General Information of the Protein
Protein ID
PT02398
Protein Name
Glucose-dependent insulinotropic receptor
Secondarily
Protein Name
G-protein coupled receptor 119
Gene Name
GPR119
Sequence
MESSFSFGVILAVLTILIIAVNALVVVAMLLSIYKNDGVGLCFTLNLAVADTLIGVAISGLVTDQLSSSAQHTQKTLCSLRMAFVTSSAAASVLTVMLIAFDRYLAIKQPLRYFQIMNGLVAGACIAGLWLVSYLIGFLPLGVSIFQQTTYHGPCSFFAVFHPRFVLTLSCAGFFPAVLLFVFFYCDMLKIASVHSQQIRKMEHAGAMAGAYRPPRSVNDFKAVRTIAVLIGSFTLSWSPFLITSIVQVACHKCCLYQVLEKYLWLLGVGNSLLNPLIYAYWQREVRQQLYHMALGVKKFFTSILLLLPARNRGPERTRESAYHIVTISHPELDG
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
Function
Receptor for the endogenous fatty-acid ethanolamide oleoylethanolamide (OEA) and lysophosphatidylcholine (LPC). Functions as a glucose-dependent insulinotropic receptor. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Seems to act through a G(s) mediated pathway.
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Uniprot ID
Primary ID:
Q7TQP3

Secondarily ID:
Q2ABS2
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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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0196960
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]ethanone
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C25H30ClFN4O2
 1
1
EC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0447464
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone
   Show/Hide
C25H31ClN4O2
 1
1
EC50 = 0.5 nM
   TI
   LI
   LO
   TS
CP0271797
4-[3-[2-[3-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]propyl]cyclopropyl]propoxy]-N-cyclopropyl-2-fluorobenzamide
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C28H36ClFN4O2
 1
1
EC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0250773
1-(azetidin-1-yl)-2-[2,6-difluoro-4-[2-[(1S,2R)-2-[1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone
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C27H34F2N4O3
 1
1
EC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0406757
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]ethanone
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C27H35FN4O2
 1
1
EC50 = 0.84 nM
   TI
   LI
   LO
   TS
CP0365277
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]-N-cyclopropylacetamide
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C25H31ClN4O2
 1
1
EC50 = 1.5 nM
   TI
   LI
   LO
   TS
CP0406760
1-(azetidin-1-yl)-2-[2-fluoro-4-[2-[(1S,2R)-2-[1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone
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C27H35FN4O3
 1
1
EC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0406761
1-(azetidin-1-yl)-2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-3-fluorophenyl]ethanone
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C25H30ClFN4O2
 1
1
EC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0422031
6-methyl-2-(2-((1S,2R)-2-(1-(5-methylpyrimidin-2-yl)piperidin-4-yl)cyclopropyl)ethoxy)pyrimidine-4-carbonitrile
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C21H26N6O
 1
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
CP0494412
tert-butyl 4-[1-(2-cyano-6-methylpyrimidin-4-yl)piperidin-4-yl]piperidine-1-carboxylate
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C21H31N5O2
 1
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
CP0501547
tert-butyl 4-[1-(6-cyano-2-methylpyrimidin-4-yl)piperidin-4-yl]piperidine-1-carboxylate
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C21H31N5O2
 1
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
CP0112328
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]-1-piperidin-1-ylethanone
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C27H34ClFN4O2
 1
1
EC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0378236
5-chloro-2-(4-((1R,2S)-2-(2-(5-(methylsulfonyl)pyridin-2-yloxy)ethyl)cyclopropyl)piperidin-1-yl)pyrimidine
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C20H25ClN4O3S
 1
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
CP0501549
2-(4-((1R,2S)-2-(2-(5-(1H-1,2,3-triazol-1-yl)pyridin-2-yloxy)ethyl)cyclopropyl)piperidin-1-yl)-5-chloropyrimidine
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C21H24ClN7O
 1
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
CP0181432
1-(azetidin-1-yl)-2-[6-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]pyridin-3-yl]ethanone
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C24H30ClN5O2
 1
1
EC50 = 5.1 nM
   TI
   LI
   LO
   TS
CP0456339
2-(4-((1R,2S)-2-(2-(4-(1H-1,2,3-triazol-1-yl)phenoxy)ethyl)cyclopropyl)piperidin-1-yl)-5-chloropyrimidine
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C22H25ClN6O
 1
1
EC50 = 6 nM
   TI
   LI
   LO
   TS
CP0106962
(1-methylcyclopropyl) 4-[(1R,2S)-2-[2-[4-[2-(azetidin-1-yl)-2-oxoethyl]-3-fluorophenoxy]ethyl]cyclopropyl]piperidine-1-carboxylate
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C26H35FN2O4
 1
1
EC50 = 6.6 nM
   TI
   LI
   LO
   TS
CP0246804
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]-2-fluorophenyl]-1-(3-hydroxyazetidin-1-yl)ethanone
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C25H30ClFN4O3
 1
1
EC50 = 6.7 nM
   TI
   LI
   LO
   TS
CP0406759
1-(azetidin-1-yl)-2-[2-fluoro-4-[2-[(1S,2R)-2-[1-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]ethanone
   Show/Hide
C26H35FN4O3
 1
1
EC50 = 6.7 nM
   TI
   LI
   LO
   TS
CP0422030
1-(5-chloropyrimidin-2-yl)-1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidine
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C21H27ClN4O2S
 1
1
EC50 = 8 nM
   TI
   LI
   LO
   TS
CP0456338
1-(4-(methylsulfonyl)phenyl)-1'-(5-(trifluoromethyl)pyridin-2-yl)-4,4'-bipiperidine
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C23H28F3N3O2S
 1
1
EC50 = 8 nM
   TI
   LI
   LO
   TS
CP0398767
ethyl (2R)-2-[6-chloro-3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]-2-methyl-3-phenylpropanoate
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C25H21ClF3N3O2
 1
1
EC50 = 8 nM
   TI
   LI
   LO
   TS
CP0413537
ethyl (3R)-3-benzyl-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C26H22F3N3O2
 1
1
EC50 = 8 nM
   TI
   LI
   LO
   TS
CP0475807
methyl (3R)-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C25H19F4N3O2
 1
1
EC50 = 9 nM
   TI
   LI
   LO
   TS
CP0301826
2-methyl-6-(1'-(5-methylpyrimidin-2-yl)-4,4'-bipiperidin-1-yl)pyrimidine-4-carbonitrile
   Show/Hide
C21H27N7
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0341195
4-(1'-(5-chloropyrimidin-2-yl)-4,4'-bipiperidin-1-yl)-6-methylpyrimidine-2-carbonitrile
   Show/Hide
C20H24ClN7
 1
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
CP0501607
tert-butyl 4-[1-(2-cyanopyrimidin-4-yl)piperidin-4-yl]piperidine-1-carboxylate
   Show/Hide
C20H29N5O2
 1
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
CP0413538
ethyl (3R)-3-benzyl-10-(4-chlorophenyl)-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C25H22ClN3O2
 1
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
CP0425781
ethyl (2R)-2-methyl-2-[6-methyl-3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]-3-phenylpropanoate
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C26H24F3N3O2
 1
1
EC50 = 11 nM
   TI
   LI
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   TS
CP0475805
methyl (3S)-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C24H18F4N4O2
 1
1
EC50 = 14 nM
   TI
   LI
   LO
   TS
CP0492414
methyl 3-benzyl-10-[4-(trifluoromethyl)phenyl]-5-oxa-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C24H18F3N3O3
 1
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
CP0269948
2-[4-[2-[(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl]ethoxy]phenyl]acetamide
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C22H27ClN4O2
 1
1
EC50 = 16 nM
   TI
   LI
   LO
   TS
CP0413542
methyl 3-benzyl-10-[4-(trifluoromethyl)phenyl]-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C25H20F3N3O2
 1
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0395450
ethyl (2R)-2-methyl-3-phenyl-2-[3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]propanoate
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C25H22F3N3O2
 1
1
EC50 = 19 nM
   TI
   LI
   LO
   TS
CP0458461
ethyl (2R)-2-methyl-2-[2-methyl-3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]-3-phenylpropanoate
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C26H24F3N3O2
 1
1
EC50 = 24 nM
   TI
   LI
   LO
   TS
CP0447281
ethyl (3S)-3-benzyl-10-[4-(trifluoromethyl)phenyl]-1,5,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C25H21F3N4O2
 1
1
EC50 = 25 nM
   TI
   LI
   LO
   TS
CP0425782
ethyl (9R)-9-benzyl-3-[4-(trifluoromethyl)phenyl]-7,8-dihydro-6H-pyrazolo[1,5-a]quinazoline-9-carboxylate
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C27H24F3N3O2
 1
1
EC50 = 27 nM
   TI
   LI
   LO
   TS
CP0425927
tert-butyl 4-[1-(6-cyanopyrimidin-4-yl)piperidin-4-yl]piperidine-1-carboxylate
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C20H29N5O2
 1
1
EC50 = 31 nM
   TI
   LI
   LO
   TS
CP0425783
methyl 3-benzyl-10-[4-(trifluoromethyl)phenyl]-4-oxa-1,8,12-triazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-3-carboxylate
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C24H18F3N3O3
 1
1
EC50 = 35 nM
   TI
   LI
   LO
   TS
CP0555183
tert-butyl 4-[1-(4-methylsulfonylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C22H34N2O4S
 1
1
EC50 = 36 nM
   TI
   LI
   LO
   TS
CP0459443
ethyl (2R)-2-methyl-3-phenyl-2-[8-[4-(trifluoromethyl)phenyl]pyrazolo[5,1-c][1,2,4]triazin-4-yl]propanoate
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C24H21F3N4O2
 1
1
EC50 = 39 nM
   TI
   LI
   LO
   TS
CP0373406
6-(1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidin-1-yl)nicotinonitrile
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C23H28N4O2S
 1
1
EC50 = 41 nM
   TI
   LI
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   TS
CP0498686
1-(5-methylpyrimidin-2-yl)-1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidine
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C22H30N4O2S
 1
1
EC50 = 45 nM
   TI
   LI
   LO
   TS
CP0395453
N-(2-methoxyethyl)-N,2-dimethyl-3-phenyl-2-[3-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]propanamide
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C27H27F3N4O2
 1
1
EC50 = 49 nM
   TI
   LI
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   TS
CP0248879
4-methyl-6-(1'-(5-methylpyrazin-2-yl)-4,4'-bipiperidin-1-yl)pyrimidine-2-carbonitrile
   Show/Hide
C21H27N7
 1
1
EC50 = 64 nM
   TI
   LI
   LO
   TS
CP0456337
1-(5-methylpyridin-2-yl)-1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidine
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C23H31N3O2S
 1
1
EC50 = 73 nM
   TI
   LI
   LO
   TS
CP0459442
ethyl 3-(2-chloro-6-fluorophenyl)-2-[3-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl]propanoate
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C23H18Cl2FN3O2
 1
1
EC50 = 76 nM
   TI
   LI
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   TS
CP0467869
ethyl (2R)-2-[3-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl]-2-methyl-3-phenylpropanoate
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C24H22ClN3O2
 1
1
EC50 = 76 nM
   TI
   LI
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   TS
CP0050460
2-methyl-6-(1'-(5-methylpyrazin-2-yl)-4,4'-bipiperidin-1-yl)pyrimidine-4-carbonitrile
   Show/Hide
C21H27N7
 1
1
EC50 = 82 nM
   TI
   LI
   LO
   TS
CP0501548
1-(5-chloropyridin-2-yl)-1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidine
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C22H28ClN3O2S
 1
1
EC50 = 131 nM
   TI
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CP0456335
tert-butyl 4-[1-(4-methylsulfinylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C22H34N2O3S
 1
1
EC50 = 132 nM
   TI
   LI
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   TS
CP0418176
methyl (3S)-3-[(3-fluorophenyl)methyl]-10-[4-(trifluoromethyl)phenyl]-1,4,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),4,7,9,11-pentaene-3-carboxylate
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C24H16F4N4O2
 1
1
EC50 = 135 nM
   TI
   LI
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   TS
CP0425926
tert-butyl 4-(1-pyrazin-2-ylpiperidin-4-yl)piperidine-1-carboxylate
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C19H30N4O2
 1
1
EC50 = 142 nM
   TI
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   TS
CP0501606
tert-butyl 4-[1-(4-carbamoylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C22H33N3O3
 1
1
EC50 = 165 nM
   TI
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   TS
CP0373403
1-(5-fluoropyridin-2-yl)-1'-(4-(methylsulfonyl)phenyl)-4,4'-bipiperidine
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C22H28FN3O2S
 1
1
EC50 = 206 nM
   TI
   LI
   LO
   TS
CP0373405
1-(4-(methylsulfonyl)phenyl)-1'-(pyrazin-2-yl)-4,4'-bipiperidine
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C21H28N4O2S
 1
1
EC50 = 239 nM
   TI
   LI
   LO
   TS
CP0501592
tert-butyl 4-[1-(4-acetylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C23H34N2O3
 1
1
EC50 = 341 nM
   TI
   LI
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   TS
CP0456336
tert-butyl 4-(1-pyrimidin-4-ylpiperidin-4-yl)piperidine-1-carboxylate
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C19H30N4O2
 1
1
EC50 = 379 nM
   TI
   LI
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   TS
CP0373402
tert-butyl 4-[1-(4-methylsulfanylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C22H34N2O2S
 1
1
EC50 = 513 nM
   TI
   LI
   LO
   TS
CP0425925
tert-butyl 4-(1-pyrimidin-2-ylpiperidin-4-yl)piperidine-1-carboxylate
   Show/Hide
C19H30N4O2
 1
1
EC50 = 523 nM
   TI
   LI
   LO
   TS
CP0422029
1-(4-(methylsulfonyl)phenyl)-1'-(pyridin-2-yl)-4,4'-bipiperidine
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C22H29N3O2S
 1
1
EC50 = 682 nM
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CP0459186
1-(4-(methylsulfonyl)phenyl)-1'-(pyrimidin-2-yl)-4,4'-bipiperidine
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C21H28N4O2S
 1
1
EC50 = 887 nM
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CP0373404
tert-butyl 4-[1-(4-methylphenyl)piperidin-4-yl]piperidine-1-carboxylate
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C22H34N2O2
 1
1
EC50 = 1900 nM
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CP0422028
tert-butyl 4-(1-pyridin-2-ylpiperidin-4-yl)piperidine-1-carboxylate
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C20H31N3O2
 1
1
EC50 = 2500 nM
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