General Information of the Protein
Protein ID
PT02455
Protein Name
Glucose-dependent insulinotropic receptor
Secondarily
Protein Name
G-protein coupled receptor 119
Gene Name
GPR119
Sequence
MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG
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Organism
Homo sapiens, Human
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:
Q8TDV5

Secondarily ID:
Q495H7
Q4VBN3
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HGNC ID
HGNC:19060
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: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0462142
tert-butyl (1S,5R)-3-[[4-(2-fluoro-4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
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C25H30FN7O4S
 1
1
EC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0116940
tert-butyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
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C24H29FN4O4S2
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0272880
GSK-1292263A
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C23H28N4O4S
 1
1
EC50 = 3.4 nM
   TI
   LI
   LO
   TS
CP0078155
(2-Fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-1-yl]-5-nitropyrimidin-4-yl}-amine
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C21H24FN7O5S
 1
1
EC50 = 6 nM
   TI
   LI
   LO
   TS
CP0548546
tert-butyl (1S,5R)-3-[[4-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
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C25H27FN8O2
 1
1
EC50 = 8.1 nM
   TI
   LI
   LO
   TS
CP0397597
S-propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carbothioate
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C22H27FN4O4S2
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0397673
phenyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carbodithioate
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C25H25FN4O3S3
 1
1
EC50 = 12.59 nM
   TI
   LI
   LO
   TS
CP0523536
1,1,1,3,3,3-hexafluoropropan-2-yl 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C30H28F6N2O5S
 1
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0062434
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-methylphenyl]methylidene]pyrrolidine-2,5-dione
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C27H29N5O3S
 1
1
EC50 = 18 nM
   TI
   LI
   LO
   TS
CP0541311
tert-butyl 4-[4-[[4-[(E)-(2,5-dioxopyrrolidin-3-ylidene)methyl]-2-methylphenoxy]methyl]-1,3-thiazol-2-yl]piperidine-1-carboxylate
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C26H31N3O5S
 1
1
EC50 = 19 nM
   TI
   LI
   LO
   TS
CP0507615
tert-butyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C23H29FN4O5S
 1
1
EC50 = 19.95 nM
   TI
   LI
   LO
   TS
CP0397608
3-fluoro-4-[[5-fluoro-6-[4-[3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl]pyrimidin-4-yl]amino]-N,N-dimethylbenzamide
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C23H26F3N7O2
 1
1
EC50 = 23.4 nM
   TI
   LI
   LO
   TS
CP0389508
2-methylpropyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C23H29FN4O5S
 1
1
EC50 = 25.12 nM
   TI
   LI
   LO
   TS
CP0513071
(1-methylcyclopropyl) 4-[[7-(2-fluoro-4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
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C24H27FN4O4S2
 1
1
EC50 = 26 nM
   TI
   LI
   LO
   TS
CP0460668
3-fluoro-4-[[5-fluoro-6-[4-[3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl]pyrimidin-4-yl]amino]-N-methylbenzamide
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C22H24F3N7O2
 1
1
EC50 = 27 nM
   TI
   LI
   LO
   TS
CP0508640
3-fluoro-4-[[5-fluoro-6-[4-[3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl]pyrimidin-4-yl]amino]benzamide
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C21H22F3N7O2
 1
1
EC50 = 28.2 nM
   TI
   LI
   LO
   TS
CP0389493
S-ethyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carbothioate
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C21H25FN4O4S2
 1
1
EC50 = 31.62 nM
   TI
   LI
   LO
   TS
CP0517584
tert-butyl (1R,5S)-3-[8-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate
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C25H26FN7O3
 1
1
EC50 = 36 nM
   TI
   LI
   LO
   TS
CP0419572
tert-butyl 4-[methyl-[7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]amino]piperidine-1-carboxylate
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C24H30N4O4S2
 1
1
EC50 = 39 nM
   TI
   LI
   LO
   TS
CP0500584
2,2-dimethylpropyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C24H31FN4O5S
 1
1
EC50 = 39.81 nM
   TI
   LI
   LO
   TS
CP0417502
7-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidine
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C26H28N6O3S
 1
1
EC50 = 41 nM
   TI
   LI
   LO
   TS
CP0495698
7-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]-4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidine
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C24H23ClN6O3S
 1
1
EC50 = 42 nM
   TI
   LI
   LO
   TS
CP0562987
tert-butyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
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C25H28N4O6S
 1
1
EC50 = 43 nM
   TI
   LI
   LO
   TS
CP0471846
tert-butyl (1R,5S)-3-[[4-(4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
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C25H31N7O4S
 1
1
EC50 = 44 nM
   TI
   LI
   LO
   TS
CP0377360
tert-butyl 4-[3-[(3-oxo-1,2-dihydroinden-5-yl)amino]propyl]piperidine-1-carboxylate
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C22H32N2O3
 1
1
EC50 = 46 nM
   TI
   LI
   LO
   TS
CP0412076
tert-butyl 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C31H36N2O5S
 1
1
EC50 = 46 nM
   TI
   LI
   LO
   TS
CP0097714
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-fluorophenyl]methylidene]pyrrolidine-2,5-dione
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C26H26FN5O3S
 1
1
EC50 = 49 nM
   TI
   LI
   LO
   TS
CP0559074
tert-butyl (1S,4S,5S)-5-[[4-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-2-azabicyclo[2.2.2]octane-2-carboxylate
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C25H27FN8O2
 1
1
EC50 = 49 nM
   TI
   LI
   LO
   TS
CP0368437
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C22H27FN4O5S
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0500585
butyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C23H29FN4O5S
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0538951
1-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-4-ol
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C10H17N3O2
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0852737
(S)-1,1-Dimethylethyl 4-({1-[4-(Methylsulfinyl)phenyl]-2,3-dihydro-1H-indol-4-yl}oxy)-1-piperidinecarboxylate
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C22H27FN4O4S
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0445388
6-[3-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]propylamino]-2,3-dihydroinden-1-one
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C23H30N4O
 1
1
EC50 = 51 nM
   TI
   LI
   LO
   TS
CP0847394
tert-butyl 4-(3-(3-oxo-2,3-dihydrobenzofuran-6-ylamino)propyl)piperidine-1-carboxylate
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C21H30N2O4
 1
1
EC50 = 52 nM
   TI
   LI
   LO
   TS
CP0513902
tert-butyl 4-[4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
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C25H30N4O5S
 1
1
EC50 = 53 nM
   TI
   LI
   LO
   TS
CP0482538
tert-butyl 4-[[7-[3-fluoro-4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
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C26H32FN5O4S
 1
1
EC50 = 53 nM
   TI
   LI
   LO
   TS
CP0359455
[(2R)-1,1,1-trifluoropropan-2-yl] 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C30H31F3N2O5S
 1
1
EC50 = 54 nM
   TI
   LI
   LO
   TS
CP0478754
tert-butyl 6-[4-(benzylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C32H37NO5S
 1
1
EC50 = 56 nM
   TI
   LI
   LO
   TS
CP0512840
tert-butyl 4-[7-[3-fluoro-4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C25H29FN4O5S
 1
1
EC50 = 57 nM
   TI
   LI
   LO
   TS
CP0423368
6-[3-[1-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-4-yl]propylamino]-2,3-dihydroinden-1-one
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C22H30N4O2
 1
1
EC50 = 58 nM
   TI
   LI
   LO
   TS
CP0462603
propan-2-yl 4-[[7-(4-cyano-2-fluorophenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C22H24FN5O3
 1
1
EC50 = 63.1 nM
   TI
   LI
   LO
   TS
CP0544815
tert-butyl 4-[7-[4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C25H30N4O5S
 1
1
EC50 = 64 nM
   TI
   LI
   LO
   TS
CP0534193
propan-2-yl 4-[[7-[3-fluoro-4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
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C25H30FN5O4S
 1
1
EC50 = 67 nM
   TI
   LI
   LO
   TS
CP0389389
tert-butyl 6-[4-(pyridin-3-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C31H36N2O5S
 1
1
EC50 = 68 nM
   TI
   LI
   LO
   TS
CP0912750
6-(3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
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C21H28N4O3
 1
1
EC50 = 73 nM
   TI
   LI
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   TS
CP0482540
tert-butyl 4-[[6-[3-fluoro-4-[methoxy(methyl)carbamoyl]phenyl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C25H32FN3O5
 1
1
EC50 = 73 nM
   TI
   LI
   LO
   TS
CP0552249
2-methylpropyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
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C25H28N4O6S
 1
1
EC50 = 75.1 nM
   TI
   LI
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   TS
CP0468704
4-[5-[[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]methoxy]pyridin-2-yl]-2-fluoro-N-methoxy-N-methylbenzamide
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C26H30FN5O3
 1
1
EC50 = 77 nM
   TI
   LI
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   TS
CP0417501
1-[2-[4-[4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidin-7-yl]piperidin-1-yl]pyrimidin-5-yl]ethanone
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C26H26N6O4S
 1
1
EC50 = 78 nM
   TI
   LI
   LO
   TS
CP0478402
tert-butyl 4-[4-(2-fluoro-4-methylsulfonylanilino)thieno[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
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C23H27FN4O4S2
 1
1
EC50 = 79 nM
   TI
   LI
   LO
   TS
CP0381374
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]sulfanyl]piperidine-1-carboxylate
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C22H27FN4O4S2
 1
1
EC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0389509
propan-2-yl 4-[[7-[2-fluoro-4-(1,3-thiazol-2-yl)phenyl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C24H26FN5O3S
 1
1
EC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0499453
propyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C22H27FN4O5S
 1
1
EC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0500583
5-[4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole
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C23H27FN6O4S
 1
1
EC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0410630
propan-2-yl 4-[methyl-[7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]amino]piperidine-1-carboxylate
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C23H28N4O4S2
 1
1
EC50 = 82 nM
   TI
   LI
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   TS
CP0557640
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-fluorophenyl]methylidene]-1-phenylpyrrolidine-2,5-dione
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C32H30FN5O3S
 1
1
EC50 = 82 nM
   TI
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   TS
CP0489053
tert-butyl 4-[methyl-[7-[4-(phenylmethoxycarbamoyl)phenyl]thieno[3,2-d]pyrimidin-4-yl]amino]piperidine-1-carboxylate
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C31H35N5O4S
 1
1
EC50 = 83 nM
   TI
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   TS
CP0428973
tert-butyl 4-[3-[(1-oxo-2,3-dihydroinden-5-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C22H32N2O3
 1
1
EC50 = 86 nM
   TI
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CP0062435
2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole
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C22H24N8OS
 1
1
EC50 = 87 nM
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CP0847395
tert-butyl 4-(3-(3-oxo-2,3-dihydrobenzofuran-5-ylamino)propyl)piperidine-1-carboxylate
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C21H30N2O4
 1
1
EC50 = 88 nM
   TI
   LI
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   TS
CP0560133
tert-butyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C25H28N4O6S
 1
1
EC50 = 88 nM
   TI
   LI
   LO
   TS
CP0532358
propan-2-yl 4-[[6-[4-(cyclohexylmethylsulfonyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C26H42N4O5S
 1
1
EC50 = 90 nM
   TI
   LI
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   TS
CP0544816
propan-2-yl 4-[[6-[3-fluoro-4-[methoxy(methyl)carbamoyl]phenyl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C24H30FN3O5
 1
1
EC50 = 92 nM
   TI
   LI
   LO
   TS
CP0489058
tert-butyl 4-[[7-[4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
   Show/Hide
C26H33N5O4S
 1
1
EC50 = 98 nM
   TI
   LI
   LO
   TS
CP0536877
tert-butyl 6-[4-(pyridin-4-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
   Show/Hide
C31H36N2O5S
 1
1
EC50 = 98 nM
   TI
   LI
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   TS
CP0430837
propan-2-yl 4-[[6-(4-butylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C23H38N4O5S
 1
1
EC50 = 100 nM
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CP0389502
propan-2-yl 4-[[7-(2-methyl-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C23H30N4O5S
 1
1
EC50 = 100 nM
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CP0500582
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-2-methyl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C23H29FN4O5S
 1
1
EC50 = 100 nM
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CP0537782
tert-butyl 4-[7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C23H27N3O5S2
 1
1
EC50 = 100 nM
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CP0429715
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-fluorophenyl]methylidene]pyrrolidin-2-one
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C26H28FN5O2S
 1
1
EC50 = 100 nM
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CP0412074
(1,1,1-trifluoro-2-methylpropan-2-yl) 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C31H33F3N2O5S
 1
1
EC50 = 101 nM
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CP0541309
tert-butyl 4-[4-[[4-(tetrazol-1-yl)phenoxy]methyl]-1,3-thiazol-2-yl]piperidine-1-carboxylate
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C21H26N6O3S
 1
1
EC50 = 103 nM
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CP0470487
4-[4-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]oxythieno[3,2-d]pyrimidin-7-yl]-2-fluoro-N-methoxy-N-methylbenzamide
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C26H27FN6O3S
 1
1
EC50 = 105 nM
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CP0514788
benzyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
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C28H26N4O6S
 1
1
EC50 = 105.7 nM
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CP0425755
benzyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C27H24N4O6S
 1
1
EC50 = 107.4 nM
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CP0883016
6-(3-(1-(5-methoxypyrimidin-2-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
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C21H26N4O3
 1
1
EC50 = 115 nM
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CP0883015
6-(3-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
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C22H28N4O2
 1
1
EC50 = 117 nM
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CP0882141
6-(3-(1-(3-isopropyl-1,2,4-thiadiazol-5-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
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C21H28N4O2S
 1
1
EC50 = 121 nM
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CP0492299
tert-butyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C24H26N4O6S
 1
1
EC50 = 125.3 nM
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CP0408799
tert-butyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-2-methyl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C24H31FN4O5S
 1
1
EC50 = 125.89 nM
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CP0441815
propan-2-yl 4-[[7-(5-methylsulfonylpyridin-2-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C21H27N5O5S
 1
1
EC50 = 125.89 nM
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CP0507183
propan-2-yl 4-[[7-(4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C22H28N4O5S
 1
1
EC50 = 125.89 nM
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CP0392576
[(2S)-1,1,1-trifluoropropan-2-yl] 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C30H31F3N2O5S
 1
1
EC50 = 126 nM
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CP0536878
propan-2-yl 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C30H34N2O5S
 1
1
EC50 = 128 nM
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CP0547831
tert-butyl 4-[4-(2-fluoro-4-methylsulfonylanilino)furo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
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C23H27FN4O5S
 1
1
EC50 = 129 nM
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CP0560134
tert-butyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C24H26N4O6S
 1
1
EC50 = 130 nM
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CP0537779
1-[4-[[7-(2-fluoro-4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidin-1-yl]-2-methylpropan-1-one
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C23H27FN4O3S2
 1
1
EC50 = 140 nM
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CP0514151
tert-butyl 6-[4-(propan-2-ylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C28H37NO5S
 1
1
EC50 = 142 nM
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CP0409533
tert-butyl 4-[5-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-5-yl)amino]pentyl]piperidine-1-carboxylate
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C23H36N2O4S
 1
1
EC50 = 145 nM
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CP0416546
tert-butyl 4-[[4-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]piperidine-1-carboxylate
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C23H25FN8O2
 1
1
EC50 = 147 nM
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CP0873797
methyl 2-(4-(3-(3-oxo-2,3-dihydrobenzofuran-6-ylamino)propyl)piperidin-1-yl)pyrimidine-5-carboxylate
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C22H26N4O4
 1
1
EC50 = 149 nM
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CP0493089
benzyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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C27H24N4O6S
 1
1
EC50 = 153.4 nM
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CP0543533
propan-2-yl 4-[[6-[4-[methoxy(methyl)carbamoyl]phenyl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C24H31N3O5
 1
1
EC50 = 155 nM
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CP0482539
propan-2-yl 4-[[7-[4-[methoxy(methyl)carbamoyl]phenyl]thieno[3,2-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
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C25H31N5O4S
 1
1
EC50 = 156 nM
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CP0541310
tert-butyl 4-[4-[[4-[(E)-(2,5-dioxopyrrolidin-3-ylidene)methyl]-2-fluorophenoxy]methyl]-1,3-thiazol-2-yl]piperidine-1-carboxylate
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C25H28FN3O5S
 1
1
EC50 = 157 nM
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CP0549422
ethyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
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C23H24N4O6S
 1
1
EC50 = 157.4 nM
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CP0397674
propan-2-yl 4-[[7-[2-fluoro-4-(1-methylpyrrol-2-yl)phenyl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C26H30FN5O3
 1
1
EC50 = 158.49 nM
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CP0462600
tert-butyl 4-[[1-(4-methylsulfonylphenyl)-2,3-dihydroindol-4-yl]oxy]piperidine-1-carboxylate
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C25H32N2O5S
 1
1
EC50 = 158.49 nM
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CP0488622
propan-2-yl 4-[[7-(3-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C22H27FN4O5S
 1
1
EC50 = 158.49 nM
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CP0862997
6-(3-(1-(5-isopropyl-1,2,4-oxadiazol-3-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
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C21H28N4O3
 1
1
EC50 = 161 nM
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CP0514153
2,2,2-trifluoroethyl 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C29H29F3N2O5S
 1
1
EC50 = 169 nM
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CP0481096
tert-butyl 4-[[6-[4-[methoxy(methyl)carbamoyl]phenyl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C25H33N3O5
 1
1
EC50 = 171 nM
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CP0539742
cyclopropyl-[4-[methyl-[7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]amino]piperidin-1-yl]methanone
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C23H26N4O3S2
 1
1
EC50 = 173 nM
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CP0552609
tert-butyl (1S,4S,5S)-5-[[4-(4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-2-azabicyclo[2.2.2]octane-2-carboxylate
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C25H31N7O4S
 1
1
EC50 = 179 nM
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CP0511664
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]phenyl]methylidene]pyrrolidine-2,5-dione
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C26H27N5O3S
 1
1
EC50 = 182 nM
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CP0489054
4-[4-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]oxythieno[3,2-d]pyrimidin-7-yl]-N-methoxy-N-methylbenzamide
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C26H28N6O3S
 1
1
EC50 = 199 nM
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CP0498634
propan-2-yl 4-[[6-(4-cyclohexylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C25H40N4O5S
 1
1
EC50 = 200 nM
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CP0441812
5-nitro-6-(4-pyridin-2-ylsulfanylpiperidin-1-yl)-N-[4-(1,2,4-triazol-1-yl)phenyl]pyrimidin-4-amine
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C22H21N9O2S
 1
1
EC50 = 200 nM
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CP0483142
7-[1-(5-fluoropyrimidin-2-yl)piperidin-4-yl]-4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidine
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C24H23FN6O3S
 1
1
EC50 = 201 nM
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CP0377358
tert-butyl 4-[4-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-5-yl)amino]butyl]piperidine-1-carboxylate
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C22H34N2O4S
 1
1
EC50 = 210 nM
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CP0404229
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3,5-difluorophenyl]methylidene]pyrrolidine-2,5-dione
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C26H25F2N5O3S
 1
1
EC50 = 211 nM
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CP0443932
ethyl 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
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C29H32N2O5S
 1
1
EC50 = 235 nM
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CP0419571
4-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]oxy-7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidine
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C24H25N5O3S2
 1
1
EC50 = 240 nM
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CP0559934
(3E)-3-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-fluorophenyl]methylidene]-1-(oxan-4-ylmethyl)pyrrolidine-2,5-dione
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C32H36FN5O4S
 1
1
EC50 = 240 nM
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CP0391279
5-[4-[[7-(2-fluoro-4-methylsulfonylphenyl)-2-methyl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole
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C24H29FN6O4S
 1
1
EC50 = 251.19 nM
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CP0413836
propan-2-yl 4-[[7-(6-methylsulfonylpyridin-3-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C21H27N5O5S
 1
1
EC50 = 251.19 nM
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CP0507182
S-methyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carbothioate
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C20H23FN4O4S2
 1
1
EC50 = 251.19 nM
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CP0544374
ethyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C21H25FN4O5S
 1
1
EC50 = 251.19 nM
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CP0494082
7-[1-(5-methylpyrimidin-2-yl)piperidin-4-yl]-4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidine
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C25H26N6O3S
 1
1
EC50 = 252 nM
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CP0445387
tert-butyl 4-[3-[(3,3-dioxo-1,3lambda6-benzoxathiol-6-yl)amino]propyl]piperidine-1-carboxylate
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C20H30N2O5S
 1
1
EC50 = 254 nM
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CP0409532
tert-butyl 4-[3-[(1,1-dioxo-2,3-dihydro-1lambda6,2,3-benzothiadiazol-5-yl)amino]propyl]piperidine-1-carboxylate
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C19H30N4O4S
 1
1
EC50 = 268 nM
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CP0502941
tert-butyl 4-[3-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-5-yl)amino]propyl]piperidine-1-carboxylate
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C21H32N2O4S
 1
1
EC50 = 270 nM
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CP0497650
tert-butyl 4-[3-[(4-oxo-2,3-dihydrochromen-6-yl)amino]propyl]piperidine-1-carboxylate
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C22H32N2O4
 1
1
EC50 = 272 nM
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CP0400301
propan-2-yl 4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C22H36N4O5S
 1
1
EC50 = 300 nM
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CP0458941
propan-2-yl 4-[[6-[4-(2-methoxyethylsulfonyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C22H36N4O6S
 1
1
EC50 = 300 nM
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CP0498631
propan-2-yl 4-[[6-(4-propan-2-ylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C22H36N4O5S
 1
1
EC50 = 300 nM
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CP0417503
7-[1-(5-methoxypyrimidin-2-yl)piperidin-4-yl]-4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidine
   Show/Hide
C25H26N6O4S
 1
1
EC50 = 310 nM
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CP0381375
4-hydroxypiperidine-1-carbonitrile
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C6H10N2O
 1
1
EC50 = 316.23 nM
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CP0389494
methyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C20H23FN4O5S
 1
1
EC50 = 316.23 nM
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CP0507614
2-methoxyethyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C22H27FN4O6S
 1
1
EC50 = 316.23 nM
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CP0512841
4-[5-[[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]methoxy]pyridin-2-yl]-N-methoxy-N-methylbenzamide
   Show/Hide
C26H31N5O3
 1
1
EC50 = 319 nM
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CP0475366
tert-butyl 4-[[6-[4-(oxazinane-2-carbonyl)phenyl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
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C27H35N3O5
 1
1
EC50 = 321 nM
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CP0514152
3-[[4-[1'-[(2-methylpropan-2-yl)oxycarbonyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-6-yl]phenyl]methylsulfonylmethyl]benzoic acid
   Show/Hide
C33H37NO7S
 1
1
EC50 = 321 nM
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CP0443933
2-[[4-[1'-[(2-methylpropan-2-yl)oxycarbonyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-6-yl]phenyl]methylsulfonylmethyl]benzoic acid
   Show/Hide
C33H37NO7S
 1
1
EC50 = 334 nM
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CP0517583
tert-butyl 4-[[4-(4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]piperidine-1-carboxylate
   Show/Hide
C23H29N7O4S
 1
1
EC50 = 345 nM
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CP0494084
tert-butyl 4-[7-(2-fluoro-4-methylsulfonylanilino)-[1,2]oxazolo[4,5-d]pyrimidin-3-yl]piperidine-1-carboxylate
   Show/Hide
C22H26FN5O5S
 1
1
EC50 = 353 nM
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   TS
CP0412075
4-[[4-[1'-[(2-methylpropan-2-yl)oxycarbonyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-6-yl]phenyl]methylsulfonylmethyl]benzoic acid
   Show/Hide
C33H37NO7S
 1
1
EC50 = 360 nM
   TI
   LI
   LO
   TS
CP0440217
tert-butyl 6-[4-(methylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
   Show/Hide
C26H33NO5S
 1
1
EC50 = 369 nM
   TI
   LI
   LO
   TS
CP0408601
2-[4-[4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidin-7-yl]piperidin-1-yl]pyrimidin-5-ol
   Show/Hide
C24H24N6O4S
 1
1
EC50 = 391 nM
   TI
   LI
   LO
   TS
CP0389505
propan-2-yl 4-[[7-(4-cyano-3-fluorophenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C22H24FN5O3
 1
1
EC50 = 398.11 nM
   TI
   LI
   LO
   TS
CP0441814
propan-2-yl 4-[[7-(3-fluoro-4-methylsulfanylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C22H27FN4O3S
 1
1
EC50 = 398.11 nM
   TI
   LI
   LO
   TS
CP0462601
4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]-N,N-dimethylpiperidine-1-sulfonamide
   Show/Hide
C20H26FN5O5S2
 1
1
EC50 = 398.11 nM
   TI
   LI
   LO
   TS
CP0552608
tert-butyl (1S,5R)-3-[[4-(2-fluoro-4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
   Show/Hide
C25H30FN7O4S
 1
1
EC50 = 452 nM
   TI
   LI
   LO
   TS
CP0389499
propan-2-yl 4-[[1-(4-methylsulfonylphenyl)-2,3-dihydroindol-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C24H30N2O5S
 1
1
EC50 = 501.19 nM
   TI
   LI
   LO
   TS
CP0397598
propan-2-yl 4-[[7-(4-dimethylsulfinamoylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C23H31N5O4S
 1
1
EC50 = 501.19 nM
   TI
   LI
   LO
   TS
CP0462599
2-fluoroethyl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C21H24F2N4O5S
 1
1
EC50 = 501.19 nM
   TI
   LI
   LO
   TS
CP0470607
tert-butyl 4-[3-[(4,4-dioxo-2,3-dihydro-1,4lambda6-benzoxathiin-7-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C21H32N2O5S
 1
1
EC50 = 511 nM
   TI
   LI
   LO
   TS
CP0478401
4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)-7-(1-pyrimidin-2-ylpiperidin-4-yl)furo[3,2-d]pyrimidine
   Show/Hide
C24H24N6O3S
 1
1
EC50 = 512 nM
   TI
   LI
   LO
   TS
CP0377359
tert-butyl 4-[3-[(1-oxo-2,3-dihydroisoindol-5-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C21H31N3O3
 1
1
EC50 = 550 nM
   TI
   LI
   LO
   TS
CP0483141
1-[2-[4-[4-(5-methylsulfonyl-2,3-dihydroindol-1-yl)furo[3,2-d]pyrimidin-7-yl]piperidin-1-yl]pyrimidin-5-yl]ethanol
   Show/Hide
C26H28N6O4S
 1
1
EC50 = 586 nM
   TI
   LI
   LO
   TS
CP0389496
tert-butyl 4-[1-(4-methylsulfonylphenyl)indol-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C25H30N2O5S
 1
1
EC50 = 630.96 nM
   TI
   LI
   LO
   TS
CP0427709
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]-methylamino]piperidine-1-carboxylate
   Show/Hide
C23H30FN5O4S
 1
1
EC50 = 630.96 nM
   TI
   LI
   LO
   TS
CP0852738
(R)-1,1-Dimethylethyl 4-({1-[4-(Methylsulfinyl)phenyl]-2,3-dihydro-1H-indol-4-yl}oxy)-1-piperidinecarboxylate
   Show/Hide
C22H27FN4O4S
 1
1
EC50 = 630.96 nM
   TI
   LI
   LO
   TS
CP0447587
propan-2-yl 4-[2-[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxyethyl]piperidine-1-carboxylate
   Show/Hide
C23H38N4O5S
 1
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0862996
6-(3-(1-(5-isopropyl-1,3,4-oxadiazol-2-yl)piperidin-4-yl)propylamino)benzofuran-3(2H)-one
   Show/Hide
C21H28N4O3
 1
1
EC50 = 704 nM
   TI
   LI
   LO
   TS
CP0389391
1'-(5-chloropyrimidin-2-yl)-6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]
   Show/Hide
C30H29ClN4O3S
 1
1
EC50 = 716 nM
   TI
   LI
   LO
   TS
CP0511759
2-methylpropyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C24H26N4O6S
 1
1
EC50 = 720 nM
   TI
   LI
   LO
   TS
CP0409535
tert-butyl 4-[3-[(3-oxo-1,2-dihydroisoindol-5-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C21H31N3O3
 1
1
EC50 = 734 nM
   TI
   LI
   LO
   TS
CP0502942
tert-butyl 4-[3-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-5-yl)oxy]propyl]piperidine-1-carboxylate
   Show/Hide
C21H31NO5S
 1
1
EC50 = 736 nM
   TI
   LI
   LO
   TS
CP0532856
2-methylpropyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C24H26N4O6S
 1
1
EC50 = 745 nM
   TI
   LI
   LO
   TS
CP0489884
tert-butyl 4-[3-[(5-oxo-6,7,8,9-tetrahydrobenzo[7]annulen-2-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C24H36N2O3
 1
1
EC50 = 770 nM
   TI
   LI
   LO
   TS
CP0548544
(5Z)-5-[[4-[[2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-1,3-thiazol-4-yl]methoxy]-3-fluorophenyl]methylidene]-1,3-thiazolidine-2,4-dione
   Show/Hide
C25H24FN5O3S2
 1
1
EC50 = 780 nM
   TI
   LI
   LO
   TS
CP0508165
2-methyl-1-[4-[methyl-[7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-yl]amino]piperidin-1-yl]propan-1-one
   Show/Hide
C23H28N4O3S2
 1
1
EC50 = 781 nM
   TI
   LI
   LO
   TS
CP0425649
ethyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C22H22N4O6S
 1
1
EC50 = 790 nM
   TI
   LI
   LO
   TS
CP0463409
tert-butyl 4-[4-(6-methylsulfonyl-3,4-dihydro-2H-quinolin-1-yl)furo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
   Show/Hide
C26H32N4O5S
 1
1
EC50 = 793 nM
   TI
   LI
   LO
   TS
CP0413754
propan-2-yl 4-[[2-amino-7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C22H28FN5O5S
 1
1
EC50 = 794.33 nM
   TI
   LI
   LO
   TS
CP0486968
propan-2-yl 4-[[7-(5-cyanopyridin-2-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C21H24N6O3
 1
1
EC50 = 794.33 nM
   TI
   LI
   LO
   TS
CP0532359
N-tert-butyl-4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxamide
   Show/Hide
C23H39N5O4S
 1
1
EC50 = 800 nM
   TI
   LI
   LO
   TS
CP0549421
benzyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C28H26N4O6S
 1
1
EC50 = 805 nM
   TI
   LI
   LO
   TS
CP0552845
ethyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C22H22N4O6S
 1
1
EC50 = 819 nM
   TI
   LI
   LO
   TS
CP0452227
N-(4-propan-2-ylphenyl)-4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxamide
   Show/Hide
C28H41N5O4S
 1
1
EC50 = 900 nM
   TI
   LI
   LO
   TS
CP0506167
propan-2-yl 4-[[6-(4-piperidin-1-ylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C24H39N5O5S
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0533386
N-propan-2-yl-4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxamide
   Show/Hide
C22H37N5O4S
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0500587
propan-2-yl 4-[[1-(2-fluoro-4-methylsulfonylphenyl)-2,3-dihydroindol-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C24H29FN2O5S
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0552610
tert-butyl 4-[8-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C23H24FN7O3
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0377361
tert-butyl 4-[3-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-6-yl)amino]propyl]piperidine-1-carboxylate
   Show/Hide
C21H32N2O4S
 1
1
EC50 = 1029 nM
   TI
   LI
   LO
   TS
CP0400302
propan-2-yl 4-[[6-[4-(diethylsulfamoyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C23H39N5O5S
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0504560
propan-2-yl 4-[2-[6-(4-ethylsulfonylpiperazin-1-yl)pyridin-3-yl]oxyethyl]piperidine-1-carboxylate
   Show/Hide
C22H36N4O5S
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0537781
N-methyl-7-(4-methylsulfonylphenyl)-N-(1-propan-2-ylsulfonylpiperidin-4-yl)thieno[3,2-d]pyrimidin-4-amine
   Show/Hide
C22H28N4O4S3
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0537783
N-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-N-methyl-7-(4-methylsulfonylphenyl)thieno[3,2-d]pyrimidin-4-amine
   Show/Hide
C25H28N6O2S2
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0507617
7-(2-fluoro-4-methylsulfonylphenyl)-4-(1-propan-2-ylsulfonylpiperidin-4-yl)oxy-5,6-dihydropyrrolo[2,3-d]pyrimidine
   Show/Hide
C21H27FN4O5S2
 1
1
EC50 = 1258.93 nM
   TI
   LI
   LO
   TS
CP0496118
propan-2-yl 4-[[6-(4-ethylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C21H34N4O5S
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0548545
tert-butyl (1R,5S)-3-[[4-(4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
   Show/Hide
C25H31N7O4S
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0425648
methyl 4-[6-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C22H22N4O6S
 1
1
EC50 = 1414 nM
   TI
   LI
   LO
   TS
CP0462083
4-(1-ethylsulfonylpiperidin-4-yl)oxy-7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidine
   Show/Hide
C20H25FN4O5S2
 1
1
EC50 = 1584.89 nM
   TI
   LI
   LO
   TS
CP0498633
3-methyl-1-(4-((6-(4-(propylsulfonyl)piperazin-1-yl)pyridin-3-yloxy)methyl)piperidin-1-yl)butan-1-one
   Show/Hide
C23H38N4O4S
 1
1
EC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0547027
tert-butyl (1S,5R)-3-[[4-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-8-azabicyclo[3.2.1]octane-8-carboxylate
   Show/Hide
C25H27FN8O2
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0430679
propan-2-yl 4-[[6-(4-thiophen-2-ylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C23H32N4O5S2
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0492298
methyl 4-[6-[3-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]pyrimidin-4-yl]oxypiperidine-1-carboxylate
   Show/Hide
C21H20N4O6S
 1
1
EC50 = 1870 nM
   TI
   LI
   LO
   TS
CP0498630
propan-2-yl 4-[[6-[4-(furan-2-carbonyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C24H32N4O5
 1
1
EC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0396591
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]amino]piperidine-1-carboxylate
   Show/Hide
C22H28FN5O4S
 1
1
EC50 = 1995.26 nM
   TI
   LI
   LO
   TS
CP0507181
7-(2-fluoro-4-methylsulfonylphenyl)-4-[1-(1,4,5,6-tetrahydropyrimidin-2-yl)piperidin-4-yl]oxy-5,6-dihydropyrrolo[2,3-d]pyrimidine
   Show/Hide
C22H27FN6O3S
 1
1
EC50 = 1995.26 nM
   TI
   LI
   LO
   TS
CP0447590
furan-2-yl-[4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidin-1-yl]methanone
   Show/Hide
C23H32N4O5S
 1
1
EC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0498632
propan-2-yl 4-[[6-(4-pyridin-3-ylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C24H33N5O5S
 1
1
EC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0430680
propan-2-yl 4-[6-(4-ethylsulfonylpiperazin-1-yl)pyridin-3-yl]oxypiperidine-1-carboxylate
   Show/Hide
C20H32N4O5S
 1
1
EC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0477488
2,2-difluoro-1-(4-((6-(4-(propylsulfonyl)piperazin-1-yl)pyridin-3-yloxy)methyl)piperidin-1-yl)ethanone
   Show/Hide
C20H30F2N4O4S
 1
1
EC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0547029
tert-butyl (1S,4S,5R)-5-[[4-(2-fluoro-4-methylsulfonylanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-2-azabicyclo[2.2.2]octane-2-carboxylate
   Show/Hide
C25H30FN7O4S
 1
1
EC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0532357
propan-2-yl 4-[[6-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C22H36N4O4
 1
1
EC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0489448
tert-butyl 4-[4-[(1,1-dioxo-2,3-dihydro-1-benzothiophen-5-yl)amino]-4-oxobutyl]piperidine-1-carboxylate
   Show/Hide
C22H32N2O5S
 1
1
EC50 = 2610 nM
   TI
   LI
   LO
   TS
CP0447588
3,3-dimethyl-1-(4-((6-(4-(propylsulfonyl)piperazin-1-yl)pyridin-3-yloxy)methyl)piperidin-1-yl)butan-1-one
   Show/Hide
C24H40N4O4S
 1
1
EC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0438908
propan-2-yl 4-[[6-[4-(dimethylcarbamoyl)piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C22H35N5O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0447589
N-cyclohexyl-4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxamide
   Show/Hide
C25H41N5O4S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0452108
propan-2-yl 4-[[6-[4-[2-oxo-2-(propan-2-ylamino)ethyl]piperazin-1-yl]pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C24H39N5O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0470415
morpholin-4-yl-[4-[[6-(4-propylsulfonylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidin-1-yl]methanone
   Show/Hide
C23H37N5O5S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0498642
propan-2-yl 4-[[6-(4-acetylpiperazin-1-yl)pyridin-3-yl]oxymethyl]piperidine-1-carboxylate
   Show/Hide
C21H32N4O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0389506
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-6-methyl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C23H29FN4O5S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0389507
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]sulfonyl]piperidine-1-carboxylate
   Show/Hide
C22H27FN4O6S2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0397672
propan-2-yl 4-[[7-(5-fluoropyridin-2-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
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C20H24FN5O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0462082
propan-2-yl 4-[[7-(2-fluoro-4-methylsulfonylphenyl)-2-(methylamino)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C23H30FN5O5S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0507616
2-[4-[[7-(2-fluoro-4-methylsulfonylphenyl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidin-1-yl]-N,N-dimethylacetamide
   Show/Hide
C22H28FN5O4S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0553352
propan-2-yl 4-[[7-(2-methylpyridin-3-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylate
   Show/Hide
C21H27N5O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0547031
tert-butyl (1R,5S)-3-[8-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-4-yl]oxy-8-azabicyclo[3.2.1]octane-8-carboxylate
   Show/Hide
C25H26FN7O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0552607
tert-butyl (1S,4S,5R)-5-[[4-(4-cyano-2-fluoroanilino)pyrimido[5,4-d]pyrimidin-8-yl]amino]-2-azabicyclo[2.2.2]octane-2-carboxylate
   Show/Hide
C25H27FN8O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0408600
tert-butyl 4-[4-(2-fluoro-N-methyl-4-methylsulfonylanilino)furo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
   Show/Hide
C24H29FN4O5S
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0460783
tert-butyl 4-[4-(2-fluoro-4-methylsulfonylanilino)-5-methylpyrrolo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
   Show/Hide
C24H30FN5O4S
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0478405
tert-butyl 4-[4-(2-fluoro-4-methylsulfonylanilino)-5H-pyrrolo[3,2-d]pyrimidin-7-yl]piperidine-1-carboxylate
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C23H28FN5O4S
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0426564
tert-butyl 6-[4-(2-methylsulfonylethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
   Show/Hide
C27H35NO5S
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0426566
tert-butyl 6-(4-methylsulfonylphenyl)spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
   Show/Hide
C25H31NO5S
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0062435
2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole
   Show/Hide
C22H24N8OS
 1
1 EC50 = 3.9 nM
CP0204778
6-[[2-fluoro-3-[1-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-4-yl]propyl]amino]-2,3-dihydroinden-1-one
   Show/Hide
C22H29FN4O2
 1
1 EC50 = 33 nM
CP0359455
[(2R)-1,1,1-trifluoropropan-2-yl] 6-[4-(pyridin-2-ylmethylsulfonylmethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
   Show/Hide
C30H31F3N2O5S
 1
1 EC50 = 54 nM
CP0035557
(Z)-N-(2-hydroxyethyl)octadec-9-enamide
   Show/Hide
C20H39NO2
 2
1 EC50 = 930 nM
2 EC50 = 3200 nM
CP0215429
tert-butyl 4-[(3-pyridin-4-yl-1,2,4-oxadiazol-5-yl)methoxy]piperidine-1-carboxylate
   Show/Hide
C18H24N4O4
 1
1 EC50 = 5130 nM
CP0310370
4-[(4-cyano-2-fluorophenoxy)methyl]-2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]pyrazole-3-carbonitrile
   Show/Hide
C23H22FN7O
 1
1 Ki = 9.25 nM
CP0282904
2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazole-3-carbonitrile
   Show/Hide
C23H24N10O
 1
1 Ki = 14.9 nM
CP0388345
(1-methylcyclopropyl) 4-[5-cyano-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazol-1-yl]piperidine-1-carboxylate
   Show/Hide
C22H24N8O3
 1
1 Ki = 29.8 nM
CP0210924
(1-methylcyclopropyl) 4-[5-cyano-4-[(4-cyano-2-fluorophenoxy)methyl]pyrazol-1-yl]piperidine-1-carboxylate
   Show/Hide
C22H22FN5O3
 1
1 Ki = 36.5 nM
CP0210925
(1-methylcyclopropyl) 4-[5-cyano-4-[[2-fluoro-4-(1-methyltetrazol-5-yl)phenoxy]methyl]pyrazol-1-yl]piperidine-1-carboxylate
   Show/Hide
C23H25FN8O3
 1
1 Ki = 99 nM
Clinical Information about the Protein
Target 1 ( Glucose-dependent insulinotropic receptor (GPR119) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
2 Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s) 1 Approved Drug  1
1 Guanfacine extended release Approved
Attention deficit hyperactivity disorder
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 GSK1292263 Phase 2
Type-2 diabetes
2 SAR-260093 Phase 2
Type-2 diabetes
3 APD-597 Phase 1
Type-2 diabetes
4 BMS-903452 Phase 1
Type-2 diabetes
Discontinued Drug(s) 1 Discontinued Drug  1
1 APD668 Discontinued in Phase 1
Type-2 diabetes
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01297 Glucose-dependent insulinotropic receptor Rattus norvegicus, Rat