General Information of the Protein
Protein ID
PT06277
Protein Name
Probable G-protein coupled receptor 139
Secondarily
Protein Name
G(q)-coupled orphan receptor GPRg1
G-protein-coupled receptor PGR3
Gene Name
GPR139
Secondarily
Gene Name
GPRG1
PGR3
Sequence
MEHTHAHLAANSSLSWWSPGSACGLGFVPVVYYSLLLCLGLPANILTVIILSQLVARRQKSSYNYLLALAAADILVLFFIVFVDFLLEDFILNMQMPQVPDKIIEVLEFSSIHTSIWITVPLTIDRYIAVCHPLKYHTVSYPARTRKVIVSVYITCFLTSIPYYWWPNIWTEDYISTSVHHVLIWIHCFTVYLVPCSIFFILNSIIVYKLRRKSNFRLRGYSTGKTTAILFTITSIFATLWAPRIIMILYHLYGAPIQNRWLVHIMSDIANMLALLNTAINFFLYCFISKRFRTMAAATLKAFFKCQKQPVQFYTNHNFSITSSPWISPANSHCIKMLVYQYDKNGKPIKVSP
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
Function
Orphan receptor. Seems to act through a G(q/11)-mediated pathway.
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Uniprot ID
Primary ID:
Q6DWJ6

Secondarily ID:
A8K5R9
Q86SP2
Q8TDU8
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Ensembl ID
ENSG00000180269
HGNC ID
HGNC:19995
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0868363
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(8-(4-methylpiperazin-1-yl)-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C20H23ClFN7O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0870177
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(6-fluoro-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C15H13ClFN5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0870178
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(5,7-dimethyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C17H17ClFN5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0870313
 Compound Info 
(S)-2-(5-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C17H16F3N5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0870328
 Compound Info 
(S)-2-(8-amino-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H19N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0870331
 Compound Info 
(S)-2-(5-(3-hydroxyazetidin-1-yl)-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C20H20F3N5O4
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0870332
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(5-morpholino-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C20H21ClFN5O3
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0887597
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(5-(4-methylpiperazin-1-yl)-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C21H24ClFN6O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0903316
 Compound Info 
(S)-2-(7-methoxy-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H19N5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0903344
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(8-iodo-3-oxo-[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)acetamide
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C15H12ClFIN5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0903346
 Compound Info 
(S)-2-(6-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H19N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0911968
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(3-oxo-8-(piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C20H22ClFN6O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0914629
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(6-fluoro-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C15H12ClF2N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0914630
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C17H15F3N4O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0922696
 Compound Info 
(S)-2-(7-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C17H16F3N5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0942934
 Compound Info 
N-((S)-1-(4-chloro-3-fluorophenyl)ethyl)-2-(5-(3-methylmorpholino)-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C21H23ClFN5O3
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0942935
 Compound Info 
(S)-tert-butyl(3-oxo-2-(2-oxo-2-((1-(p-tolyl)ethyl)amino)ethyl)-2,3-dihydro-[1,2,4]triazolo[4,3-a]pyridin-8-yl)carbamate
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C22H27N5O4
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0943679
 Compound Info 
N-((S)-1-(4-chloro-3-fluorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)propanamide
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C16H15ClFN5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0943681
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C15H13ClFN5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0943682
 Compound Info 
(S)-N-(1-(3,4-dichlorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C15H13Cl2N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0943687
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C16H14F3N5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0943688
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(6-chloro-3-oxo-[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)acetamide
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C15H12Cl2FN5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0943697
 Compound Info 
(S)-N-(1-(4-(difluoromethoxy)-3-fluorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C17H15F3N4O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0954296
 Compound Info 
(S)-2-(8-chloro-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H17ClN4O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0955712
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(3-oxo-8-(piperazin-1-yl)-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C19H21ClFN7O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0955715
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(7-methoxy-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C16H16ClN5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0956047
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(5,7-dimethyl-3-oxo-[1,2,4]triazolo[4,3-c]pyrimidin-2(3H)-yl)acetamide
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C17H18ClN5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0958445
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(6-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C16H15ClFN5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0958447
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(5,7-dimethyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C17H18ClN5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0958688
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(8-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C16H15ClFN5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0958689
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(8-(oxetan-3-ylamino)-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C18H18ClFN6O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0958693
 Compound Info 
(S)-2-(6-bromo-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H17BrN4O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0958694
 Compound Info 
(S)-2-(8-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C17H16F3N5O3
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0958695
 Compound Info 
(S)-2-(6-methyl-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C17H16F3N5O3
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0961052
 Compound Info 
(S)-2-(5-bromo-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H17BrN4O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0962196
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(7-iodo-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C16H13ClFIN4O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0962200
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-c]pyrimidin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C16H17N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0962207
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(8-(methylamino)-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)acetamide
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C16H16ClFN6O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0962208
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C16H15ClN4O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0964630
 Compound Info 
(S)-N-(1-(4-chloro-3-fluorophenyl)ethyl)-2-(5-(3,3-difluoroazetidin-1-yl)-3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C19H17ClF3N5O2
  1
1
EC50 < 1 nM
 Bioactivity Info 
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CP0969626
 Compound Info 
(S)-2-(5,7-dimethyl-3-oxo-[1,2,4]triazolo[4,3-c]pyrimidin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C18H21N5O2
  1
1
EC50 = 1 nM
 Bioactivity Info 
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CP0870310
 Compound Info 
(S)-N-(1-(4-cyclopropylphenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)acetamide
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C18H19N5O2
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0870312
 Compound Info 
(S)-2-(3-oxo-6-(piperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C21H23F3N6O3
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0903218
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C16H17N5O2
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0903315
 Compound Info 
(S)-N-(1-(4-chlorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C15H14ClN5O2
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0903317
 Compound Info 
(S)-N-(1-(4-isopropoxyphenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C19H22N4O3
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0914625
 Compound Info 
(S)-N-(1-(4-(difluoromethoxy)-3-fluorophenyl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)acetamide
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C16H14F3N5O3
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0955717
 Compound Info 
(S)-2-(3-oxo-5-(piperazin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C21H23F3N6O3
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0956044
 Compound Info 
N-((4-chlorophenyl)(cyclopropyl)methyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C18H17ClN4O2
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0958696
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide
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C16H14F3N5O3
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0962194
 Compound Info 
(S)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C16H17N5O2
  1
1
EC50 = 10 nM
 Bioactivity Info 
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CP0870299
 Compound Info 
2-(3-oxo-8-(pyrrolidin-3-yl)-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-((S)-1-(p-tolyl)ethyl)acetamide
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C21H25N5O2
  1
1
EC50 >= 100 nM
 Bioactivity Info 
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CP0943684
 Compound Info 
(S)-N-(1-(5-fluoropyridin-3-yl)ethyl)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)acetamide
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C15H14FN5O2
  1
1
EC50 >= 100 nM
 Bioactivity Info 
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CP0960360
 Compound Info 
(S)-2-(8-(azetidin-3-yloxy)-3-oxo-[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-N-(1-(4-chloro-3-fluorophenyl)ethyl)acetamide
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C18H18ClFN6O3
  1
1
EC50 >= 100 nM
 Bioactivity Info 
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CP0960979
 Compound Info 
(R)-2-(3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(1-(p-tolyl)ethyl)acetamide
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C17H18N4O2
  1
1
EC50 >= 100 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000308 , T-REx-CHO
 Cell Line Info 
Clinical Information about the Protein
Target 1 ( G-protein-coupled receptor PGR3 (GPR139) )
Target Type Clinical trial Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06789 Probable G-protein coupled receptor 139 Rattus norvegicus, Rat
 Protein Info