N3O2
 1
1
Ki = 18.2 nM
   TI
   LI
   LO
   TS
CP0248952
1-(3,5-dichlorophenyl)-3-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
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C22H26Cl2N4O
 1
1
Ki = 19.1 nM
   TI
   LI
   LO
   TS
CP0956798
N-(2-methyl-4-(2-methyl-1,3'-bipyrrolidin-1'-yl)phenyl)bicyclo[2.2.1]heptane-2-carboxamide
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C24H35N3O
 1
1
Ki = 19.9 nM
   TI
   LI
   LO
   TS
CP0085869
1-(3,5-dichlorophenyl)-3-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
   Show/Hide
C23H28Cl2N4O
 1
1
Ki = 22.2 nM
   TI
   LI
   LO
   TS
CP0456100
4-acetyl-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperazine-1-carboxamide
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C23H35N5O2
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0380997
4-methyl-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperazine-1-carboxamide
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C21H33N5O
 1
1
Ki = 25.7 nM
   TI
   LI
   LO
   TS
CP0456097
1-[(3,5-dichlorophenyl)methyl]-3-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
   Show/Hide
C24H30Cl2N4O
 1
1
Ki = 28.8 nM
   TI
   LI
   LO
   TS
CP0406980
4-acetyl-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]piperazine-1-carboxamide
   Show/Hide
C22H33N5O2
 1
1
Ki = 34.1 nM
   TI
   LI
   LO
   TS
CP0456098
3-[acetyl(methyl)amino]-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]pyrrolidine-1-carboxamide
   Show/Hide
C23H35N5O2
 1
1
Ki = 35.5 nM
   TI
   LI
   LO
   TS
CP0905229
2,2,3,3-tetramethyl-N-(2-methyl-4-(2-methyl-1,3'-bipyrrolidin-1'-yl)phenyl)cyclopropanecarboxamide
   Show/Hide
C24H37N3O
 1
1
Ki = 37.3 nM
   TI
   LI
   LO
   TS
CP0456096
1-(3,5-dichlorophenyl)-3-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]urea
   Show/Hide
C23H28Cl2N4O
 1
1
Ki = 43 nM
   TI
   LI
   LO
   TS
CP0539731
1-acetyl-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]pyrrolidine-2-carboxamide
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C23H34N4O2
 1
1
Ki = 44.9 nM
   TI
   LI
   LO
   TS
CP0380163
1-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]-3-(4-phenoxyphenyl)urea
   Show/Hide
C28H32N4O2
 1
1
Ki = 46.8 nM
   TI
   LI
   LO
   TS
CP0476802
1-acetyl-N-[2-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C23H34N4O2
 1
1
Ki = 57.7 nM
   TI
   LI
   LO
   TS
CP0500999
2,2,3,3-tetramethyl-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]cyclopropane-1-carboxamide
   Show/Hide
C24H37N3O
 1
1
Ki = 65.5 nM
   TI
   LI
   LO
   TS
CP0374980
3-[acetyl(methyl)amino]-N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]pyrrolidine-1-carboxamide
   Show/Hide
C24H37N5O2
 1
1
Ki = 89.7 nM
   TI
   LI
   LO
   TS
CP0524039
1-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]-3-(4-phenoxyphenyl)urea
   Show/Hide
C29H34N4O2
 1
1
Ki = 115.2 nM
   TI
   LI
   LO
   TS
CP0478833
N-[3-methyl-4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]bicyclo[2.2.1]heptane-2-carboxamide
   Show/Hide
C24H35N3O
 1
1
Ki = 130.3 nM
   TI
   LI
   LO
   TS
CP0407021
2,2,3,3-tetramethyl-N-[4-[3-(2-methylpyrrolidin-1-yl)pyrrolidin-1-yl]phenyl]cyclopropane-1-carboxamide
   Show/Hide
C23H35N3O
 1
1
Ki = 143.8 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01194 Histamine H3 receptor Homo sapiens, Human
PT03573 Histamine H3 receptor Cavia porcellus, Guinea pig