Details of the Target

General Information of Target

Target ID LDTP10985
Target Name Equilibrative nucleoside transporter 1 (SLC29A1)
Gene Name SLC29A1
Gene ID 2030
Synonyms
ENT1; Equilibrative nucleoside transporter 1; hENT1; Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter; Equilibrative NBMPR-sensitive nucleoside transporter; es nucleoside transporter; Nucleoside transporter, es-type; Solute carrier family 29 member 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSCAGAAAAPRLWRLRPGARRSLSAYGRRTSVRFRSSGMTLDNISRAAVDRIIRVDHAGE
YGANRIYAGQMAVLGRTSVGPVIQKMWDQEKDHLKKFNELMVTFRVRPTVLMPLWNVLGF
ALGAGTALLGKEGAMACTVAVEESIAHHYNNQIRTLMEEDPEKYEELLQLIKKFRDEELE
HHDIGLDHDAELAPAYAVLKSIIQAGCRVAIYLSERL
Target Type
Successful
Target Bioclass
Transporter and channel
Family
SLC29A/ENT transporter (TC 2.A.57) family
Subcellular location
Basolateral cell membrane
Function
Uniporter involved in the facilitative transport of nucleosides and nucleobases, and contributes to maintaining their cellular homeostasis. Functions as a Na(+)-independent transporter. Involved in the transport of nucleosides such as adenosine, guanosine, inosine, uridine, thymidine and cytidine. Also transports purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil). Mediates basolateral nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis barrier. Regulates inosine levels in brown adipocytes tissues (BAT) and extracellular inosine levels, which controls BAT-dependent energy expenditure.
TTD ID
T13491
Uniprot ID
Q99808
DrugMap ID
TTLXAKE
Ensemble ID
ENST00000371708.1
HGNC ID
HGNC:11003
ChEMBL ID
CHEMBL1997

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.L116P; p.A183V .
HEC1B SNV: p.A183V .
IGROV1 SNV: p.E313D .
MEWO SNV: p.P362L .
SW620 Insertion: p.Y409delinsTer .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CHEMBL5175495
 Probe Info  		8.80  LDD0196  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
CY4
 Probe Info  		100.00  LDD0244  [2]
YN-4
 Probe Info  		100.00  LDD0445  [3]
STPyne
 Probe Info  		K255(0.83)  LDD0277  [4]
Jackson_14
 Probe Info  		2.50  LDD0123  [5]
DBIA
 Probe Info  		C378(0.98)  LDD1507  [6]
m-APA
 Probe Info  		N.A.  LDD2231  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [8]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [8]
PAL-AfBPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C027
 Probe Info  		13.74  LDD1733  [9]
C158
 Probe Info  		11.88  LDD1838  [9]
C199
 Probe Info  		7.78  LDD1875  [9]
C231
 Probe Info  		11.39  LDD1904  [9]
C293
 Probe Info  		18.00  LDD1963  [9]
C296
 Probe Info  		12.91  LDD1966  [9]
C361
 Probe Info  		29.65  LDD2022  [9]
C362
 Probe Info  		27.47  LDD2023  [9]
C373
 Probe Info  		14.83  LDD2033  [9]
VE-P
 Probe Info  		N.A.  LDD0396  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C378(0.98)  LDD1507  [6]
 LDCM0215  AC10 HEK-293T C378(1.05)  LDD1508  [6]
 LDCM0226  AC11 HEK-293T C378(0.88)  LDD1509  [6]
 LDCM0237  AC12 HEK-293T C378(0.73)  LDD1510  [6]
 LDCM0270  AC15 HEK-293T C378(1.05)  LDD1513  [6]
 LDCM0276  AC17 HEK-293T C378(0.95)  LDD1515  [6]
 LDCM0277  AC18 HEK-293T C378(0.88)  LDD1516  [6]
 LDCM0278  AC19 HEK-293T C378(0.80)  LDD1517  [6]
 LDCM0279  AC2 HEK-293T C378(0.98)  LDD1518  [6]
 LDCM0280  AC20 HEK-293T C378(0.65)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C378(0.86)  LDD1520  [6]
 LDCM0283  AC23 HEK-293T C378(1.15)  LDD1522  [6]
 LDCM0284  AC24 HEK-293T C378(0.99)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C378(0.93)  LDD1524  [6]
 LDCM0286  AC26 HEK-293T C378(0.93)  LDD1525  [6]
 LDCM0287  AC27 HEK-293T C378(0.83)  LDD1526  [6]
 LDCM0288  AC28 HEK-293T C378(0.72)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C378(0.98)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C378(0.88)  LDD1529  [6]
 LDCM0292  AC31 HEK-293T C378(0.92)  LDD1531  [6]
 LDCM0293  AC32 HEK-293T C378(0.96)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C378(0.99)  LDD1533  [6]
 LDCM0295  AC34 HEK-293T C378(1.04)  LDD1534  [6]
 LDCM0296  AC35 HEK-293T C378(0.88)  LDD1535  [6]
 LDCM0297  AC36 HEK-293T C378(0.81)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C378(0.98)  LDD1537  [6]
 LDCM0300  AC39 HEK-293T C378(1.13)  LDD1539  [6]
 LDCM0301  AC4 HEK-293T C378(0.81)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C378(1.19)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C378(0.98)  LDD1542  [6]
 LDCM0304  AC42 HEK-293T C378(1.05)  LDD1543  [6]
 LDCM0305  AC43 HEK-293T C378(0.89)  LDD1544  [6]
 LDCM0306  AC44 HEK-293T C378(0.86)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C378(0.97)  LDD1546  [6]
 LDCM0309  AC47 HEK-293T C378(0.98)  LDD1548  [6]
 LDCM0310  AC48 HEK-293T C378(1.02)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C378(1.02)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C378(1.04)  LDD1551  [6]
 LDCM0313  AC50 HEK-293T C378(0.96)  LDD1552  [6]
 LDCM0314  AC51 HEK-293T C378(0.91)  LDD1553  [6]
 LDCM0315  AC52 HEK-293T C378(0.94)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C378(0.96)  LDD1555  [6]
 LDCM0318  AC55 HEK-293T C378(1.07)  LDD1557  [6]
 LDCM0319  AC56 HEK-293T C378(0.94)  LDD1558  [6]
 LDCM0320  AC57 HEK-293T C378(1.08)  LDD1559  [6]
 LDCM0321  AC58 HEK-293T C378(1.02)  LDD1560  [6]
 LDCM0322  AC59 HEK-293T C378(0.93)  LDD1561  [6]
 LDCM0324  AC60 HEK-293T C378(1.01)  LDD1563  [6]
 LDCM0325  AC61 HEK-293T C378(1.02)  LDD1564  [6]
 LDCM0327  AC63 HEK-293T C378(1.02)  LDD1566  [6]
 LDCM0328  AC64 HEK-293T C378(1.08)  LDD1567  [6]
 LDCM0334  AC7 HEK-293T C378(1.01)  LDD1568  [6]
 LDCM0345  AC8 HEK-293T C378(0.96)  LDD1569  [6]
 LDCM0248  AKOS034007472 HEK-293T C378(0.90)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C378(1.04)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C378(1.13)  LDD1514  [6]
 LDCM0371  CL102 HEK-293T C378(1.12)  LDD1575  [6]
 LDCM0375  CL106 HEK-293T C378(1.03)  LDD1579  [6]
 LDCM0379  CL11 HEK-293T C378(1.12)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C378(1.03)  LDD1584  [6]
 LDCM0384  CL114 HEK-293T C378(1.06)  LDD1588  [6]
 LDCM0388  CL118 HEK-293T C378(1.07)  LDD1592  [6]
 LDCM0390  CL12 HEK-293T C378(1.17)  LDD1594  [6]
 LDCM0393  CL122 HEK-293T C378(1.02)  LDD1597  [6]
 LDCM0397  CL126 HEK-293T C378(1.16)  LDD1601  [6]
 LDCM0401  CL14 HEK-293T C378(1.15)  LDD1605  [6]
 LDCM0404  CL17 HEK-293T C378(1.04)  LDD1608  [6]
 LDCM0405  CL18 HEK-293T C378(1.03)  LDD1609  [6]
 LDCM0406  CL19 HEK-293T C378(0.97)  LDD1610  [6]
 LDCM0407  CL2 HEK-293T C378(1.25)  LDD1611  [6]
 LDCM0408  CL20 HEK-293T C378(1.23)  LDD1612  [6]
 LDCM0409  CL21 HEK-293T C378(1.03)  LDD1613  [6]
 LDCM0411  CL23 HEK-293T C378(1.06)  LDD1615  [6]
 LDCM0412  CL24 HEK-293T C378(1.05)  LDD1616  [6]
 LDCM0414  CL26 HEK-293T C378(1.18)  LDD1618  [6]
 LDCM0417  CL29 HEK-293T C378(0.94)  LDD1621  [6]
 LDCM0419  CL30 HEK-293T C378(0.92)  LDD1623  [6]
 LDCM0420  CL31 HEK-293T C378(0.80)  LDD1624  [6]
 LDCM0421  CL32 HEK-293T C378(1.01)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C378(1.26)  LDD1626  [6]
 LDCM0424  CL35 HEK-293T C378(0.98)  LDD1628  [6]
 LDCM0425  CL36 HEK-293T C378(0.96)  LDD1629  [6]
 LDCM0431  CL41 HEK-293T C378(0.94)  LDD1635  [6]
 LDCM0432  CL42 HEK-293T C378(0.82)  LDD1636  [6]
 LDCM0433  CL43 HEK-293T C378(0.95)  LDD1637  [6]
 LDCM0434  CL44 HEK-293T C378(0.70)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C378(0.88)  LDD1639  [6]
 LDCM0437  CL47 HEK-293T C378(0.84)  LDD1641  [6]
 LDCM0438  CL48 HEK-293T C378(0.90)  LDD1642  [6]
 LDCM0440  CL5 HEK-293T C378(1.15)  LDD1644  [6]
 LDCM0441  CL50 HEK-293T C378(1.08)  LDD1645  [6]
 LDCM0444  CL53 HEK-293T C378(1.13)  LDD1647  [6]
 LDCM0445  CL54 HEK-293T C378(0.99)  LDD1648  [6]
 LDCM0446  CL55 HEK-293T C378(0.86)  LDD1649  [6]
 LDCM0447  CL56 HEK-293T C378(1.17)  LDD1650  [6]
 LDCM0448  CL57 HEK-293T C378(0.89)  LDD1651  [6]
 LDCM0450  CL59 HEK-293T C378(1.02)  LDD1653  [6]
 LDCM0451  CL6 HEK-293T C378(1.01)  LDD1654  [6]
 LDCM0452  CL60 HEK-293T C378(0.98)  LDD1655  [6]
 LDCM0454  CL62 HEK-293T C378(0.93)  LDD1657  [6]
 LDCM0457  CL65 HEK-293T C378(1.07)  LDD1660  [6]
 LDCM0458  CL66 HEK-293T C378(0.89)  LDD1661  [6]
 LDCM0459  CL67 HEK-293T C378(0.79)  LDD1662  [6]
 LDCM0460  CL68 HEK-293T C378(1.07)  LDD1663  [6]
 LDCM0461  CL69 HEK-293T C378(0.89)  LDD1664  [6]
 LDCM0462  CL7 HEK-293T C378(0.85)  LDD1665  [6]
 LDCM0464  CL71 HEK-293T C378(0.95)  LDD1667  [6]
 LDCM0465  CL72 HEK-293T C378(1.02)  LDD1668  [6]
 LDCM0467  CL74 HEK-293T C378(1.03)  LDD1670  [6]
 LDCM0470  CL77 HEK-293T C378(1.07)  LDD1673  [6]
 LDCM0471  CL78 HEK-293T C378(0.91)  LDD1674  [6]
 LDCM0472  CL79 HEK-293T C378(0.79)  LDD1675  [6]
 LDCM0473  CL8 HEK-293T C378(1.43)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C378(1.00)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C378(0.88)  LDD1678  [6]
 LDCM0477  CL83 HEK-293T C378(0.93)  LDD1680  [6]
 LDCM0478  CL84 HEK-293T C378(1.01)  LDD1681  [6]
 LDCM0480  CL86 HEK-293T C378(1.35)  LDD1683  [6]
 LDCM0483  CL89 HEK-293T C378(1.06)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C378(1.02)  LDD1687  [6]
 LDCM0485  CL90 HEK-293T C378(0.92)  LDD1688  [6]
 LDCM0486  CL91 HEK-293T C378(0.92)  LDD1689  [6]
 LDCM0487  CL92 HEK-293T C378(1.13)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C378(1.10)  LDD1691  [6]
 LDCM0490  CL95 HEK-293T C378(1.07)  LDD1693  [6]
 LDCM0491  CL96 HEK-293T C378(1.11)  LDD1694  [6]
 LDCM0493  CL98 HEK-293T C378(1.09)  LDD1696  [6]
 LDCM0625  F8 Ramos C378(1.96)  LDD2187  [11]
 LDCM0572  Fragment10 Ramos C378(0.42)  LDD2189  [11]
 LDCM0573  Fragment11 Ramos C378(0.27)  LDD2190  [11]
 LDCM0574  Fragment12 Ramos C378(0.51)  LDD2191  [11]
 LDCM0575  Fragment13 Ramos C378(0.43)  LDD2192  [11]
 LDCM0576  Fragment14 Ramos C378(11.11)  LDD2193  [11]
 LDCM0579  Fragment20 Ramos C378(0.88)  LDD2194  [11]
 LDCM0580  Fragment21 Ramos C378(0.45)  LDD2195  [11]
 LDCM0582  Fragment23 Ramos C378(0.84)  LDD2196  [11]
 LDCM0578  Fragment27 Ramos C378(0.41)  LDD2197  [11]
 LDCM0586  Fragment28 Ramos C378(0.89)  LDD2198  [11]
 LDCM0588  Fragment30 Ramos C378(0.40)  LDD2199  [11]
 LDCM0589  Fragment31 Ramos C378(0.39)  LDD2200  [11]
 LDCM0590  Fragment32 Ramos C378(0.31)  LDD2201  [11]
 LDCM0468  Fragment33 Ramos C378(0.39)  LDD2202  [11]
 LDCM0596  Fragment38 Ramos C378(11.04)  LDD2203  [11]
 LDCM0566  Fragment4 Ramos C378(0.86)  LDD2184  [11]
 LDCM0427  Fragment51 HEK-293T C378(1.00)  LDD1631  [6]
 LDCM0610  Fragment52 Ramos C378(1.08)  LDD2204  [11]
 LDCM0614  Fragment56 Ramos C378(0.61)  LDD2205  [11]
 LDCM0569  Fragment7 Ramos C378(1.04)  LDD2186  [11]
 LDCM0571  Fragment9 Ramos C378(1.10)  LDD2188  [11]
 LDCM0015  HNE MDA-MB-231 C378(1.26)  LDD0346  [11]
 LDCM0022  KB02 Ramos C378(0.86)  LDD2182  [11]
 LDCM0023  KB03 Ramos C378(13.33)  LDD2183  [11]
 LDCM0024  KB05 Ramos C378(3.80)  LDD2185  [11]
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 2.50  LDD0123  [5]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adenosine Small molecular drug DB00640
Cannabidiol Small molecular drug DB09061
Cytarabine Small molecular drug DB00987
Didanosine Small molecular drug DB00900
Ethanol Small molecular drug DB00898
Fludarabine Small molecular drug DB01073
Fluorouracil Small molecular drug DB00544
Fostamatinib Small molecular drug DB12010
Gemcitabine Small molecular drug DB00441
Lidoflazine Small molecular drug D0L7VL
Mercaptopurine Small molecular drug DB01033
Pemetrexed Small molecular drug DB00642
Ribavirin Small molecular drug DB00811
Tegafur-uracil Small molecular drug DB09327
Trifluridine Small molecular drug DB00432
Troglitazone Small molecular drug DB00197
Zalcitabine Small molecular drug DB00943
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
6-(4-nitro-benzylsulfanyl)-9-phenethyl-9h-purine Small molecular drug D0V8DJ
9-benzyl-6-(4-nitro-benzylsulfanyl)-9h-purine Small molecular drug D0I7ON
Dilazep Small molecular drug D00GUM
Kf24345 Small molecular drug D08GKT
N6-cyclopentyladenosine Small molecular drug D03RFA
Nabiximols Small molecular drug DB14011
Nbtgr Small molecular drug D09FHE
Nitrobenzylthioinosine Small molecular drug D0S0PI
S6-nitrobenzyl Mercaptopurine Riboside Small molecular drug D02TOP
Uridine Small molecular drug DB02745
[3h]Nitrobenzylmercaptopurine Ribonucleoside Small molecular drug D07EVI
Medical Cannabis . DB14009

References

1 Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20. ACS Med Chem Lett. 2022 Sep 26;13(10):1648-1654. doi: 10.1021/acsmedchemlett.2c00336. eCollection 2022 Oct 13.
2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
5 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
6 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
7 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
8 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
9 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
10 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
11 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578