General Information of the Protein
Protein ID
PT01717
Protein Name
Adenosine receptor A1
Gene Name
ADORA1
Sequence
MPPYISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGALVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKTVVTQRRAAVAIAGCWILSLVVGLTPMFGWNNLSVVEQDWRANGSVGEPVIKCEFEKVISMEYMVYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALILFLFALSWLPLHILNCITLFCPTCQKPSILIYIAIFLTHGNSAMNPIVYAFRIHKFRVTFLKIWNDHFRCQPKPPIDEDLPEEKAED
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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. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
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Uniprot ID
P25099
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
CP0362924
(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 = 0.34 nM
   TI
   LI
   LO
   TS
CP0039632
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-N-cyclopropyl-3,4-dihydroxyoxolane-2-carboxamide
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C13H16N6O4
 1
1
Ki = 6.4 nM
   TI
   LI
   LO
   TS
CP0378926
(1S,2R,3S,4R,5S)-4-(2-chloro-6-(cyclopentylamino)-9H-purin-9-yl)-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamide
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C18H23ClN6O3
 1
1
Ki = 17.4 nM
   TI
   LI
   LO
   TS
CP0211418
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-N-cyclobutyl-3,4-dihydroxyoxolane-2-carboxamide
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C14H18N6O4
 1
1
Ki = 43 nM
   TI
   LI
   LO
   TS
CP0039348
(2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,4-dihydroxyoxolane-2-carboxamide
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C12H16N6O4
 1
1
Ki = 63 nM
   TI
   LI
   LO
   TS
CP0217091
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxy-N-methyloxolane-2-carboxamide
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C11H14N6O4
 1
1
Ki = 84 nM
   TI
   LI
   LO
   TS
CP0118650
(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 = 140 nM
   TI
   LI
   LO
   TS
CP0316519
(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 = 198 nM
   TI
   LI
   LO
   TS
CP0435131
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-N-(2-chloroethyl)-3,4-dihydroxyoxolane-2-carboxamide
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C12H15ClN6O4
 1
1
Ki = 248 nM
   TI
   LI
   LO
   TS
CP0378001
(2-chloropurin-9-yl)-3,4-dihydroxytetrahydrothiphene-2-carboxylic acid methyl amide
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C11H13ClN6O3S
 1
1
Ki = 294 nM
   TI
   LI
   LO
   TS
CP0039042
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 = 305 nM
   TI
   LI
   LO
   TS
CP0379088
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-N-cyclopentyl-3,4-dihydroxyoxolane-2-carboxamide
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C15H20N6O4
 1
1
Ki = 770 nM
   TI
   LI
   LO
   TS
CP0017043
(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 = 820 nM
   TI
   LI
   LO
   TS
CP0198142
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxy-N-(2,2,2-trifluoroethyl)oxolane-2-carboxamide
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C12H13F3N6O4
 1
1
Ki = 1190 nM
   TI
   LI
   LO
   TS
CP0198141
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxy-N-propyloxolane-2-carboxamide
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C13H18N6O4
 1
1
Ki = 1240 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0039348
(2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,4-dihydroxyoxolane-2-carboxamide
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C12H16N6O4
 5
1 IC50 = 10 nM
2 IC50 = 52000 nM
3 IC50 = 90000 nM
4 Ki = 6.3 nM
5 Ki = 10.3 nM
CP0362924
(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 = 0.34 nM
CP0058033
1,3-dipropyl-8-cyclopentylxanthine
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C16H24N4O2
 7
1 Ki = 0.46 nM
2 Ki = 0.5 nM
3 Ki = 0.6166 nM
4 Ki = 0.77 nM
5 Ki = 0.9 nM
6 Ki = 1.2 nM
7 Ki = 1.46 nM
CP0077413
(2R,3R,4S,5R)-2-(2-Chloro-6-cyclopentylamino-purin-9-yl)-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C15H20ClN5O4
 1
1 Ki = 0.6 nM
CP0330238
(2R,3R,4S,5R)-2-[6-(9H-fluoren-9-ylmethylamino)purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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C24H23N5O4
 1
1 Ki = 5.2 nM
CP0146806
(2R,3R,4S,5R)-2-[6-(2,2-Diphenyl-ethylamino)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C24H25N5O4
 1
1 Ki = 6.8 nM
CP0001102
(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
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C10H13N5O4
 1
1 Ki = 10 nM
CP0083663
8-(2-Hydroxy-4-methoxy-phenyl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
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C18H22N4O4
 1
1 Ki = 11 nM
CP0150055
8-Cyclopentyl-1-propyl-3,7-dihydro-purine-2,6-dione
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C13H18N4O2
 1
1 Ki = 14 nM
CP0255221
8-(2,4-Dihydroxy-phenyl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
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C17H20N4O4
 1
1 Ki = 15 nM
CP0069838
(4-Cyano-phenyl)-carbamic acid 4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-phenyl ester
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C26H26N6O4
 1
1 Ki = 16.8 nM
CP0277937
8-(2,3-Dihydroxy-phenyl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
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C17H20N4O4
 1
1 Ki = 33 nM
CP0018686
(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 = 54 nM
CP0301653
8-(2,5-Dihydroxy-phenyl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
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C17H20N4O4
 1
1 Ki = 360 nM
CP0017043
(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 = 820 nM
CP0042654
1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
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C7H8N4O2
 2
1 Ki = 8500 nM
2 Ki = 14000 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT05020 Adenosine receptor A1 Mus musculus, Mouse
50% Identity
Protein ID Protein Name Protein Organism
PT00840 Adenosine receptor A1 Homo sapiens, Human