General Information of the Protein
Protein ID
PT04241
Protein Name
Equilibrative nucleoside transporter 1
Secondarily
Protein Name
Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter
Nucleoside transporter
es-type
Solute carrier family 29 member 1
Gene Name
SLC29A1
Secondarily
Gene Name
ENT1
Sequence
MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDAQASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAILLVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQGLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKLEGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIFTITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRWLPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPKKVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC28 and SLC29 families of nucleoside transporters
>
SLC29 Facilitative nucleoside transporter family
Function
Uniporter involved in the facilitative transport of nucleosides and nucleobases, and contributes to maintaining their cellular homeostasis (PubMed:8986748, PubMed:10755314, PubMed:12527552, PubMed:10722669, PubMed:21795683, PubMed:35790189, PubMed:27995448, PubMed:17379602, PubMed:14759222, PubMed:15037197, PubMed:26406980). Functions as a Na(+)-independent transporter (PubMed:8986748). Involved in the transport of nucleosides such as adenosine, guanosine, inosine, uridine, thymidine and cytidine (PubMed:8986748, PubMed:10755314, PubMed:12527552, PubMed:10722669, PubMed:17379602, PubMed:14759222, PubMed:15037197, PubMed:26406980). Also transports purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) (PubMed:21795683, PubMed:27995448). Mediates basolateral nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis barrier (By similarity). Regulates inosine levels in brown adipocytes tissues (BAT) and extracellular inosine levels, which controls BAT-dependent energy expenditure (PubMed:35790189).
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Uniprot ID
Primary ID:
Q99808

Secondarily ID:
B3KQV7
B3KQY5
Q5T9W9
Q9UJY2
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Ensembl ID
ENSG00000112759
HGNC ID
HGNC:11003
Subcellular Location
Basolateral cell membrane
Apical cell membrane
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: CL000448 , BxPC-3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0057024
 Compound Info 
med.21724, Compound Gemcitabine
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C9H11F2N3O4
  1
1
IC50 = 190 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0955356
 Compound Info 
N'-[(1S)-2-[[(1S)-5-amino-1-[[(1S)-1-[(2S)-2-[[(1S)-1-[[(1S)-1-carbamoyl-3-methylsulfanyl-propyl]carbamoyl]-2-methyl-propyl]carbamoyl]pyrrolidine-1-carbonyl]-3-methyl-butyl]carbamoyl]pentyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]-N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-2-oxo-pyrimidin-4-yl]butanediamide
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C51H74F2N12O12S
  1
1
IC50 = 380 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0968860
 Compound Info 
N'-[(1S)-2-[[(1S)-1-[(2S)-2-[[(1S,2R)-1-[[(1S)-1-[[(1S)-5-amino-1-carbamoyl-pentyl]carbamoyl]-3-methyl-butyl]carbamoyl]-2-hydroxy-propyl]carbamoyl]pyrrolidine-1-carbonyl]-2-methyl-propyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]-N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-2-oxo-pyrimidin-4-yl]butanediamide
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C50H72F2N12O13
  1
1
IC50 = 381 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0955875
 Compound Info 
N'-[(1S)-5-amino-1-[[(1S)-1-[(2S)-2-[[(1S)-1-[[(1S)-1-[[(1S)-2-amino-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]carbamoyl]-3-methylsulfanyl-propyl]carbamoyl]-2-methyl-propyl]carbamoyl]pyrrolidine-1-carbonyl]-3-methyl-butyl]carbamoyl]pentyl]-N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-2-oxo-pyrimidin-4-yl]butanediamide
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C51H74F2N12O12S
  1
1
IC50 = 384 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0961945
 Compound Info 
(2S)-N-[(1S,2R)-1-[[(1S)-1-[[(1S)-5-amino-1-carbamoyl-pentyl]carbamoyl]-3-methyl-butyl]carbamoyl]-2-hydroxy-propyl]-1-[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-methyl-butanoyl]pyrrolidine-2-carboxamide
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C37H59N9O7
  1
1
IC50 > 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0963259
 Compound Info 
(2S)-N-[(1S)-1-[[(1S)-1-[[(1S)-2-amino-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]carbamoyl]-3-methylsulfanyl-propyl]carbamoyl]-2-methyl-propyl]-1-[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-4-methyl-pentanoyl]pyrrolidine-2-carboxamide
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C38H61N9O6S
  1
1
IC50 > 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0967034
 Compound Info 
(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-4-methyl-pentanoyl]-N-[(1R)-1-[[(1S)-1-carbamoyl-3-methylsulfanyl-propyl]carbamoyl]-2-methyl-propyl]pyrrolidine-2-carboxamide
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C38H61N9O6S
  1
1
IC50 > 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000002 , K-562
 Cell Line Info 
Cell Line ID: CL000896 , PK15NTD
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0076031
 Compound Info 
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-(6-{[(4-nitrophenyl)methyl]sulfanyl}-9H-purin-9-yl)oxolane-3,4-diol
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C17H17N5O6S
  4
1 IC50 = 0.3 nM
2 IC50 = 8.511 nM
3 Ki = 0.7 nM
4 Ki = 0.7079 nM
CP0369407
 Compound Info 
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-(7-nitro-3,4-dihydro-1H-isoquinolin-2-yl)purin-9-yl]oxolane-3,4-diol
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C19H20N6O6
  1
1 IC50 = 5.495 nM
CP0359806
 Compound Info 
(2R,3R,4S,5R)-2-(6-(4-nitrobenzylthio)-2-amino-9H-purin-9-yl)-5-(hydroxymethyl)-tetrahydrofuran-3,4-diol
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C17H18N6O6S
  1
1 IC50 = 21.38 nM
CP0341342
 Compound Info 
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-(6-nitro-3,4-dihydro-1H-isoquinolin-2-yl)purin-9-yl]oxolane-3,4-diol
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C19H20N6O6
  1
1 IC50 = 181.97 nM
CP0156773
 Compound Info 
(1R,13R,14S,15R)-7-(7-nitro-3,4-dihydro-1H-isoquinolin-2-yl)-11,16-dioxa-2,4,6,9-tetrazatetracyclo[11.2.1.02,10.03,8]hexadeca-3(8),4,6,9-tetraene-14,15-diol
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C19H18N6O6
  1
1 IC50 = 331.13 nM
CP0347694
 Compound Info 
(2R,3R,4S,5R)-2-[6-(3,4-dihydro-1H-isoquinolin-2-yl)purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
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C19H21N5O4
  1
1 IC50 = 1819.7 nM
CP0208987
 Compound Info 
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-(5-nitro-3,4-dihydro-1H-isoquinolin-2-yl)purin-9-yl]oxolane-3,4-diol
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C19H20N6O6
  1
1 IC50 = 3019.95 nM
CP0341341
 Compound Info 
(2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-(8-nitro-3,4-dihydro-1H-isoquinolin-2-yl)purin-9-yl]oxolane-3,4-diol
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C19H20N6O6
  1
1 IC50 = 3630.78 nM
CP0789894
 Compound Info 
2-Hydroxymethyl-5-[6-(4-iodo-benzylsulfanyl)-purin-9-yl]-tetrahydro-furan-3,4-diol
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C17H17IN4O4S
  1
1 Ki = 3.802 nM
CP0673068
 Compound Info 
(2R,3R,4S,5R)-2-[6-(4-Fluoro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17FN4O4S
  1
1 Ki = 9.12 nM
CP0745773
 Compound Info 
(2R,3R,4S,5R)-2-[6-(4-Bromo-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17BrN4O4S
  1
1 Ki = 11.48 nM
CP0759038
 Compound Info 
2-[6-(3-Fluoro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17FN4O4S
  1
1 Ki = 12.88 nM
CP0772894
 Compound Info 
2-Hydroxymethyl-5-[6-(3-iodo-benzylsulfanyl)-purin-9-yl]-tetrahydro-furan-3,4-diol
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C17H17IN4O4S
  1
1 Ki = 13.8 nM
CP0648097
 Compound Info 
(2R,3R,4S,5R)-2-[6-(4-Chloro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17ClN4O4S
  1
1 Ki = 14.79 nM
CP0837409
 Compound Info 
2-[6-(3-Chloro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17ClN4O4S
  1
1 Ki = 18.2 nM
CP0759039
 Compound Info 
2-Hydroxymethyl-5-[6-(2-iodo-benzylsulfanyl)-purin-9-yl]-tetrahydro-furan-3,4-diol
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C17H17IN4O4S
  1
1 Ki = 19.5 nM
CP0787107
 Compound Info 
2-[6-(3-Bromo-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17BrN4O4S
  1
1 Ki = 20.89 nM
CP0661465
 Compound Info 
(2R,3R,4S,5R)-2-[6-(2-Fluoro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17FN4O4S
  1
1 Ki = 23.99 nM
CP0648095
 Compound Info 
(2R,3R,4S,5R)-2-[6-(2-Chloro-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17ClN4O4S
  1
1 Ki = 117.49 nM
CP0701187
 Compound Info 
2-[6-(2-Bromo-benzylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
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C17H17BrN4O4S
  1
1 Ki = 151.36 nM
Clinical Information about the Protein
Target 1 ( Solute carrier family 29 member 1 (SLC29A1) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Angina pectoris [ICD-11: BA40]
Approved Drug(s) 1 Approved Drug  1
1 LIDOFLAZINE
 Drug Info 
Approved
Angina pectoris