General Information of the Protein
Protein ID
PT01274
Protein Name
Adenosine kinase
Secondarily
Protein Name
Adenosine 5'-phosphotransferase
Gene Name
ADK
Sequence
MAAAEEEPKPKKLKVEAPQALRENILFGMGNPLLDISAVVDKDFLDKYSLKPNDQILAEDKHKELFDELVKKFKVEYHAGGSTQNSIKVAQWMIQQPHKAATFFGCIGIDKFGEILKRKAAEAHVDAHYYEQNEQPTGTCAACITGDNRSLIANLAAANCYKKEKHLDLEKNWMLVEKARVCYIAGFFLTVSPESVLKVAHHASENNRIFTLNLSAPFISQFYKESLMKVMPYVDILFGNETEAATFAREQGFETKDIKEIAKKTQALPKMNSKRQRIVIFTQGRDDTIMATESEVTAFAVLDQDQKEIIDTNGAGDAFVGGFLSQLVSDKPLTECIRAGHYAASIIIRRTGCTFPEKPDFH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Catalyzes the phosphorylation of the purine nucleoside adenosine at the 5' position in an ATP-dependent manner. Serves as a potential regulator of concentrations of extracellular adenosine and intracellular adenine nucleotides.
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Uniprot ID
Primary ID:
P55263

Secondarily ID:
B7Z783
B7Z800
O00741
O00742
Q16710
Q5JQ10
Q5JQ11
Q9BTN2
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Ensembl ID
ENSG00000156110
HGNC ID
HGNC:257
Subcellular Location
Nucleus
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: CL000016 , IMR-32
Compound ID Compound Name Compound Formula
CP0071313
(2R,3R,4S,5R)-2-(2-amino-9-iodo-3,5,7-triazabicyclo[4.3.0]nona-1,3,5,8-tetraen-7-yl)-5-methyl-oxolane-3,4-diol
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C11H13IN4O3
 1
1
IC50 = 22.8 nM
   TI
   LI
   LO
   TS
CP0528733
5-(4-Bromo-thiophen-2-yl)-6-(3,4-dimethoxy-phenyl)-7-thiophen-2-yl-pyrido[2,3-d]pyrimidin-4-ylamine
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C23H17BrN4O2S2
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0198332
5-(3-Bromo-phenyl)-7-(6-dimethylamino-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C20H17BrN6
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0550871
5,6-Diphenyl-7-thiophen-2-yl-pyrido[2,3-d]pyrimidin-4-ylamine
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C23H16N4S
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0103761
5-(3-Bromo-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C22H19BrN6O
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0507642
7-(6-Dimethylamino-pyridin-3-yl)-5,6-diphenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C26H22N6
 1
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
CP0437004
5-(3-Chloro-phenyl)-7-(6-dimethylamino-pyridin-3-yl)-6-phenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C26H21ClN6
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0518331
5-(3-Chloro-phenyl)-6-(4-dimethylamino-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C30H28ClN7O
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0138070
(2R,3R,4S,5R)-2-[4-(4-Fluoro-phenylamino)-5-phenyl-pyrrolo[2,3-d]pyrimidin-7-yl]-5-methyl-tetrahydro-furan-3,4-diol
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C23H21FN4O3
 1
1
IC50 = 134 nM
   TI
   LI
   LO
   TS
CP0492876
5-(3-Bromo-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-6-phenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C28H23BrN6O
 1
1
IC50 = 155 nM
   TI
   LI
   LO
   TS
CP0402039
methyl 2-[4-amino-5-(3-bromophenyl)-7-thiophen-2-ylpyrido[2,3-d]pyrimidin-6-yl]acetate
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C20H15BrN4O2S
 1
1
IC50 = 163 nM
   TI
   LI
   LO
   TS
CP0200853
5-(3-Bromo-phenyl)-7-(4-dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H18BrN5
 1
1
IC50 = 167 nM
   TI
   LI
   LO
   TS
CP0383205
5-(3-Bromo-phenyl)-6-(4-fluoro-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C28H22BrFN6O
 1
1
IC50 = 197 nM
   TI
   LI
   LO
   TS
CP0425859
7-(4-Dimethylamino-phenyl)-5,6-diphenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C27H23N5
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0431457
5,6-Bis-(3-fluoro-4-methyl-phenyl)-7-thiophen-2-yl-pyrido[2,3-d]pyrimidin-4-ylamine
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C25H18F2N4S
 1
1
IC50 = 288 nM
   TI
   LI
   LO
   TS
CP0366798
7-(4-Dimethylamino-phenyl)-6-phenyl-pteridin-4-ylamine
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C20H18N6
 1
1
IC50 = 333 nM
   TI
   LI
   LO
   TS
CP0480643
5-(3-Bromo-phenyl)-6-(3,4-dimethoxy-phenyl)-7-(4-dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C29H26BrN5O2
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0460157
5-(4-Bromo-thiophen-2-yl)-6-(3,4-dimethoxy-phenyl)-7-{4-[(2-methoxy-ethyl)-methyl-amino]-phenyl}-pyrido[2,3-d]pyrimidin-4-ylamine
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C29H28BrN5O3S
 1
1
IC50 = 367 nM
   TI
   LI
   LO
   TS
CP0406658
6-Benzyl-5-(3-bromo-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C29H25BrN6O
 1
1
IC50 = 450 nM
   TI
   LI
   LO
   TS
CP0047724
7-(4-Dimethylamino-phenyl)-5-phenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H19N5
 1
1
IC50 = 467 nM
   TI
   LI
   LO
   TS
CP0134601
5-Cyclohexyl-7-(4-dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H25N5
 1
1
IC50 = 467 nM
   TI
   LI
   LO
   TS
CP0166322
7-(4-Dimethylamino-phenyl)-6-p-tolyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C22H21N5
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0281006
7-(4-Dimethylamino-phenyl)-6-(4-methoxy-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C22H21N5O
 1
1
IC50 = 567 nM
   TI
   LI
   LO
   TS
CP0448113
5-(3-Bromo-phenyl)-7-(6-dimethylamino-pyridin-3-yl)-6-pentyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C25H27BrN6
 1
1
IC50 = 625 nM
   TI
   LI
   LO
   TS
CP0495479
5-(4-Bromo-thiophen-2-yl)-6-cyclopropyl-7-(6-dimethylamino-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H19BrN6S
 1
1
IC50 = 625 nM
   TI
   LI
   LO
   TS
CP0079164
3-[4-Amino-7-(4-dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-6-yl]-benzoic acid methyl ester
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C23H21N5O2
 1
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
CP0276766
7-(4-Morpholin-4-yl-phenyl)-pteridin-4-ylamine
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C16H16N6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0281868
7-(4-Dimethylamino-phenyl)-6-phenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H19N5
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0076829
7-(4-Dimethylamino-phenyl)-pteridin-4-ylamine
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C14H14N6
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0257633
(2R,3S,4R,5R)-2-Aminomethyl-5-(6-amino-purin-9-yl)-tetrahydro-furan-3,4-diol
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C10H14N6O3
 1
1
IC50 = 6330 nM
   TI
   LI
   LO
   TS
CP0049447
7-(4-Dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C15H15N5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0078974
7-Phenyl-pteridin-4-ylamine
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C12H9N5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0220501
7-(4-Methoxy-phenyl)-pteridin-4-ylamine
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C13H11N5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0252859
7-(4-Amino-phenyl)-pteridin-4-ylamine
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C12H10N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
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CP0366787
7-(4-Nitro-phenyl)-pteridin-4-ylamine
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C12H8N6O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0382304
7-(4-Chloro-phenyl)-4-morpholin-4-yl-pteridine
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C16H14ClN5O
 1
1
IC50 = 22000 nM
   TI
   LI
   LO
   TS
CP0179736
(2R,3R,4S,5R)-2-(6-Amino-5-nitro-pyrimidin-4-ylamino)-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C9H13N5O6
 1
1
IC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0161822
6-(4-tert-Butyl-phenyl)-7-(4-dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C25H27N5
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0399477
7-(4-Dimethylamino-phenyl)-5,6-bis-(4-isopropyl-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C33H35N5
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0503565
5-(3-Bromo-phenyl)-6-isopropyl-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C25H25BrN6O
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0505927
5-(3-Bromo-phenyl)-6-cyclohexyl-7-(6-dimethylamino-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C26H27BrN6
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0071313
(2R,3R,4S,5R)-2-(2-amino-9-iodo-3,5,7-triazabicyclo[4.3.0]nona-1,3,5,8-tetraen-7-yl)-5-methyl-oxolane-3,4-diol
   Show/Hide
C11H13IN4O3
 2
1 IC50 = 0.9 nM
2 IC50 = 9 nM
CP0103761
5-(3-Bromo-phenyl)-7-(6-morpholin-4-yl-pyridin-3-yl)-pyrido[2,3-d]pyrimidin-4-ylamine
   Show/Hide
C22H19BrN6O
 3
1 IC50 = 1.3 nM
2 IC50 = 1.7 nM
3 IC50 = 2 nM
CP0138070
(2R,3R,4S,5R)-2-[4-(4-Fluoro-phenylamino)-5-phenyl-pyrrolo[2,3-d]pyrimidin-7-yl]-5-methyl-tetrahydro-furan-3,4-diol
   Show/Hide
C23H21FN4O3
 2
1 IC50 = 1.5 nM
2 IC50 = 5 nM
CP0281006
7-(4-Dimethylamino-phenyl)-6-(4-methoxy-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C22H21N5O
 1
1 IC50 = 92 nM
CP0257633
(2R,3S,4R,5R)-2-Aminomethyl-5-(6-amino-purin-9-yl)-tetrahydro-furan-3,4-diol
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C10H14N6O3
 1
1 IC50 = 170 nM
CP0281868
7-(4-Dimethylamino-phenyl)-6-phenyl-pyrido[2,3-d]pyrimidin-4-ylamine
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C21H19N5
 1
1 IC50 = 350 nM
CP0076829
7-(4-Dimethylamino-phenyl)-pteridin-4-ylamine
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C14H14N6
 1
1 IC50 = 440 nM
CP0049447
7-(4-Dimethylamino-phenyl)-pyrido[2,3-d]pyrimidin-4-ylamine
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C15H15N5
 1
1 IC50 = 773 nM
CP0179736
(2R,3R,4S,5R)-2-(6-Amino-5-nitro-pyrimidin-4-ylamino)-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C9H13N5O6
 1
1 Ki = 300 nM
Clinical Information about the Protein
Target 1 ( Adenosine kinase (ADK) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Epilepsy [ICD-11: 8A60-8A68]
2 Pain [ICD-11: MG30-MG3Z]
Discontinued Drug(s) 3 Discontinued Drugs  3
1 A-134974 Terminated
Epilepsy
2 ABT-702 Terminated
Pain
3 GP-683 Terminated
Pain