General Information of the Protein
Protein ID
PT01608
Protein Name
Adenosine receptor A2a
Gene Name
ADORA2A
Sequence
MGSSVYITVELAIAVLAILGNVLVCWAVWINSNLQNVTNFFVVSLAAADIAVGVLAIPFAITISTGFCAACHGCLFFACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGVRAKGIIAICWVLSFAIGLTPMLGWNNCSQKDGNSTKTCGEGRVTCLFEDVVPMNYMVYYNFFAFVLLPLLLMLAIYLRIFLAARRQLKQMESQPLPGERTRSTLQKEVHAAKSLAIIVGLFALCWLPLHIINCFTFFCSTCRHAPPWLMYLAIILSHSNSVVNPFIYAYRIREFRQTFRKIIRTHVLRRQEPFQAGGSSAWALAAHSTEGEQVSLRLNGHPLGVWANGSATHSGRRPNGYTLGLGGGGSAQGSPRDVELPTQERQEGQEHPGLRGHLVQARVGASSWSSEFAPS
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Nucleotide-like receptor (family A GPCR)
>
Adenosine receptor
Function
Receptor for adenosine (By similarity). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (PubMed:23994616).
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Uniprot ID
P30543
Ensembl ID
ENSG00000128271
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0415983
 Compound Info 
3-ethyl-6-(4-hydroxypiperidine-1-carbonyl)-5-methyl-1-(3,3,3-trifluoropropyl)thieno[2,3-d]pyrimidine-2,4-dione
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C18H22F3N3O4S
  1
1
IC50 = 750 nM
 Bioactivity Info 
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CP0399741
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-[6-(3-methoxyazetidin-1-yl)pyridin-2-yl]pyrimidin-4-yl]acetamide
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C20H23N7O2
  1
1
Ki = 1.5 nM
 Bioactivity Info 
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CP0130086
 Compound Info 
8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione
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C20H24N4O4
  1
1
Ki = 2 nM
 Bioactivity Info 
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CP0053494
 Compound Info 
4-(2-{[5-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-yl]amino}ethyl)phenol
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C16H15N7O2
  1
1
Ki = 2.8 nM
 Bioactivity Info 
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CP0373930
 Compound Info 
N-[6-(3,5-dimethoxyphenyl)-2-(3,5-dimethylpyrazol-1-yl)pyrimidin-4-yl]acetamide
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C19H21N5O3
  1
1
Ki = 3 nM
 Bioactivity Info 
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CP0127357
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-[6-(4-methylpiperazin-1-yl)pyridin-2-yl]pyrimidin-4-yl]acetamide
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C21H26N8O
  1
1
Ki = 7 nM
 Bioactivity Info 
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CP0482762
 Compound Info 
N-[2-[4-(8-amino-3-oxo-2-phenyl-[1,2,4]triazolo[4,3-a]pyrazin-6-yl)phenoxy]ethyl]-5-(dithiolan-3-yl)pentanamide
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C27H30N6O3S2
  1
1
Ki = 9 nM
 Bioactivity Info 
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CP0310128
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-[6-(morpholin-4-yl)pyridin-2-yl]pyrimidin-4-yl]acetamide
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C20H23N7O2
  1
1
Ki = 10 nM
 Bioactivity Info 
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CP0373931
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-[6-(4-hydroxypiperidin-1-yl)pyridin-2-yl]pyrimidin-4-yl]acetamide
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C21H25N7O2
  1
1
Ki = 10 nM
 Bioactivity Info 
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CP0405015
 Compound Info 
N-[2-(furan-2-yl)-6-(1,3-thiazol-2-yl)pyrimidin-4-yl]-2-(4-methylpiperazin-1-yl)acetamide
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C18H20N6O2S
  1
1
Ki = 11 nM
 Bioactivity Info 
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CP0497739
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(2-fluoro-3-methoxyphenyl)pyrimidin-4-yl]acetamide
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C18H18FN5O2
  1
1
Ki = 12 nM
 Bioactivity Info 
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CP0427854
 Compound Info 
N-[6-(3,5-dimethylpyrazol-1-yl)-2-(furan-2-yl)pyrimidin-4-yl]-2-(4-methylpiperazin-1-yl)acetamide
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C20H25N7O2
  1
1
Ki = 14 nM
 Bioactivity Info 
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CP0394856
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3S)-3-[(dimethylamino)methyl]piperidin-1-yl]acetamide
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C24H33N7O2
  1
1
Ki = 14 nM
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CP0439413
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-{6-[(2-methoxyethyl)(methyl)amino]pyridin-2-yl}pyrimidin-4-yl]acetamide
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C20H25N7O2
  1
1
Ki = 14 nM
 Bioactivity Info 
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CP0466764
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-[6-(dimethylamino)pyridin-2-yl]pyrimidin-4-yl]acetamide
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C18H21N7O
  1
1
Ki = 20 nM
 Bioactivity Info 
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CP0375126
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(5-methoxypyridin-3-yl)pyrimidin-4-yl]propanamide
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C18H20N6O2
  1
1
Ki = 21 nM
 Bioactivity Info 
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CP0427857
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-{4-[(dimethylamino)methyl]piperidin-1-yl}acetamide
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C24H33N7O2
  1
1
Ki = 25 nM
 Bioactivity Info 
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CP0037365
 Compound Info 
N-[2-(furan-2-yl)-6-pyrazol-1-ylpyrimidin-4-yl]-2-(4-methylpiperazin-1-yl)acetamide
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C18H21N7O2
  1
1
Ki = 26 nM
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CP0372841
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3S)-3-[(dimethylamino)methyl]pyrrolidin-1-yl]acetamide
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C23H31N7O2
  1
1
Ki = 27.8 nM
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CP0377319
 Compound Info 
(2R,3R,4S,5S)-4-Amino-5-hydroxymethyl-2-[6-(3-iodo-benzylamino)-purin-9-yl]-tetrahydro-furan-3-ol
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C17H19IN6O3
  1
1
Ki = 28 nM
 Bioactivity Info 
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CP0467978
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(5-methoxypyridin-3-yl)pyrimidin-4-yl]-2-(morpholin-4-yl)acetamide
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C21H25N7O3
  1
1
Ki = 30 nM
 Bioactivity Info 
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CP0373932
 Compound Info 
N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(5-hydroxypyridin-3-yl)pyrimidin-4-yl]acetamide
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C16H16N6O2
  1
1
Ki = 32 nM
 Bioactivity Info 
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CP0436314
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3R)-3-[(dimethylamino)methyl]pyrrolidin-1-yl]acetamide
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C23H31N7O2
  1
1
Ki = 34 nM
 Bioactivity Info 
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CP0427855
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3S)-3-(ethylamino)pyrrolidin-1-yl]acetamide
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C22H29N7O2
  1
1
Ki = 37 nM
 Bioactivity Info 
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CP0479029
 Compound Info 
2-[4-(8-amino-3-oxo-2-phenyl-[1,2,4]triazolo[4,3-a]pyrazin-6-yl)phenoxy]acetonitrile
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C19H14N6O2
  1
1
Ki = 39 nM
 Bioactivity Info 
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CP0422562
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-3-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]propanamide
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C23H31N7O2
  1
1
Ki = 41 nM
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CP0372840
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-3-(dimethylamino)propanamide
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C19H24N6O2
  1
1
Ki = 43 nM
 Bioactivity Info 
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CP0427858
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(4-methyl-1,4-diazepan-1-yl)acetamide
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C22H29N7O2
  1
1
Ki = 46.7 nM
 Bioactivity Info 
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CP0040740
 Compound Info 
N-[2-(3,5-dimethylpyrazol-1-yl)-6-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]pyrimidin-4-yl]acetamide
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C17H24N6O2
  1
1
Ki = 48 nM
 Bioactivity Info 
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CP0272424
 Compound Info 
N-[2-(3,5-dimethylpyrazol-1-yl)-6-(5-methoxypyridin-3-yl)pyrimidin-4-yl]acetamide
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C17H18N6O2
  1
1
Ki = 62 nM
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CP0462579
 Compound Info 
methyl N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(5-methoxypyridin-3-yl)pyrimidin-4-yl]carbamate
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C17H18N6O3
  1
1
Ki = 68 nM
 Bioactivity Info 
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CP0462580
 Compound Info 
ethyl N-[2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-(5-methoxypyridin-3-yl)pyrimidin-4-yl]carbamate
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C18H20N6O3
  1
1
Ki = 82 nM
 Bioactivity Info 
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CP0445899
 Compound Info 
N-[3-[4-(8-amino-3-oxo-2-phenyl-[1,2,4]triazolo[4,3-a]pyrazin-6-yl)anilino]-3-oxopropyl]-3,5-ditert-butyl-4-hydroxybenzamide
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C35H39N7O4
  1
1
Ki = 86 nM
 Bioactivity Info 
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CP0394857
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3R)-3-[(dimethylamino)methyl]piperidin-1-yl]acetamide
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C24H33N7O2
  1
1
Ki = 87 nM
 Bioactivity Info 
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CP0372833
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(1-methylpiperidin-4-yl)acetamide
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C22H28N6O2
  1
1
Ki = 103 nM
 Bioactivity Info 
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CP0169910
 Compound Info 
JMC511730 Compound 1
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C21H27N7O2
  1
1
Ki = 131.3 nM
 Bioactivity Info 
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CP0403160
 Compound Info 
2-[(3S)-3-(diethylamino)pyrrolidin-1-yl]-N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]acetamide
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C24H33N7O2
  1
1
Ki = 155 nM
 Bioactivity Info 
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CP0433201
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]acetamide
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C22H29N7O2
  1
1
Ki = 160 nM
 Bioactivity Info 
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CP0403158
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(4-acetylpiperazin-1-yl)acetamide
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C22H27N7O3
  1
1
Ki = 170 nM
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CP0372836
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(1,4-oxazepan-4-yl)acetamide
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C21H26N6O3
  1
1
Ki = 230 nM
 Bioactivity Info 
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CP0412622
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(4-ethylpiperazin-1-yl)acetamide
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C22H29N7O2
  1
1
Ki = 270 nM
 Bioactivity Info 
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CP0118650
 Compound Info 
(2S,3S,4R,5R)-5-(2-chloro-6-(3-iodobenzylamino)-9H-purin-9-yl)-3,4-dihydroxy-N-methyltetrahydrothiophene-2-carboxamide
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C18H18ClIN6O3S
  1
1
Ki = 348 nM
 Bioactivity Info 
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CP0372834
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(morpholin-4-yl)acetamide
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C20H24N6O3
  1
1
Ki = 430 nM
 Bioactivity Info 
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CP0017043
 Compound Info 
(2S,3S,4R,5R)-5-(2-chloro-6-{[(3-iodophenyl)methyl]amino}-9H-purin-9-yl)-3,4-dihydroxy-N-methyloxolane-2-carboxamide
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C18H18ClIN6O4
  1
1
Ki = 470 nM
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CP0372839
 Compound Info 
N-[6-(3,5-dimethyl-1H-pyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(4-methoxypiperidin-1-yl)acetamide
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C22H28N6O3
  1
1
Ki = 1600 nM
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CP0316519
 Compound Info 
(2S,3S,4R,5R)-5-(2-chloro-6-(methylamino)-9H-purin-9-yl)-3,4-dihydroxy-N-methyltetrahydrothiophene-2-carboxamide
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C12H15ClN6O3S
  1
1
Ki = 6340 nM
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CP0065233
 Compound Info 
4-(2,6-Dioxo-1-propyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-benzenesulfonic acid
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C14H14N4O5S
  1
1
Ki = 24000 nM
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CP0183628
 Compound Info 
(2S,3S,4R,5R)-5-(6-Amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-carboxylic acid (2-amino-ethyl)-amide
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C12H17N7O4
  1
1
Ki > 10 nM
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CP0257633
 Compound Info 
(2R,3S,4R,5R)-2-Aminomethyl-5-(6-amino-purin-9-yl)-tetrahydro-furan-3,4-diol
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C10H14N6O3
  1
1
Ki > 10 nM
 Bioactivity Info 
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CP0409614
 Compound Info 
4-Amino-2-(6-cyclopentylamino-purin-9-yl)-5-hydroxymethyl-tetrahydro-furan-3-ol
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C15H22N6O3
  1
1
Ki > 10 nM
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CP0426831
 Compound Info 
2-[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]guanidine
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C11H16N8O3
  1
1
Ki > 10 nM
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CP0430608
 Compound Info 
2'-AMINO-2'-DEOXYADENOSINE
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C10H14N6O3
  1
1
Ki > 10 nM
 Bioactivity Info 
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CP0460291
 Compound Info 
4-Amino-5-[2-chloro-6-(3-iodo-benzylamino)-purin-9-yl]-tetrahydro-furan-2-carboxylic acid methylamide
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C18H19ClIN7O2
  1
1
Ki > 10 nM
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CP0467103
 Compound Info 
3'-amino-3'-deoxyadenosine
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C10H14N6O3
  1
1
Ki > 10 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000868 , PC12
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0039348
 Compound Info 
(2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,4-dihydroxyoxolane-2-carboxamide
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C12H16N6O4
  4
1 IC50 = 7.05 nM
2 IC50 = 366 nM
3 Ki = 7.8 nM
4 Ki = 10.3 nM
CP0053494
 Compound Info 
4-(2-{[5-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-yl]amino}ethyl)phenol
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C16H15N7O2
  1
1 Ki = 2 nM
CP0130086
 Compound Info 
8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione
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C20H24N4O4
  2
1 Ki = 4.4 nM
2 Ki = 4.46 nM
CP0039042
 Compound Info 
N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
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C21H14ClN5O2
  1
1 Ki = 10.3 nM
CP0018686
 Compound Info 
(2S,3S,4R,5R)-3,4-Dihydroxy-5-[6-(3-iodo-benzylamino)-purin-9-yl]-tetrahydro-furan-2-carboxylic acid methylamide
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C18H19IN6O4
  1
1 Ki = 56 nM
CP0017043
 Compound Info 
(2S,3S,4R,5R)-5-(2-chloro-6-{[(3-iodophenyl)methyl]amino}-9H-purin-9-yl)-3,4-dihydroxy-N-methyloxolane-2-carboxamide
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C18H18ClIN6O4
  1
1 Ki = 470 nM
CP0362924
 Compound Info 
(2R,3R,4S,5R)-2-[6-[[(1R,2S,4S)-2-bicyclo[2.2.1]heptanyl]amino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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C17H23N5O4
  1
1 Ki = 477 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06256 Adenosine receptor A2a Mus musculus, Mouse
 Protein Info